Kathy Giacomini, PhD, BSPharm

Dean School of Pharmacy
Professor of Bioengineering and Therapeutic Sciences
Committee Members

The Giacomini research group focuses on expanding our understanding of membrane transporters. Membrane transporters are of great biological and pharmacological importance, as they play a major role in human physiology and in drug disposition and response. Major questions addressed in the laboratory include: What is the function of orphan membrane transporters? What is the in vivo role of membrane transporters in the disposition of endogenous solutes as well as in drug disposition and response? How does genetic variation in membrane transporters affect solute disposition, human disease and drug response? What are the structural determinants of specificity?

Dr. Kathy Giacomini is leading an effort to deorphan transporters in the Solute Carrier 22 Family, and to determine the clinical implications of specific genetic variants in membrane transporters. Research ventures, ranging from basic discovery to clinical studies, have demonstrated that common variants of membrane transporters contribute to differences in drug response in ethnically diverse populations. Ultimately, these studies will increase our knowledge of the genetic basis underlying drug response and will contribute to advancing the era of personalized medicine. Furthermore, our studies will elucidate the genetic mechanisms of decreased drug response and, ultimately, contribute to improving drug design for safe and effective treatments of subgroups of patients who do not respond to standard treatments.

Research in the laboratory focuses on drugs used in the treatment of diseases associated with metabolic syndrome. We are particularly interested in identifying the genetic determinants of the anti-diabetic drugs, metformin and sulfonylureas, highly prescribed drugs. In particular, our research focuses on discovering functional genetic variants that underlie variation in response to these drugs in large ethnically diverse patient populations. Finally, Kathy Giacomini and her collaborator, Russ Altman of Stanford University are the Co-PIs of the UCSF–Stanford Center of Excellence in Regulatory Sciences and Innovation (CERSI) funded by the Food and Drug Administration (FDA). Established in 2014 and renewed in 2021, the UCSF-Stanford CERSI aims to advance the field of regulatory sciences and improve the development and evaluation of diagnostics, therapeutics and medical devices. The UCSF-Stanford CERSI is the first FDA funded CERSI on the west coast and seeks to address key challenges related to education and research that will advance the discovery and development of medical products.

DEI Statement: As a biracial woman faculty member with ancestries in the Philippines and Europe, I am deeply committed to issues of diversity, equity and inclusion. I am a strong advocate for graduate students and postdocs of diverse ancestries and particularly under-represented minorities (URM). In my career, I have been the academic advisor for students who are URMs and who now have vibrant careers in academia and industry. My mentoring style is very personal. That is, I tailor my advising of each trainee to their career goals and aspirations, helping them to achieve these goals. On the recommendation of my students, I have institute diversity presentations as part of our regularly scheduled research group meetings. We begin each research group meeting with a diversity presentation, given by an individual group member, who describes some aspect of their cultural background. These are fun and educational and build an inclusive and welcoming environment in my laboratory. As the co-PI of the UCSF-Stanford Center of Excellence in Regulatory Sciences and Innovation, CERSI, we established a CERSI Diversity Scholars Program in 2021 and have now made four awards to the scholars (students or postdocs) at UCSF from diverse ethnic backgrounds. My personal goal is to promote diversity, equity and inclusion at UCSF.

Publications: 

A genome-wide association analysis reveals new pathogenic pathways in gout.

Nature genetics

Major TJ, Takei R, Matsuo H, Leask MP, Sumpter NA, Topless RK, Shirai Y, Wang W, Cadzow MJ, Phipps-Green AJ, Li Z, Ji A, Merriman ME, Morice E, Kelley EE, Wei WH, McCormick SPA, Bixley MJ, Reynolds RJ, Saag KG, Fadason T, Golovina E, O'Sullivan JM, Stamp LK, Dalbeth N, Abhishek A, Doherty M, Roddy E, Jacobsson LTH, Kapetanovic MC, Melander O, Andrés M, Pérez-Ruiz F, Torres RJ, Radstake T, Jansen TL, Janssen M, Joosten LAB, Liu R, Gaal OI, Crisan TO, Rednic S, Kurreeman F, Huizinga TWJ, Toes R, Lioté F, Richette P, Bardin T, Ea HK, Pascart T, McCarthy GM, Helbert L, Stiburková B, Tausche AK, Uhlig T, Vitart V, Boutin TS, Hayward C, Riches PL, Ralston SH, Campbell A, MacDonald TM, FAST Study Group, Nakayama A, Takada T, Nakatochi M, Shimizu S, Kawamura Y, Toyoda Y, Nakaoka H, Yamamoto K, Matsuo K, Shinomiya N, Ichida K, Japan Gout Genomics Consortium, Lee C, Asia Pacific Gout Consortium, Bradbury LA, Brown MA, Robinson PC, Buchanan RRC, Hill CL, Lester S, Smith MD, Rischmueller M, Choi HK, Stahl EA, Miner JN, Solomon DH, Cui J, Giacomini KM, Brackman DJ, Jorgenson EM, GlobalGout Genetics Consortium, Liu H, Susztak K, 23andMe Research Team, Shringarpure S, So A, Okada Y, Li C, Shi Y, Merriman TR

Is Pharmacogenetic Testing a Vital Tool for Enhancing Therapeutic Management of Patients Worldwide?

Clinical pharmacology and therapeutics

Giacomini KM, van der Graaf PH

Rare Diseases Linked to Mutations in Vitamin Transporters Expressed in the Human Blood-Brain Barrier.

Clinical pharmacology and therapeutics

Yee SW, Wang J, Giacomini KM

Proteomic Profiling Reveals Age-Related Changes in Transporter Proteins in the Human Blood-Brain Barrier.

bioRxiv : the preprint server for biology

Zhou X, Azimi M, Handin N, Riselli A, Vora B, Chun E, Yee SW, Artursson P, Giacomini KM

Report of the 2023-24 AACP Research and Graduate Affairs Committee.

American journal of pharmaceutical education

Patterson ME, Ellingrod VL, Feola DJ, Kunda NK, Mei KC, Oestreich JH, Farrell DF, Giacomini KM

Illuminating the function of the orphan transporter, SLC22A10, in humans and other primates.

Nature communications

Yee SW, Ferrández-Peral L, Alentorn-Moron P, Fontsere C, Ceylan M, Koleske ML, Handin N, Artegoitia VM, Lara G, Chien HC, Zhou X, Dainat J, Zalevsky A, Sali A, Brand CM, Wolfreys FD, Yang J, Gestwicki JE, Capra JA, Artursson P, Newman JW, Marquès-Bonet T, Giacomini KM

Haploinsufficiency underlies the neurodevelopmental consequences of SLC6A1 variants.

American journal of human genetics

Silva DB, Trinidad M, Ljungdahl A, Revalde JL, Berguig GY, Wallace W, Patrick CS, Bomba L, Arkin M, Dong S, Estrada K, Hutchinson K, LeBowitz JH, Schlessinger A, Johannesen KM, Møller RS, Giacomini KM, Froelich S, Sanders SJ, Wuster A

Effect of Antioxidants in Medicinal Products on Intestinal Drug Transporters.

Pharmaceutics

Kulkarni CP, Yang J, Koleske ML, Lara G, Alam K, Raw A, Rege B, Zhao L, Lu D, Zhang L, Yu LX, Lionberger RA, Giacomini KM, Kroetz DL, Yee SW

The full spectrum of SLC22 OCT1 mutations illuminates the bridge between drug transporter biophysics and pharmacogenomics.

Molecular cell

Yee SW, Macdonald CB, Mitrovic D, Zhou X, Koleske ML, Yang J, Buitrago Silva D, Rockefeller Grimes P, Trinidad DD, More SS, Kachuri L, Witte JS, Delemotte L, Giacomini KM, Coyote-Maestas W

Structural and molecular basis of choline uptake into the brain by FLVCR2.

Nature

Cater RJ, Mukherjee D, Gil-Iturbe E, Erramilli SK, Chen T, Koo K, Santander N, Reckers A, Kloss B, Gawda T, Choy BC, Zhang Z, Katewa A, Larpthaveesarp A, Huang EJ, Mooney SWJ, Clarke OB, Yee SW, Giacomini KM, Kossiakoff AA, Quick M, Arnold T, Mancia F

Genome-Wide Association Study Identifies Pharmacogenomic Variants Associated With Metformin Glycemic Response in African American Patients With Type 2 Diabetes.

Diabetes care

Wu B, Yee SW, Xiao S, Xu F, Sridhar SB, Yang M, Hochstadt S, Cabral W, Lanfear DE, Hedderson MM, Giacomini KM, Williams LK

Membrane transporters in drug development and as determinants of precision medicine.

Nature reviews. Drug discovery

Galetin A, Brouwer KLR, Tweedie D, Yoshida K, Sjöstedt N, Aleksunes L, Chu X, Evers R, Hafey MJ, Lai Y, Matsson P, Riselli A, Shen H, Sparreboom A, Varma MVS, Yang J, Yang X, Yee SW, Zamek-Gliszczynski MJ, Zhang L, Giacomini KM

Artificial intelligence, ChatGPT, and other large language models for social determinants of health: Current state and future directions.

Cell reports. Medicine

Ong JCL, Seng BJJ, Law JZF, Low LL, Kwa ALH, Giacomini KM, Ting DSW

Maximum likelihood estimation of renal transporter ontogeny profiles for pediatric PBPK modeling.

CPT: pharmacometrics & systems pharmacology

Hunt JP, Dubinsky S, McKnite AM, Cheung KWK, van Groen BD, Giacomini KM, de Wildt SN, Edginton AN, Watt KM

Illuminating the Function of the Orphan Transporter, SLC22A10 in Humans and Other Primates.

Research square

Giacomini K, Yee SW, Ferrández-Peral L, Alentorn P, Fontsere C, Ceylan M, Koleske M, Handin N, Artegoitia V, Lara G, Chien HC, Zhou X, Dainat J, Zalevsky A, Sali A, Brand C, Capra J, Artursson P, Newman J, Marques-Bonet T

TICBase: Integrated Resource for Data on Drug and Environmental Chemical Interactions with Mammalian Drug Transporters.

Clinical pharmacology and therapeutics

Michel ME, Wen CC, Yee SW, Giacomini KM, Hamdoun A, Nicklisch SCT

Illuminating the Function of the Orphan Transporter, SLC22A10 in Humans and Other Primates.

bioRxiv : the preprint server for biology

Yee SW, Ferrández-Peral L, Alentorn P, Fontsere C, Ceylan M, Koleske ML, Handin N, Artegoitia VM, Lara G, Chien HC, Zhou X, Dainat J, Zalevsky A, Sali A, Brand CM, Capra JA, Artursson P, Newman JW, Marques-Bonet T, Giacomini KM

Identification of Genetic Variation Influencing Metformin Response in a Multi-Ancestry Genome-Wide Association Study in the Diabetes Prevention Program (DPP).

Diabetes

Li JH, Perry JA, Jablonski KA, Srinivasan S, Chen L, Todd JN, Harden M, Mercader JM, Pan Q, Dawed AY, Yee SW, Pearson ER, Giacomini KM, Giri A, Hung AM, Xiao S, Williams LK, Franks PW, Hanson RL, Kahn SE, Knowler WC, Pollin TI, Florez JC, Diabetes Prevention Program Research Group

Cardiac contraction and relaxation are regulated by distinct subcellular cAMP pools.

Nature chemical biology

Lin TY, Mai QN, Zhang H, Wilson E, Chien HC, Yee SW, Giacomini KM, Olgin JE, Irannejad R

Trends in Clinical Pharmacology and Therapeutics.

Clinical pharmacology and therapeutics

Minichmayr IK, Smith DM, Giacomini KM, van der Graaf PH

The full spectrum of OCT1 (SLC22A1) mutations bridges transporter biophysics to drug pharmacogenomics.

bioRxiv : the preprint server for biology

Yee SW, Macdonald C, Mitrovic D, Zhou X, Koleske ML, Yang J, Silva DB, Grimes PR, Trinidad D, More SS, Kachuri L, Witte JS, Delemotte L, Giacomini KM, Coyote-Maestas W

The Effect of Trimethoprim on Thiamine Absorption: A Transporter-Mediated Drug-Nutrient Interaction.

Clinical pharmacology and therapeutics

Vora B, Wen A, Yee SW, Trinh K, Azimi M, Green EAE, Sirota M, Greenberg AS, Newman JW, Giacomini KM

Initial Insights into the Genetic Variation Associated with Metformin Treatment Failure in Youth with Type 2 Diabetes.

Pediatric diabetes

Srinivasan S, Chen L, Udler M, Todd J, Kelsey MM, Haymond MW, Arslanian S, Zeitler P, Gubitosi-Klug R, Nadeau KJ, Kutney K, White NH, Li JH, Perry JA, Kaur V, Brenner L, Mercader JM, Dawed A, Pearson ER, Yee SW, Giacomini KM, Pollin T, Florez JC

Characterization of P-glycoprotein orthologs from human, sheep, pig, dog, and cat.

Journal of veterinary pharmacology and therapeutics

Azimi M, Yee SW, Riselli A, Silva DB, Giacomini CP, Giacomini KM, Brett CM

Biomarkers Come of Age in Clinical Pharmacology.

Clinical pharmacology and therapeutics

Giacomini KM

Diversity, Equity, and Inclusion: Translating Clinical Pharmacology for All.

Clinical pharmacology and therapeutics

Venkatakrishnan K, Brown KE, Giacomini KM, van der Graaf PH

Functional genomics of OCTN2 variants informs protein-specific variant effect predictor for Carnitine Transporter Deficiency.

Proceedings of the National Academy of Sciences of the United States of America

Koleske ML, McInnes G, Brown JEH, Thomas N, Hutchinson K, Chin MY, Koehl A, Arkin MR, Schlessinger A, Gallagher RC, Song YS, Altman RB, Giacomini KM

More Than Pharmacokinetics: Transporters in Clinical Pharmacology.

Clinical pharmacology and therapeutics

Giacomini KM, Huang SM

New and Emerging Research on Solute Carrier and ATP Binding Cassette Transporters in Drug Discovery and Development: Outlook From the International Transporter Consortium.

Clinical pharmacology and therapeutics

Giacomini KM, Yee SW, Koleske ML, Zou L, Matsson P, Chen EC, Kroetz DL, Miller MA, Gozalpour E, Chu X

A Critical Overview of the Biological Effects of Excipients (Part I): Impact on Gastrointestinal Absorption.

The AAPS journal

Martinez MN, Sinko B, Wu F, Flanagan T, Borbás E, Tsakalozou E, Giacomini KM

Response to Comment on Dawed et al. Genome-Wide Meta-analysis Identifies Genetic Variants Associated With Glycemic Response to Sulfonylureas. Diabetes Care 2021;44:2673-2682.

Diabetes care

Dawed AY, Yee SW, Zhou K, van Leeuwen N, Zhang Y, Siddiqui MK, Etheridge A, Innocenti F, Xu F, Li JH, Beulens JW, van der Heijden AA, Slieker RC, Chang YC, Mercader JM, Kaur V, Witte JS, Lee MTM, Kamatani Y, Momozawa Y, Kubo M, Palmer CNA, Florez JC, Hedderson MM, 't Hart LM, Giacomini KM, Pearson ER, for MetGen Plus, for the DIRECT Consortium

The Clinical Pharmacogenetics Implementation Consortium Guideline for SLCO1B1, ABCG2, and CYP2C9 genotypes and Statin-Associated Musculoskeletal Symptoms.

Clinical pharmacology and therapeutics

Cooper-DeHoff RM, Niemi M, Ramsey LB, Luzum JA, Tarkiainen EK, Straka RJ, Gong L, Tuteja S, Wilke RA, Wadelius M, Larson EA, Roden DM, Klein TE, Yee SW, Krauss RM, Turner RM, Palaniappan L, Gaedigk A, Giacomini KM, Caudle KE, Voora D

The Pandemic as a Catalyst for Disruptive Innovation in Clinical Pharmacology.

Clinical pharmacology and therapeutics

Giacomini KM, van der Graaf PH

High Throughput Screening of a Prescription Drug Library for Inhibitors of Organic Cation Transporter 3, OCT3.

Pharmaceutical research

Chen EC, Matsson P, Azimi M, Zhou X, Handin N, Yee SW, Artursson P, Giacomini KM

Emerging Roles of the Human Solute Carrier 22 Family.

Drug metabolism and disposition: the biological fate of chemicals

Yee SW, Giacomini KM

Genome-Wide Meta-analysis Identifies Genetic Variants Associated With Glycemic Response to Sulfonylureas.

Diabetes care

Dawed AY, Yee SW, Zhou K, van Leeuwen N, Zhang Y, Siddiqui MK, Etheridge A, Innocenti F, Xu F, Li JH, Beulens JW, van der Heijden AA, Slieker RC, Chang YC, Mercader JM, Kaur V, Witte JS, Lee MTM, Kamatani Y, Momozawa Y, Kubo M, Palmer CNA, Florez JC, Hedderson MM, 't Hart LM, Giacomini KM, Pearson ER, for MetGen Plus, for the DIRECT Consortium, MetGen Plus investigators:

Interaction of Commonly Used Oral Molecular Excipients with P-glycoprotein.

The AAPS journal

Bajaj R, Chong LB, Zou L, Tsakalozou E, Ni Z, Giacomini KM, Kroetz DL

Advancing Precision Medicine Through the New Pharmacogenomics Global Research Network.

Clinical pharmacology and therapeutics

Giacomini KM, Karnes JH, Crews KR, Monte AA, Murphy WA, Oni-Orisan A, Ramsey LB, Yang JJ, Whirl-Carrillo M

Drugs in COVID19 clinical trials: Predicting transporter-mediated drug-drug interactions using in vitro assays and real-world data.

Clinical pharmacology and therapeutics

Yee SW, Vora B, Oskotsky TT, Zou L, Jakobsen S, Enogieru OJ, Koleske ML, Kosti I, Rödin M, Sirota M, Giacomini KM

Opportunities and challenges for the computational interpretation of rare variation in clinically important genes.

American journal of human genetics

McInnes G, Sharo AG, Koleske ML, Brown JEH, Norstad M, Adhikari AN, Wang S, Brenner SE, Halpern J, Koenig BA, Magnus DC, Gallagher RC, Giacomini KM, Altman RB

The Effects of Genetic Mutations and Drugs on the Activity of the Thiamine Transporter, SLC19A2.

The AAPS journal

Enogieru OJ, Koleske ML, Vora B, Ngo H, Yee SW, Chatad D, Sirota M, Giacomini KM

A New Era in Pharmacovigilance: Toward Real-World Data and Digital Monitoring.

Clinical pharmacology and therapeutics

Lavertu A, Vora B, Giacomini KM, Altman R, Rensi S

Characterization of cytochrome P450 (CYP) 2D6 drugs as substrates of human organic cation transporters and multidrug and toxin extrusion proteins.

British journal of pharmacology

Neul C, Hofmann U, Schaeffeler E, Winter S, Klein K, Giacomini KM, Eichelbaum M, Schwab M, Nies AT

Deorphaning a solute carrier 22 family member, SLC22A15, through functional genomic studies.

FASEB journal : official publication of the Federation of American Societies for Experimental Biology

Yee SW, Buitrago D, Stecula A, Ngo HX, Chien HC, Zou L, Koleske ML, Giacomini KM

A Tribute to Professor Per Artursson - Scientist, Explorer, Mentor, Innovator, and Giant in Pharmaceutical Research.

Journal of pharmaceutical sciences

Matsson P, Baranczewski P, Giacomini KM, Andersson TB, Palm J, Palm K, Charman WN, Bergström CAS

Drug Metabolites Potently Inhibit Renal Organic Anion Transporters, OAT1 and OAT3.

Journal of pharmaceutical sciences

Zou L, Matsson P, Stecula A, Ngo HX, Zur AA, Giacomini KM

Scientific considerations for global drug development.

Science translational medicine

Wilson JL, Cheung KWK, Lin L, Green EAE, Porrás AI, Zou L, Mukanga D, Akpa PA, Darko DM, Yuan R, Ding S, Johnson WCN, Lee HA, Cooke E, Peck CC, Kern SE, Hartman D, Hayashi Y, Marks PW, Altman RB, Lumpkin MM, Giacomini KM, Blaschke TF

The activities of drug inactive ingredients on biological targets.

Science (New York, N.Y.)

Pottel J, Armstrong D, Zou L, Fekete A, Huang XP, Torosyan H, Bednarczyk D, Whitebread S, Bhhatarai B, Liang G, Jin H, Ghaemi SN, Slocum S, Lukacs KV, Irwin JJ, Berg EL, Giacomini KM, Roth BL, Shoichet BK, Urban L

Neural production of kynurenic acid in Caenorhabditis elegans requires the AAT-1 transporter.

Genes & development

Lin L, Lemieux GA, Enogieru OJ, Giacomini KM, Ashrafi K

COVID-19: A Defining Moment for Clinical Pharmacology?

Clinical pharmacology and therapeutics

van der Graaf PH, Giacomini KM

Bacterial metabolism rescues the inhibition of intestinal drug absorption by food and drug additives.

Proceedings of the National Academy of Sciences of the United States of America

Zou L, Spanogiannopoulos P, Pieper LM, Chien HC, Cai W, Khuri N, Pottel J, Vora B, Ni Z, Tsakalozou E, Zhang W, Shoichet BK, Giacomini KM, Turnbaugh PJ

Oral Anticoagulants and Precision Medicine: Something Old, Something New.

Clinical pharmacology and therapeutics

Shahin MH, Giacomini KM

GenEpi: gene-based epistasis discovery using machine learning.

BMC bioinformatics

Chang YC, Wu JT, Hong MY, Tung YA, Hsieh PH, Yee SW, Giacomini KM, Oyang YJ, Chen CY, Alzheimer’s Disease Neuroimaging Initiative

Interactions of Oral Molecular Excipients with Breast Cancer Resistance Protein, BCRP.

Molecular pharmaceutics

Zou L, Pottel J, Khuri N, Ngo HX, Ni Z, Tsakalozou E, Warren MS, Huang Y, Shoichet BK, Giacomini KM

Clinical Pharmacology & Therapeutics 2030.

Clinical pharmacology and therapeutics

van der Graaf PH, Giacomini KM

Drug-nutrient interactions: discovering prescription drug inhibitors of the thiamine transporter ThTR-2 (SLC19A3).

The American journal of clinical nutrition

Vora B, Green EAE, Khuri N, Ballgren F, Sirota M, Giacomini KM

Expanding Precompetitive Multisector Collaborations to Advance Drug Development and Pharmacogenomics.

Clinical pharmacology and therapeutics

Yee SW, Do TP, Huang SM, Krauss RM, Kusuhara H, Sugiyama Y, Unadkat JD, Giacomini KM

Global Pharmacogenomics Within Precision Medicine: Challenges and Opportunities.

Clinical pharmacology and therapeutics

Chenoweth MJ, Giacomini KM, Pirmohamed M, Hill SL, van Schaik RHN, Schwab M, Shuldiner AR, Relling MV, Tyndale RF

Unraveling the functional role of the orphan solute carrier, SLC22A24 in the transport of steroid conjugates through metabolomic and genome-wide association studies.

PLoS genetics

Yee SW, Stecula A, Chien HC, Zou L, Feofanova EV, van Borselen M, Cheung KWK, Yousri NA, Suhre K, Kinchen JM, Boerwinkle E, Irannejad R, Yu B, Giacomini KM

A conserved role of the insulin-like signaling pathway in diet-dependent uric acid pathologies in Drosophila melanogaster.

PLoS genetics

Lang S, Hilsabeck TA, Wilson KA, Sharma A, Bose N, Brackman DJ, Beck JN, Chen L, Watson MA, Killilea DW, Ho S, Kahn A, Giacomini K, Stoller ML, Chi T, Kapahi P

A Comprehensive Analysis of Ontogeny of Renal Drug Transporters: mRNA Analyses, Quantitative Proteomics, and Localization.

Clinical pharmacology and therapeutics

Cheung KWK, van Groen BD, Spaans E, van Borselen MD, de Bruijn ACJM, Simons-Oosterhuis Y, Tibboel D, Samsom JN, Verdijk RM, Smeets B, Zhang L, Huang SM, Giacomini KM, de Wildt SN

l-Type amino acid transporter 1 activity of 1,2,3-triazolyl analogs of l-histidine and l-tryptophan.

Bioorganic & medicinal chemistry letters

Hall C, Wolfe H, Wells A, Chien HC, Colas C, Schlessinger A, Giacomini KM, Thomas AA

Genome-Wide Association and Functional Studies Reveal Novel Pharmacological Mechanisms for Allopurinol.

Clinical pharmacology and therapeutics

Brackman DJ, Yee SW, Enogieru OJ, Shaffer C, Ranatunga D, Denny JC, Wei WQ, Kamatani Y, Kubo M, Roden DM, Jorgenson E, Giacomini KM

Organic Anion Transporter Polypeptide 1B1 Polymorphism Modulates the Extent of Drug-Drug Interaction and Associated Biomarker Levels in Healthy Volunteers.

Clinical and translational science

Yee SW, Giacomini MM, Shen H, Humphreys WG, Horng H, Brian W, Lai Y, Kroetz DL, Giacomini KM

Impact of Pharmaceutical Excipients on Oral Drug Absorption: A Focus on Intestinal Drug Transporters.

Clinical pharmacology and therapeutics

Zou L, Ni Z, Tsakalozou E, Giacomini KM

Organic cation transporter 3 (Oct3) is a distinct catecholamines clearance route in adipocytes mediating the beiging of white adipose tissue.

PLoS biology

Song W, Luo Q, Zhang Y, Zhou L, Liu Y, Ma Z, Guo J, Huang Y, Cheng L, Meng Z, Li Z, Zhang B, Li S, Yee SW, Fan H, Li P, Giacomini KM, Chen L

Clinical Probes and Endogenous Biomarkers as Substrates for Transporter Drug-Drug Interaction Evaluation: Perspectives From the International Transporter Consortium.

Clinical pharmacology and therapeutics

Chu X, Liao M, Shen H, Yoshida K, Zur AA, Arya V, Galetin A, Giacomini KM, Hanna I, Kusuhara H, Lai Y, Rodrigues D, Sugiyama Y, Zamek-Gliszczynski MJ, Zhang L, International Transporter Consortium

The International Transporter Consortium: Summarizing Advances in the Role of Transporters in Drug Development.

Clinical pharmacology and therapeutics

Giacomini KM, Galetin A, Huang SM

Reevaluating the Substrate Specificity of the L-Type Amino Acid Transporter (LAT1).

Journal of medicinal chemistry

Chien HC, Colas C, Finke K, Springer S, Stoner L, Zur AA, Venteicher B, Campbell J, Hall C, Flint A, Augustyn E, Hernandez C, Heeren N, Hansen L, Anthony A, Bauer J, Fotiadis D, Schlessinger A, Giacomini KM, Thomas AA

Transporters in Drug Development: 2018 ITC Recommendations for Transporters of Emerging Clinical Importance.

Clinical pharmacology and therapeutics

Zamek-Gliszczynski MJ, Taub ME, Chothe PP, Chu X, Giacomini KM, Kim RB, Ray AS, Stocker SL, Unadkat JD, Wittwer MB, Xia C, Yee SW, Zhang L, Zhang Y, International Transporter Consortium

Influence of Transporter Polymorphisms on Drug Disposition and Response: A Perspective From the International Transporter Consortium.

Clinical pharmacology and therapeutics

Yee SW, Brackman DJ, Ennis EA, Sugiyama Y, Kamdem LK, Blanchard R, Galetin A, Zhang L, Giacomini KM

ITC Commentary on Metformin Clinical Drug-Drug Interaction Study Design That Enables an Efficacy- and Safety-Based Dose Adjustment Decision.

Clinical pharmacology and therapeutics

Zamek-Gliszczynski MJ, Chu X, Cook JA, Custodio JM, Galetin A, Giacomini KM, Lee CA, Paine MF, Ray AS, Ware JA, Wittwer MB, Zhang L, International Transporter Consortium

Pharmacogenetics of Antidiabetic Drugs.

Advances in pharmacology (San Diego, Calif.)

Srinivasan S, Yee SW, Giacomini KM

Molecular Mechanisms for Species Differences in Organic Anion Transporter 1, OAT1: Implications for Renal Drug Toxicity.

Molecular pharmacology

Zou L, Stecula A, Gupta A, Prasad B, Chien HC, Yee SW, Wang L, Unadkat JD, Stahl SH, Fenner KS, Giacomini KM

Organic cation transporter 1 (OCT1) modulates multiple cardiometabolic traits through effects on hepatic thiamine content.

PLoS biology

Liang X, Yee SW, Chien HC, Chen EC, Luo Q, Zou L, Piao M, Mifune A, Chen L, Calvert ME, King S, Norheim F, Abad J, Krauss RM, Giacomini KM

Genetic Variants in CPA6 and PRPF31 Are Associated With Variation in Response to Metformin in Individuals With Type 2 Diabetes.

Diabetes

Rotroff DM, Yee SW, Zhou K, Marvel SW, Shah HS, Jack JR, Havener TM, Hedderson MM, Kubo M, Herman MA, Gao H, Mychaleckyi JC, McLeod HL, Doria A, Giacomini KM, Pearson ER, Wagner MJ, Buse JB, Motsinger-Reif AA, MetGen Investigators, ACCORD/ACCORDion Investigators

Reverse Translational Research of ABCG2 (BCRP) in Human Disease and Drug Response.

Clinical pharmacology and therapeutics

Brackman DJ, Giacomini KM

PharmGKB summary: very important pharmacogene information for ABCG2.

Pharmacogenetics and genomics

Fohner AE, Brackman DJ, Giacomini KM, Altman RB, Klein TE

New Pharmacogenomics Research Network: An Open Community Catalyzing Research and Translation in Precision Medicine.

Clinical pharmacology and therapeutics

Relling MV, Krauss RM, Roden DM, Klein TE, Fowler DM, Terada N, Lin L, Riel-Mehan M, Do TP, Kubo M, Yee SW, Johnson GT, Giacomini KM

PBPK Modeling of the Effect of Reduced Kidney Function on the Pharmacokinetics of Drugs Excreted Renally by Organic Anion Transporters.

Clinical pharmacology and therapeutics

Hsueh CH, Hsu V, Zhao P, Zhang L, Giacomini KM, Huang SM

Human Concentrative Nucleoside Transporter 3 (hCNT3, SLC28A3) Forms a Cyclic Homotrimer.

Biochemistry

Stecula A, Schlessinger A, Giacomini KM, Sali A

Computational Discovery and Experimental Validation of Inhibitors of the Human Intestinal Transporter OATP2B1.

Journal of chemical information and modeling

Khuri N, Zur AA, Wittwer MB, Lin L, Yee SW, Sali A, Giacomini KM

Transporters Involved in Metformin Pharmacokinetics and Treatment Response.

Journal of pharmaceutical sciences

Liang X, Giacomini KM

The Effect of Uremic Solutes on the Organic Cation Transporter 2.

Journal of pharmaceutical sciences

Cheung KWK, Hsueh CH, Zhao P, Meyer TW, Zhang L, Huang SM, Giacomini KM

Discovery of Competitive and Noncompetitive Ligands of the Organic Cation Transporter 1 (OCT1; SLC22A1).

Journal of medicinal chemistry

Chen EC, Khuri N, Liang X, Stecula A, Chien HC, Yee SW, Huang Y, Sali A, Giacomini KM

Variants in Pharmacokinetic Transporters and Glycemic Response to Metformin: A Metgen Meta-Analysis.

Clinical pharmacology and therapeutics

Dujic T, Zhou K, Yee SW, van Leeuwen N, de Keyser CE, Javorský M, Goswami S, Zaharenko L, Hougaard Christensen MM, Out M, Tavendale R, Kubo M, Hedderson MM, van der Heijden AA, Klimcáková L, Pirags V, Kooy A, Brøsen K, Klovins J, Semiz S, Tkác I, Stricker BH, Palmer C, 't Hart LM, Giacomini KM, Pearson ER

Genomic Characterization of Metformin Hepatic Response.

PLoS genetics

Luizon MR, Eckalbar WL, Wang Y, Jones SL, Smith RP, Laurance M, Lin L, Gallins PJ, Etheridge AS, Wright F, Zhou Y, Molony C, Innocenti F, Yee SW, Giacomini KM, Ahituv N

Genome-wide association studies of drug response and toxicity: an opportunity for genome medicine.

Nature reviews. Drug discovery

Giacomini KM, Yee SW, Mushiroda T, Weinshilboum RM, Ratain MJ, Kubo M

The use of drug transporters as therapeutic targets.

Clinical advances in hematology & oncology : H&O

Giacomini KM

A Molecular Basis for Innovation in Drug Excipients.

Clinical pharmacology and therapeutics

Irwin JJ, Pottel J, Zou L, Wen H, Zuk S, Zhang X, Sterling T, Shoichet BK, Lionberger R, Giacomini KM

A Longitudinal HbA1c Model Elucidates Genes Linked to Disease Progression on Metformin.

Clinical pharmacology and therapeutics

Goswami S, Yee SW, Xu F, Sridhar SB, Mosley JD, Takahashi A, Kubo M, Maeda S, Davis RL, Roden DM, Hedderson MM, Giacomini KM, Savic RM

Metabolomic and Genome-wide Association Studies Reveal Potential Endogenous Biomarkers for OATP1B1.

Clinical pharmacology and therapeutics

Yee SW, Giacomini MM, Hsueh CH, Weitz D, Liang X, Goswami S, Kinchen JM, Coelho A, Zur AA, Mertsch K, Brian W, Kroetz DL, Giacomini KM

LAT1 activity of carboxylic acid bioisosteres: Evaluation of hydroxamic acids as substrates.

Bioorganic & medicinal chemistry letters

Zur AA, Chien HC, Augustyn E, Flint A, Heeren N, Finke K, Hernandez C, Hansen L, Miller S, Lin L, Giacomini KM, Colas C, Schlessinger A, Thomas AA

Identification and Quantitative Assessment of Uremic Solutes as Inhibitors of Renal Organic Anion Transporters, OAT1 and OAT3.

Molecular pharmaceutics

Hsueh CH, Yoshida K, Zhao P, Meyer TW, Zhang L, Huang SM, Giacomini KM

Variation in the glucose transporter gene SLC2A2 is associated with glycemic response to metformin.

Nature genetics

Zhou K, Yee SW, Seiser EL, van Leeuwen N, Tavendale R, Bennett AJ, Groves CJ, Coleman RL, van der Heijden AA, Beulens JW, de Keyser CE, Zaharenko L, Rotroff DM, Out M, Jablonski KA, Chen L, Javorský M, Židzik J, Levin AM, Williams LK, Dujic T, Semiz S, Kubo M, Chien HC, Maeda S, Witte JS, Wu L, Tkác I, Kooy A, van Schaik RHN, Stehouwer CDA, Logie L, MetGen Investigators, DPP Investigators, ACCORD Investigators, Sutherland C, Klovins J, Pirags V, Hofman A, Stricker BH, Motsinger-Reif AA, Wagner MJ, Innocenti F, 't Hart LM, Holman RR, McCarthy MI, Hedderson MM, Palmer CNA, Florez JC, Giacomini KM, Pearson ER

Genomewide Association Studies in Pharmacogenomics: Meeting Report of the NIH Pharmacogenomics Research Network-RIKEN (PGRN-RIKEN) Collaboration.

Clinical pharmacology and therapeutics

Yee SW, Momozawa Y, Kamatani Y, Tyndale RF, Weinshilboum RM, Ratain MJ, Giacomini KM, Kubo M

Erratum to: Vesicular monoamine transporter protein expression correlates with clinical features, tumor biology, and MIBG avidity in neuroblastoma: a report from the Children's Oncology Group.

European journal of nuclear medicine and molecular imaging

Temple W, Mendelsohn L, Kim GE, Nekritz E, Gustafson WC, Lin L, Giacomini K, Naranjo A, Van Ryn C, Parisi MT, Shulkin BL, Yanik GA, Kreissman SG, Hogarty M, Matthay KK, DuBois SG

Pharmacometabolomic Assessment of Metformin in Non-diabetic, African Americans.

Frontiers in pharmacology

Rotroff DM, Oki NO, Liang X, Yee SW, Stocker SL, Corum DG, Meisner M, Fiehn O, Motsinger-Reif AA, Giacomini KM, Kaddurah-Daouk R

The Effect of Famotidine, a MATE1-Selective Inhibitor, on the Pharmacokinetics and Pharmacodynamics of Metformin.

Clinical pharmacokinetics

Hibma JE, Zur AA, Castro RA, Wittwer MB, Keizer RJ, Yee SW, Goswami S, Stocker SL, Zhang X, Huang Y, Brett CM, Savic RM, Giacomini KM

A research roadmap for next-generation sequencing informatics.

Science translational medicine

Altman RB, Prabhu S, Sidow A, Zook JM, Goldfeder R, Litwack D, Ashley E, Asimenos G, Bustamante CD, Donigan K, Giacomini KM, Johansen E, Khuri N, Lee E, Liang XS, Salit M, Serang O, Tezak Z, Wall DP, Mansfield E, Kass-Hout T

LAT-1 activity of meta-substituted phenylalanine and tyrosine analogs.

Bioorganic & medicinal chemistry letters

Augustyn E, Finke K, Zur AA, Hansen L, Heeren N, Chien HC, Lin L, Giacomini KM, Colas C, Schlessinger A, Thomas AA

The Effect of Nizatidine, a MATE2K Selective Inhibitor, on the Pharmacokinetics and Pharmacodynamics of Metformin in Healthy Volunteers.

Clinical pharmacokinetics

Morrissey KM, Stocker SL, Chen EC, Castro RA, Brett CM, Giacomini KM

Transcriptomic variation of pharmacogenes in multiple human tissues and lymphoblastoid cell lines.

The pharmacogenomics journal

Chhibber A, French CE, Yee SW, Gamazon ER, Theusch E, Qin X, Webb A, Papp AC, Wang A, Simmons CQ, Konkashbaev A, Chaudhry AS, Mitchel K, Stryke D, Ferrin TE, Weiss ST, Kroetz DL, Sadee W, Nickerson DA, Krauss RM, George AL, Schuetz EG, Medina MW, Cox NJ, Scherer SE, Giacomini KM, Brenner SE

Rapid Method To Determine Intracellular Drug Concentrations in Cellular Uptake Assays: Application to Metformin in Organic Cation Transporter 1-Transfected Human Embryonic Kidney 293 Cells.

Drug metabolism and disposition: the biological fate of chemicals

Chien HC, Zur AA, Maurer TS, Yee SW, Tolsma J, Jasper P, Scott DO, Giacomini KM

Unmet needs: Research helps regulators do their jobs.

Science translational medicine

Altman RB, Khuri N, Salit M, Giacomini KM

Metformin Is a Substrate and Inhibitor of the Human Thiamine Transporter, THTR-2 (SLC19A3).

Molecular pharmaceutics

Liang X, Chien HC, Yee SW, Giacomini MM, Chen EC, Piao M, Hao J, Twelves J, Lepist EI, Ray AS, Giacomini KM

Vesicular monoamine transporter protein expression correlates with clinical features, tumor biology, and MIBG avidity in neuroblastoma: a report from the Children's Oncology Group.

European journal of nuclear medicine and molecular imaging

Temple W, Mendelsohn L, Kim GE, Nekritz E, Gustafson WC, Lin L, Giacomini K, Naranjo A, Van Ryn C, Yanik GA, Kreissman SG, Hogarty M, Matthay KK, DuBois SG

Prediction and validation of enzyme and transporter off-targets for metformin.

Journal of pharmacokinetics and pharmacodynamics

Yee SW, Lin L, Merski M, Keiser MJ, Gupta A, Zhang Y, Chien HC, Shoichet BK, Giacomini KM

SLC transporters as therapeutic targets: emerging opportunities.

Nature reviews. Drug discovery

Lin L, Yee SW, Kim RB, Giacomini KM

Targeted disruption of organic cation transporter 3 attenuates the pharmacologic response to metformin.

Molecular pharmacology

Chen EC, Liang X, Yee SW, Geier EG, Stocker SL, Chen L, Giacomini KM

Genome-wide association study identifies ABCG2 (BCRP) as an allopurinol transporter and a determinant of drug response.

Clinical pharmacology and therapeutics

Wen CC, Yee SW, Liang X, Hoffmann TJ, Kvale MN, Banda Y, Jorgenson E, Schaefer C, Risch N, Giacomini KM

Phase I Study of Vorinostat as a Radiation Sensitizer with 131I-Metaiodobenzylguanidine (131I-MIBG) for Patients with Relapsed or Refractory Neuroblastoma.

Clinical cancer research : an official journal of the American Association for Cancer Research

DuBois SG, Groshen S, Park JR, Haas-Kogan DA, Yang X, Geier E, Chen E, Giacomini K, Weiss B, Cohn SL, Granger MM, Yanik GA, Hawkins R, Courtier J, Jackson H, Goodarzian F, Shimada H, Czarnecki S, Tsao-Wei D, Villablanca JG, Marachelian A, Matthay KK

A pharmacogenetic candidate gene study of tenofovir-associated Fanconi syndrome.

Pharmacogenetics and genomics

Dahlin A, Wittwer M, de la Cruz M, Woo JM, Bam R, Scharen-Guivel V, Flaherty J, Ray AS, Cihlar T, Gupta SK, Giacomini KM

OCT1 in hepatic steatosis and thiamine disposition.

Cell cycle (Georgetown, Tex.)

Chen L, Yee SW, Giacomini KM

Genome-wide discovery of drug-dependent human liver regulatory elements.

PLoS genetics

Smith RP, Eckalbar WL, Morrissey KM, Luizon MR, Hoffmann TJ, Sun X, Jones SL, Force Aldred S, Ramamoorthy A, Desta Z, Liu Y, Skaar TC, Trinklein ND, Giacomini KM, Ahituv N

Metformin pharmacogenomics: current status and future directions.

Diabetes

Pawlyk AC, Giacomini KM, McKeon C, Shuldiner AR, Florez JC

OCT1 is a high-capacity thiamine transporter that regulates hepatic steatosis and is a target of metformin.

Proceedings of the National Academy of Sciences of the United States of America

Chen L, Shu Y, Liang X, Chen EC, Yee SW, Zur AA, Li S, Xu L, Keshari KR, Lin MJ, Chien HC, Zhang Y, Morrissey KM, Liu J, Ostrem J, Younger NS, Kurhanewicz J, Shokat KM, Ashrafi K, Giacomini KM

PharmGKB summary: very important pharmacogene information for SLC22A1.

Pharmacogenetics and genomics

Goswami S, Gong L, Giacomini K, Altman RB, Klein TE

Genetic variants in transcription factors are associated with the pharmacokinetics and pharmacodynamics of metformin.

Clinical pharmacology and therapeutics

Goswami S, Yee SW, Stocker S, Mosley JD, Kubo M, Castro R, Mefford JA, Wen C, Liang X, Witte J, Brett C, Maeda S, Simpson MD, Hedderson MM, Davis RL, Roden DM, Giacomini KM, Savic RM

Clinical Pharmacogenetics Implementation Consortium (CPIC) guidelines for ivacaftor therapy in the context of CFTR genotype.

Clinical pharmacology and therapeutics

Clancy JP, Johnson SG, Yee SW, McDonagh EM, Caudle KE, Klein TE, Cannavo M, Giacomini KM, Clinical Pharmacogenetics Implementation Consortium

Profiling solute carrier transporters in the human blood-brain barrier.

Clinical pharmacology and therapeutics

Geier EG, Chen EC, Webb A, Papp AC, Yee SW, Sadee W, Giacomini KM

A genome-wide association study of bronchodilator response in Latinos implicates rare variants.

The Journal of allergy and clinical immunology

Drake KA, Torgerson DG, Gignoux CR, Galanter JM, Roth LA, Huntsman S, Eng C, Oh SS, Yee SW, Lin L, Bustamante CD, Moreno-Estrada A, Sandoval K, Davis A, Borrell LN, Farber HJ, Kumar R, Avila PC, Brigino-Buenaventura E, Chapela R, Ford JG, Lenoir MA, Lurmann F, Meade K, Serebrisky D, Thyne S, Rodríguez-Cintrón W, Sen S, Rodríguez-Santana JR, Hernandez RD, Giacomini KM, Burchard EG

International Transporter Consortium commentary on clinically important transporter polymorphisms.

Clinical pharmacology and therapeutics

Giacomini KM, Balimane PV, Cho SK, Eadon M, Edeki T, Hillgren KM, Huang SM, Sugiyama Y, Weitz D, Wen Y, Xia CQ, Yee SW, Zimdahl H, Niemi M, International Transporter Consortium

SLC classification: an update.

Clinical pharmacology and therapeutics

Schlessinger A, Yee SW, Sali A, Giacomini KM

Transporters in drug development and clinical pharmacology.

Clinical pharmacology and therapeutics

Giacomini KM, Huang SM

Special Section on Pharmacogenomics: recent advances and future directions.

Journal of human genetics

Mushiroda T, Giacomini KM, Kubo M

Impact of polymorphisms in drug pathway genes on disease-free survival in adults with acute myeloid leukemia.

Journal of human genetics

Yee SW, Mefford JA, Singh N, Percival ME, Stecula A, Yang K, Witte JS, Takahashi A, Kubo M, Matsuda K, Giacomini KM, Andreadis C

Reduced renal clearance of cefotaxime in asians with a low-frequency polymorphism of OAT3 (SLC22A8).

Journal of pharmaceutical sciences

Yee SW, Nguyen AN, Brown C, Savic RM, Zhang Y, Castro RA, Cropp CD, Choi JH, Singh D, Tahara H, Stocker SL, Huang Y, Brett CM, Giacomini KM

Emerging transporters of clinical importance: an update from the International Transporter Consortium.

Clinical pharmacology and therapeutics

Hillgren KM, Keppler D, Zur AA, Giacomini KM, Stieger B, Cass CE, Zhang L, International Transporter Consortium

Structure-based ligand discovery for the Large-neutral Amino Acid Transporter 1, LAT-1.

Proceedings of the National Academy of Sciences of the United States of America

Geier EG, Schlessinger A, Fan H, Gable JE, Irwin JJ, Sali A, Giacomini KM

Gene expression profiling of transporters in the solute carrier and ATP-binding cassette superfamilies in human eye substructures.

Molecular pharmaceutics

Dahlin A, Geier E, Stocker SL, Cropp CD, Grigorenko E, Bloomer M, Siegenthaler J, Xu L, Basile AS, Tang-Liu DD, Giacomini KM

Discovery of potent, selective multidrug and toxin extrusion transporter 1 (MATE1, SLC47A1) inhibitors through prescription drug profiling and computational modeling.

Journal of medicinal chemistry

Wittwer MB, Zur AA, Khuri N, Kido Y, Kosaka A, Zhang X, Morrissey KM, Sali A, Huang Y, Giacomini KM

Molecular modeling and ligand docking for solute carrier (SLC) transporters.

Current topics in medicinal chemistry

Schlessinger A, Khuri N, Giacomini KM, Sali A

Renal transporters in drug development.

Annual review of pharmacology and toxicology

Morrissey KM, Stocker SL, Wittwer MB, Xu L, Giacomini KM

Highlights from the International Transporter Consortium second workshop.

Clinical pharmacology and therapeutics

Zamek-Gliszczynski MJ, Hoffmaster KA, Tweedie DJ, Giacomini KM, Hillgren KM

Metformin pathways: pharmacokinetics and pharmacodynamics.

Pharmacogenetics and genomics

Gong L, Goswami S, Giacomini KM, Altman RB, Klein TE

The UCSF-FDA TransPortal: a public drug transporter database.

Clinical pharmacology and therapeutics

Morrissey KM, Wen CC, Johns SJ, Zhang L, Huang SM, Giacomini KM

The effect of novel promoter variants in MATE1 and MATE2 on the pharmacokinetics and pharmacodynamics of metformin.

Clinical pharmacology and therapeutics

Stocker SL, Morrissey KM, Yee SW, Castro RA, Xu L, Dahlin A, Ramirez AH, Roden DM, Wilke RA, McCarty CA, Davis RL, Brett CM, Giacomini KM

Pharmacogenomics and patient care: one size does not fit all.

Science translational medicine

Giacomini KM, Yee SW, Ratain MJ, Weinshilboum RM, Kamatani N, Nakamura Y

Evaluation of Norepinephrine Transporter Expression and Metaiodobenzylguanidine Avidity in Neuroblastoma: A Report from the Children's Oncology Group.

International journal of molecular imaging

Dubois SG, Geier E, Batra V, Yee SW, Neuhaus J, Segal M, Martinez D, Pawel B, Yanik G, Naranjo A, London WB, Kreissman S, Baker D, Attiyeh E, Hogarty MD, Maris JM, Giacomini K, Matthay KK

High selectivity of the γ-aminobutyric acid transporter 2 (GAT-2, SLC6A13) revealed by structure-based approach.

The Journal of biological chemistry

Schlessinger A, Wittwer MB, Dahlin A, Khuri N, Bonomi M, Fan H, Giacomini KM, Sali A

Dedication to professor Leslie Z. Benet: 50 years of scientific excellence and still going strong!

Pharmaceutical research

Smith DE, Rowland M, Giacomini KM, Amidon GL

Genetic and epigenetic regulation of the organic cation transporter 3, SLC22A3.

The pharmacogenomics journal

Chen L, Hong C, Chen EC, Yee SW, Xu L, Almof EU, Wen C, Fujii K, Johns SJ, Stryke D, Ferrin TE, Simko J, Chen X, Costello JF, Giacomini KM

Rare versus common variants in pharmacogenetics: SLCO1B1 variation and methotrexate disposition.

Genome research

Ramsey LB, Bruun GH, Yang W, Treviño LR, Vattathil S, Scheet P, Cheng C, Rosner GL, Giacomini KM, Fan Y, Sparreboom A, Mikkelsen TS, Corydon TJ, Pui CH, Evans WE, Relling MV

A genome-wide association study of overall survival in pancreatic cancer patients treated with gemcitabine in CALGB 80303.

Clinical cancer research : an official journal of the American Association for Cancer Research

Innocenti F, Owzar K, Cox NL, Evans P, Kubo M, Zembutsu H, Jiang C, Hollis D, Mushiroda T, Li L, Friedman P, Wang L, Glubb D, Hurwitz H, Giacomini KM, McLeod HL, Goldberg RM, Schilsky RL, Kindler HL, Nakamura Y, Ratain MJ

PharmGKB summary: methotrexate pathway.

Pharmacogenetics and genomics

Mikkelsen TS, Thorn CF, Yang JJ, Ulrich CM, French D, Zaza G, Dunnenberger HM, Marsh S, McLeod HL, Giacomini K, Becker ML, Gaedigk R, Leeder JS, Kager L, Relling MV, Evans W, Klein TE, Altman RB

A common 5'-UTR variant in MATE2-K is associated with poor response to metformin.

Clinical pharmacology and therapeutics

Choi JH, Yee SW, Ramirez AH, Morrissey KM, Jang GH, Joski PJ, Mefford JA, Hesselson SE, Schlessinger A, Jenkins G, Castro RA, Johns SJ, Stryke D, Sali A, Ferrin TE, Witte JS, Kwok PY, Roden DM, Wilke RA, McCarty CA, Davis RL, Giacomini KM

Structure-based discovery of prescription drugs that interact with the norepinephrine transporter, NET.

Proceedings of the National Academy of Sciences of the United States of America

Schlessinger A, Geier E, Fan H, Irwin JJ, Shoichet BK, Giacomini KM, Sali A

Interaction of sirolimus and everolimus with hepatic and intestinal organic anion-transporting polypeptide transporters.

Xenobiotica; the fate of foreign compounds in biological systems

Picard N, Levoir L, Lamoureux F, Yee SW, Giacomini KM, Marquet P

Vorinostat increases expression of functional norepinephrine transporter in neuroblastoma in vitro and in vivo model systems.

Clinical cancer research : an official journal of the American Association for Cancer Research

More SS, Itsara M, Yang X, Geier EG, Tadano MK, Seo Y, Vanbrocklin HF, Weiss WA, Mueller S, Haas-Kogan DA, Dubois SG, Matthay KK, Giacomini KM

Discovery of regulatory elements in human ATP-binding cassette transporters through expression quantitative trait mapping.

The pharmacogenomics journal

Matsson P, Yee SW, Markova S, Morrissey K, Jenkins G, Xuan J, Jorgenson E, Kroetz DL, Giacomini KM

Functional characterization of liver enhancers that regulate drug-associated transporters.

Clinical pharmacology and therapeutics

Kim MJ, Skewes-Cox P, Fukushima H, Hesselson S, Yee SW, Ramsey LB, Nguyen L, Eshragh JL, Castro RA, Wen CC, Stryke D, Johns SJ, Ferrin TE, Kwok PY, Relling MV, Giacomini KM, Kroetz DL, Ahituv N

GABAA receptor open-state conformation determines non-competitive antagonist binding.

Toxicology and applied pharmacology

Chen L, Xue L, Giacomini KM, Casida JE

Consequences of POR mutations and polymorphisms.

Molecular and cellular endocrinology

Miller WL, Agrawal V, Sandee D, Tee MK, Huang N, Choi JH, Morrissey K, Giacomini KM

Effects of genetic variants of human P450 oxidoreductase on catalysis by CYP2D6 in vitro.

Pharmacogenetics and genomics

Sandee D, Morrissey K, Agrawal V, Tam HK, Kramer MA, Tracy TS, Giacomini KM, Miller WL

Role of organic cation transporter 3 (SLC22A3) and its missense variants in the pharmacologic action of metformin.

Pharmacogenetics and genomics

Chen L, Pawlikowski B, Schlessinger A, More SS, Stryke D, Johns SJ, Portman MA, Chen E, Ferrin TE, Sali A, Giacomini KM

SLC19A1 pharmacogenomics summary.

Pharmacogenetics and genomics

Yee SW, Gong L, Badagnani I, Giacomini KM, Klein TE, Altman RB

Substrate-specific modulation of CYP3A4 activity by genetic variants of cytochrome P450 oxidoreductase.

Pharmacogenetics and genomics

Agrawal V, Choi JH, Giacomini KM, Miller WL

Genetic variants of human organic anion transporter 4 demonstrate altered transport of endogenous substrates.

American journal of physiology. Renal physiology

Shima JE, Komori T, Taylor TR, Stryke D, Kawamoto M, Johns SJ, Carlson EJ, Ferrin TE, Giacomini KM

Genetic polymorphisms in organic cation transporter 1 (OCT1) in Chinese and Japanese populations exhibit altered function.

The Journal of pharmacology and experimental therapeutics

Chen L, Takizawa M, Chen E, Schlessinger A, Segenthelar J, Choi JH, Sali A, Kubo M, Nakamura S, Iwamoto Y, Iwasaki N, Giacomini KM

Role of the copper transporter, CTR1, in platinum-induced ototoxicity.

The Journal of neuroscience : the official journal of the Society for Neuroscience

More SS, Akil O, Ianculescu AG, Geier EG, Lustig LR, Giacomini KM

Genotype-dependent effects of inhibitors of the organic cation transporter, OCT1: predictions of metformin interactions.

The pharmacogenomics journal

Ahlin G, Chen L, Lazorova L, Chen Y, Ianculescu AG, Davis RL, Giacomini KM, Artursson P

Organic cation transporters modulate the uptake and cytotoxicity of picoplatin, a third-generation platinum analogue.

Molecular cancer therapeutics

More SS, Li S, Yee SW, Chen L, Xu Z, Jablons DM, Giacomini KM

Pharmacogenomics of membrane transporters: past, present and future.

Pharmacogenomics

Yee SW, Chen L, Giacomini KM

Transport of thyroid hormones is selectively inhibited by 3-iodothyronamine.

Molecular bioSystems

Ianculescu AG, Friesema EC, Visser TJ, Giacomini KM, Scanlan TS

Comparison of human solute carriers.

Protein science : a publication of the Protein Society

Schlessinger A, Matsson P, Shima JE, Pieper U, Yee SW, Kelly L, Apeltsin L, Stroud RM, Ferrin TE, Giacomini KM, Sali A

Membrane transporters in drug development.

Nature reviews. Drug discovery

International Transporter Consortium, Giacomini KM, Huang SM, Tweedie DJ, Benet LZ, Brouwer KL, Chu X, Dahlin A, Evers R, Fischer V, Hillgren KM, Hoffmaster KA, Ishikawa T, Keppler D, Kim RB, Lee CA, Niemi M, Polli JW, Sugiyama Y, Swaan PW, Ware JA, Wright SH, Yee SW, Zamek-Gliszczynski MJ, Zhang L

Germline genetic variation in an organic anion transporter polypeptide associated with methotrexate pharmacokinetics and clinical effects.

Journal of clinical oncology : official journal of the American Society of Clinical Oncology

Treviño LR, Shimasaki N, Yang W, Panetta JC, Cheng C, Pei D, Chan D, Sparreboom A, Giacomini KM, Pui CH, Evans WE, Relling MV

The role of organic anion-transporting polypeptides and their common genetic variants in mycophenolic acid pharmacokinetics.

Clinical pharmacology and therapeutics

Picard N, Yee SW, Woillard JB, Lebranchu Y, Le Meur Y, Giacomini KM, Marquet P

Identification and characterization of novel polymorphisms in the basal promoter of the human transporter, MATE1.

Pharmacogenetics and genomics

Ha Choi J, Wah Yee S, Kim MJ, Nguyen L, Ho Lee J, Kang JO, Hesselson S, Castro RA, Stryke D, Johns SJ, Kwok PY, Ferrin TE, Goo Lee M, Black BL, Ahituv N, Giacomini KM

A survey of integral alpha-helical membrane proteins.

Journal of structural and functional genomics

Kelly L, Pieper U, Eswar N, Hays FA, Li M, Roe-Zurz Z, Kroetz DL, Giacomini KM, Stroud RM, Sali A

Genetic variation in the proximal promoter of ABC and SLC superfamilies: liver and kidney specific expression and promoter activity predict variation.

PloS one

Hesselson SE, Matsson P, Shima JE, Fukushima H, Yee SW, Kobayashi Y, Gow JM, Ha C, Ma B, Poon A, Johns SJ, Stryke D, Castro RA, Tahara H, Choi JH, Chen L, Picard N, Sjödin E, Roelofs MJ, Ferrin TE, Myers R, Kroetz DL, Kwok PY, Giacomini KM

Effect of genetic variation in the organic cation transporter 2 on the renal elimination of metformin.

Pharmacogenetics and genomics

Chen Y, Li S, Brown C, Cheatham S, Castro RA, Leabman MK, Urban TJ, Chen L, Yee SW, Choi JH, Huang Y, Brett CM, Burchard EG, Giacomini KM

The organic cation transporter, OCTN1, expressed in the human heart, potentiates antagonism of the HERG potassium channel.

Journal of cardiovascular pharmacology

McBride BF, Yang T, Liu K, Urban TJ, Giacomini KM, Kim RB, Roden DM

Genetic variants in multidrug and toxic compound extrusion-1, hMATE1, alter transport function.

The pharmacogenomics journal

Chen Y, Teranishi K, Li S, Yee SW, Hesselson S, Stryke D, Johns SJ, Ferrin TE, Kwok P, Giacomini KM

Functional genetic variation in the basal promoter of the organic cation/carnitine transporters OCTN1 (SLC22A4) and OCTN2 (SLC22A5).

The Journal of pharmacology and experimental therapeutics

Tahara H, Yee SW, Urban TJ, Hesselson S, Castro RA, Kawamoto M, Stryke D, Johns SJ, Ferrin TE, Kwok PY, Giacomini KM

Identification and characterization of proximal promoter polymorphisms in the human concentrative nucleoside transporter 2 (SLC28A2).

The Journal of pharmacology and experimental therapeutics

Yee SW, Shima JE, Hesselson S, Nguyen L, De Val S, Lafond RJ, Kawamoto M, Johns SJ, Stryke D, Kwok PY, Ferrin TE, Black BL, Gurwitz D, Ahituv N, Giacomini KM

Identification and characterization of 3-iodothyronamine intracellular transport.

Endocrinology

Ianculescu AG, Giacomini KM, Scanlan TS

Selecting optimum eukaryotic integral membrane proteins for structure determination by rapid expression and solubilization screening.

Journal of molecular biology

Li M, Hays FA, Roe-Zurz Z, Vuong L, Kelly L, Ho CM, Robbins RM, Pieper U, O'Connell JD, Miercke LJ, Giacomini KM, Sali A, Stroud RM

Genetic variation in human P450 oxidoreductase.

Molecular and cellular endocrinology

Miller WL, Huang N, Agrawal V, Giacomini KM

Pharm. D. pathways to biomedical research: the National Institutes of Health special conference on pharmacy research.

Pharmacotherapy

Figg WD, Chau CH, Okita R, Preusch P, Tracy TS, McLeod H, Reed M, Pieper J, Knoell D, Miller K, Speedie M, Blouin R, Kroboth P, Koda-Kimble MA, Taylor P, Cohen J, Giacomini K

cis-Diammine(pyridine)chloroplatinum(II), a monofunctional platinum(II) antitumor agent: Uptake, structure, function, and prospects.

Proceedings of the National Academy of Sciences of the United States of America

Lovejoy KS, Todd RC, Zhang S, McCormick MS, D'Aquino JA, Reardon JT, Sancar A, Giacomini KM, Lippard SJ

Creating and evaluating genetic tests predictive of drug response.

Nature reviews. Drug discovery

Weiss ST, McLeod HL, Flockhart DA, Dolan ME, Benowitz NL, Johnson JA, Ratain MJ, Giacomini KM

Genetic variation in drug transporters in ethnic populations.

Clinical pharmacology and therapeutics

Cropp CD, Yee SW, Giacomini KM

Novel variants in human Aquaporin-4 reduce cellular water permeability.

Human molecular genetics

Sorani MD, Zador Z, Hurowitz E, Yan D, Giacomini KM, Manley GT

The human multidrug resistance protein 4 (MRP4, ABCC4): functional analysis of a highly polymorphic gene.

The Journal of pharmacology and experimental therapeutics

Abla N, Chinn LW, Nakamura T, Liu L, Huang CC, Johns SJ, Kawamoto M, Stryke D, Taylor TR, Ferrin TE, Giacomini KM, Kroetz DL

Genetics of P450 oxidoreductase: sequence variation in 842 individuals of four ethnicities and activities of 15 missense mutations.

Proceedings of the National Academy of Sciences of the United States of America

Huang N, Agrawal V, Giacomini KM, Miller WL

Organic anion transporter 2 (SLC22A7) is a facilitative transporter of cGMP.

Molecular pharmacology

Cropp CD, Komori T, Shima JE, Urban TJ, Yee SW, More SS, Giacomini KM

Identifying genetic risk factors for serious adverse drug reactions: current progress and challenges.

Nature reviews. Drug discovery

Wilke RA, Lin DW, Roden DM, Watkins PB, Flockhart D, Zineh I, Giacomini KM, Krauss RM

Functional effects of protein sequence polymorphisms in the organic cation/ergothioneine transporter OCTN1 (SLC22A4).

Pharmacogenetics and genomics

Urban TJ, Yang C, Lagpacan LL, Brown C, Castro RA, Taylor TR, Huang CC, Stryke D, Johns SJ, Kawamoto M, Carlson EJ, Ferrin TE, Burchard EG, Giacomini KM

Effect of genetic variation in the organic cation transporter 1, OCT1, on metformin pharmacokinetics.

Clinical pharmacology and therapeutics

Shu Y, Brown C, Castro RA, Shi RJ, Lin ET, Owen RP, Sheardown SA, Yue L, Burchard EG, Brett CM, Giacomini KM

Effects of genetic variation in the novel organic cation transporter, OCTN1, on the renal clearance of gabapentin.

Clinical pharmacology and therapeutics

Urban TJ, Brown C, Castro RA, Shah N, Mercer R, Huang Y, Brett CM, Burchard EG, Giacomini KM

Transport of paraquat by human organic cation transporters and multidrug and toxic compound extrusion family.

The Journal of pharmacology and experimental therapeutics

Chen Y, Zhang S, Sorani M, Giacomini KM

Effect of genetic variation in the organic cation transporter 1 (OCT1) on metformin action.

The Journal of clinical investigation

Shu Y, Sheardown SA, Brown C, Owen RP, Zhang S, Castro RA, Ianculescu AG, Yue L, Lo JC, Burchard EG, Brett CM, Giacomini KM

Genetic nondiscrimination legislation: a critical prerequisite for pharmacogenomics data sharing.

Pharmacogenomics

Altman RB, Benowitz N, Gurwitz D, Lunshof J, Relling M, Lamba J, Wieben E, Mooney S, Giacomini K, Weiss S, Johnson JA, McLeod H, Flockhart D, Weinshilboum R, Shuldiner AR, Roden D, Krauss RM, Ratain M

When good drugs go bad.

Nature

Giacomini KM, Krauss RM, Roden DM, Eichelbaum M, Hayden MR, Nakamura Y

The pharmacogenetics research network: from SNP discovery to clinical drug response.

Clinical pharmacology and therapeutics

Giacomini KM, Brett CM, Altman RB, Benowitz NL, Dolan ME, Flockhart DA, Johnson JA, Hayes DF, Klein T, Krauss RM, Kroetz DL, McLeod HL, Nguyen AT, Ratain MJ, Relling MV, Reus V, Roden DM, Schaefer CA, Shuldiner AR, Skaar T, Tantisira K, Tyndale RF, Wang L, Weinshilboum RM, Weiss ST, Zineh I, Pharmacogenetics Research Network

Pharmacogenomics: challenges and opportunities.

Annals of internal medicine

Roden DM, Altman RB, Benowitz NL, Flockhart DA, Giacomini KM, Johnson JA, Krauss RM, McLeod HL, Ratain MJ, Relling MV, Ring HZ, Shuldiner AR, Weinshilboum RM, Weiss ST, Pharmacogenetics Research Network

Organic cation transporters are determinants of oxaliplatin cytotoxicity.

Cancer research

Zhang S, Lovejoy KS, Shima JE, Lagpacan LL, Shu Y, Lapuk A, Chen Y, Komori T, Gray JW, Chen X, Lippard SJ, Giacomini KM

Functional genetic diversity in the high-affinity carnitine transporter OCTN2 (SLC22A5).

Molecular pharmacology

Urban TJ, Gallagher RC, Brown C, Castro RA, Lagpacan LL, Brett CM, Taylor TR, Carlson EJ, Ferrin TE, Burchard EG, Packman S, Giacomini KM

Interaction of methotrexate with organic-anion transporting polypeptide 1A2 and its genetic variants.

The Journal of pharmacology and experimental therapeutics

Badagnani I, Castro RA, Taylor TR, Brett CM, Huang CC, Stryke D, Kawamoto M, Johns SJ, Ferrin TE, Carlson EJ, Burchard EG, Giacomini KM

PharmGKB submission update: IV. PMT submissions of genetic variations in ATP-Binding cassette transporters to the PharmGKB network.

Pharmacological reviews

Nguyen TD, Gow JM, Chinn LW, Kelly L, Jeong H, Huang CC, Stryke D, Kawamoto M, Johns SJ, Carlson E, Taylor T, Ferrin TE, Sali A, Giacomini KM, Kroetz DL

PharmGKB submission update: V. PMT submissions of genetic variation in SLC22 family transporters.

Pharmacological reviews

Shu Y, Urban TJ, Leabman MK, Fujita T, Erdman AR, Lagpacan LL, Brown C, Castro RA, Huang CC, Stryke D, Kawamoto M, Johns SJ, Taylor TR, Chan W, De La Cruz M, Carlson EJ, Ferrin TE, Brett CM, Burchard EG, Herskowitz I, Kroetz DL, Giacomini KM

PharmGKB submission update: VI. PMT submissions of genetic variations in neurotransmitter transporters (SLC6, SLC17, and SLC18) to the PharmGKB network.

Pharmacological reviews

Badagnani I, Sorani M, Edwards RH, Brown C, Castro RA, Huang CC, Stryke D, Kawamoto M, Johns SJ, Carlson EJ, Taylor T, Chan W, De La Cruz M, Ferrin TE, Burchard EG, Herskowitz I, Kroetz DL, Giacomini KM

Transport of drugs in the kidney by the human organic cation transporter, OCT2 and its genetic variants.

Journal of pharmaceutical sciences

Fujita T, Urban TJ, Leabman MK, Fujita K, Giacomini KM

Functional genomics of membrane transporters in human populations.

Genome research

Urban TJ, Sebro R, Hurowitz EH, Leabman MK, Badagnani I, Lagpacan LL, Risch N, Giacomini KM

The human organic anion transporter 3 (OAT3; SLC22A8): genetic variation and functional genomics.

American journal of physiology. Renal physiology

Erdman AR, Mangravite LM, Urban TJ, Lagpacan LL, Castro RA, de la Cruz M, Chan W, Huang CC, Johns SJ, Kawamoto M, Stryke D, Taylor TR, Carlson EJ, Ferrin TE, Brett CM, Burchard EG, Giacomini KM

Functional characterization and haplotype analysis of polymorphisms in the human equilibrative nucleoside transporter, ENT2.

Drug metabolism and disposition: the biological fate of chemicals

Owen RP, Lagpacan LL, Taylor TR, De La Cruz M, Huang CC, Kawamoto M, Johns SJ, Stryke D, Ferrin TE, Giacomini KM

Functional analysis of polymorphisms in the organic anion transporter, SLC22A6 (OAT1).

Pharmacogenetics and genomics

Fujita T, Brown C, Carlson EJ, Taylor T, de la Cruz M, Johns SJ, Stryke D, Kawamoto M, Fujita K, Castro R, Chen CW, Lin ET, Brett CM, Burchard EG, Ferrin TE, Huang CC, Leabman MK, Giacomini KM

Genetic analysis and functional characterization of polymorphisms in the human concentrative nucleoside transporter, CNT2.

Pharmacogenetics and genomics

Owen RP, Gray JH, Taylor TR, Carlson EJ, Huang CC, Kawamoto M, Johns SJ, Stryke D, Ferrin TE, Giacomini KM

Enhancing data sharing in collaborative research projects with DASH.

Pacific Symposium on Biocomputing. Pacific Symposium on Biocomputing

Ferrin TE, Huang CC, Greenblatt DM, Stryke D, Giacomini KM, Morris JH

Functional analysis of genetic variants in the human concentrative nucleoside transporter 3 (CNT3; SLC28A3).

The pharmacogenomics journal

Badagnani I, Chan W, Castro RA, Brett CM, Huang CC, Stryke D, Kawamoto M, Johns SJ, Ferrin TE, Carlson EJ, Burchard EG, Giacomini KM

PharmGKB update: III. Genetic variants of SLC22A1, solute carrier family 22 (organic cation transporter), member 1.

Pharmacological reviews

Shu Y, Leabman MK, Feng B, Mangravite LM, Huang CC, Stryke D, Kawamoto M, Johns SJ, DeYoung J, Carlson E, Ferrin TE, Herskowitz I, Giacomini KM

Functional and genetic diversity in the concentrative nucleoside transporter, CNT1, in human populations.

Molecular pharmacology

Gray JH, Mangravite LM, Owen RP, Urban TJ, Chan W, Carlson EJ, Huang CC, Kawamoto M, Johns SJ, Stryke D, Ferrin TE, Giacomini KM

Nucleoside transporters in the disposition and targeting of nucleoside analogs in the kidney.

European journal of pharmacology

Mangravite LM, Badagnani I, Giacomini KM

Sequence diversity and haplotype structure in the human ABCB1 (MDR1, multidrug resistance transporter) gene.

Pharmacogenetics

Kroetz DL, Pauli-Magnus C, Hodges LM, Huang CC, Kawamoto M, Johns SJ, Stryke D, Ferrin TE, DeYoung J, Taylor T, Carlson EJ, Herskowitz I, Giacomini KM, Clark AG, Pharmacogenetics of Membrane Transporters Investigators

PharmGKB update: I. Genetic variants of the organic cation transporter 2 (OCT2, SLC22A2).

Pharmacological reviews

Leabman MK, Huang CC, Stryke D, Johns SJ, Kawamoto M, Ferrin TE, DeYoung J, Taylor TR, De La Cruz M, Herskowitz I, Giacomini KM

The concentrative nucleoside transporter family, SLC28.

Pflugers Archiv : European journal of physiology

Gray JH, Owen RP, Giacomini KM

Functional characterization in yeast of genetic variants in the human equilibrative nucleoside transporter, ENT1.

Pharmacogenetics

Osato DH, Huang CC, Kawamoto M, Johns SJ, Stryke D, Wang J, Ferrin TE, Herskowitz I, Giacomini KM

Evolutionary conservation predicts function of variants of the human organic cation transporter, OCT1.

Proceedings of the National Academy of Sciences of the United States of America

Shu Y, Leabman MK, Feng B, Mangravite LM, Huang CC, Stryke D, Kawamoto M, Johns SJ, DeYoung J, Carlson E, Ferrin TE, Herskowitz I, Giacomini KM, Pharmacogenetics Of Membrane Transporters Investigators

Natural variation in human membrane transporter genes reveals evolutionary and functional constraints.

Proceedings of the National Academy of Sciences of the United States of America

Leabman MK, Huang CC, DeYoung J, Carlson EJ, Taylor TR, de la Cruz M, Johns SJ, Stryke D, Kawamoto M, Urban TJ, Kroetz DL, Ferrin TE, Clark AG, Risch N, Herskowitz I, Giacomini KM

Sorting of rat SPNT in renal epithelium is independent of N-glycosylation.

Pharmaceutical research

Mangravite LM, Giacomini KM

Localization of human equilibrative nucleoside transporters, hENT1 and hENT2, in renal epithelial cells.

American journal of physiology. Renal physiology

Mangravite LM, Xiao G, Giacomini KM

SNP analysis and presentation in the Pharmacogenetics of Membrane Transporters Project.

Pacific Symposium on Biocomputing. Pacific Symposium on Biocomputing

Stryke D, Huang CC, Kawamoto M, Johns SJ, Carlson EJ, Deyoung JA, Leabman MK, Herskowitz I, Giacomini KM, Ferrin TE

Interactions of n-tetraalkylammonium compounds and biguanides with a human renal organic cation transporter (hOCT2).

Pharmaceutical research

Dresser MJ, Xiao G, Leabman MK, Gray AT, Giacomini KM

Specificity of human and rat orthologs of the concentrative nucleoside transporter, SPNT.

American journal of physiology. Renal physiology

Gerstin KM, Dresser MJ, Giacomini KM

Polymorphisms in a human kidney xenobiotic transporter, OCT2, exhibit altered function.

Pharmacogenetics

Leabman MK, Huang CC, Kawamoto M, Johns SJ, Stryke D, Ferrin TE, DeYoung J, Taylor T, Clark AG, Herskowitz I, Giacomini KM, Pharmacogenetics of Membrane Transporters Investigators

Functional characteristics and steroid hormone-mediated regulation of an organic cation transporter in Madin-Darby canine kidney cells.

The Journal of pharmacology and experimental therapeutics

Shu Y, Bello CL, Mangravite LM, Feng B, Giacomini KM

Localization of GFP-tagged concentrative nucleoside transporters in a renal polarized epithelial cell line.

American journal of physiology. Renal physiology

Mangravite LM, Lipschutz JH, Mostov KE, Giacomini KM

Screening a large reference sample to identify very low frequency sequence variants: comparisons between two genes.

Nature genetics

Glatt CE, DeYoung JA, Delgado S, Service SK, Giacomini KM, Edwards RH, Risch N, Freimer NB

A novel proton-dependent nucleoside transporter, CeCNT3, from Caenorhabditis elegans.

Molecular pharmacology

Xiao G, Wang J, Tangen T, Giacomini KM

Electrophysiological analysis of the substrate selectivity of a sodium-coupled nucleoside transporter (rCNT1) expressed in Xenopus laevis oocytes.

Drug metabolism and disposition: the biological fate of chemicals

Dresser MJ, Gerstin KM, Gray AT, Loo DD, Giacomini KM

Molecular cloning of a Na+-dependent nucleoside transporter from rabbit intestine.

Pharmaceutical research

Gerstin KM, Dresser MJ, Wang J, Giacomini KM

Interactions of HIV protease inhibitors with a human organic cation transporter in a mammalian expression system.

Drug metabolism and disposition: the biological fate of chemicals

Zhang L, Gorset W, Washington CB, Blaschke TF, Kroetz DL, Giacomini KM

Kinetic and selectivity differences between rodent, rabbit, and human organic cation transporters (OCT1).

The Journal of pharmacology and experimental therapeutics

Dresser MJ, Gray AT, Giacomini KM

Functional characterization of a human purine-selective, Na+-dependent nucleoside transporter (hSPNT1) in a mammalian expression system.

The Journal of pharmacology and experimental therapeutics

Schaner ME, Wang J, Zhang L, Su SF, Gerstin KM, Giacomini KM

The interaction of n-tetraalkylammonium compounds with a human organic cation transporter, hOCT1.

The Journal of pharmacology and experimental therapeutics

Zhang L, Gorset W, Dresser MJ, Giacomini KM

Molecular and functional characteristics of cloned human organic cation transporters.

Pharmaceutical biotechnology

Dresser MJ, Zhang L, Giacomini KM

Functional characterization of an organic cation transporter (hOCT1) in a transiently transfected human cell line (HeLa).

The Journal of pharmacology and experimental therapeutics

Zhang L, Schaner ME, Giacomini KM

Nucleoside transport in isolated human and rhesus choroid plexus tissue slices.

Pharmaceutical research

Washington CB, Giacomini KM, Brett CM

Nicotine transport in a human choriocarcinoma cell line (JAR).

Journal of pharmaceutical sciences

Zevin S, Schaner ME, Giacomini KM

Molecular cloning and functional expression of a rabbit renal organic cation transporter.

Biochimica et biophysica acta

Terashita S, Dresser MJ, Zhang L, Gray AT, Yost SC, Giacomini KM

Role of organic cation transporters in drug absorption and elimination.

Annual review of pharmacology and toxicology

Zhang L, Brett CM, Giacomini KM

Membrane transporters in drug disposition.

Journal of pharmacokinetics and biopharmaceutics

Giacomini KM

Na(+)-dependent purine nucleoside transporter from human kidney: cloning and functional characterization.

The American journal of physiology

Wang J, Su SF, Dresser MJ, Schaner ME, Washington CB, Giacomini KM

Na+-dependent gamma-aminobutyric acid (GABA) transport in the choroid plexus of rabbit.

Biochimica et biophysica acta

Ramanathan VK, Brett CM, Giacomini KM

Functional and molecular characteristics of Na(+)-dependent nucleoside transporters.

Pharmaceutical research

Wang J, Schaner ME, Thomassen S, Su SF, Piquette-Miller M, Giacomini KM

Transient expression of a purine-selective nucleoside transporter (SPNTint) in a human cell line (HeLa).

Pharmaceutical research

Schaner ME, Wang J, Zevin S, Gerstin KM, Giacomini KM

Characterization of guanidine transport in human renal brush border membranes.

Pharmaceutical research

Chun JK, Zhang L, Piquette-Miller M, Lau E, Tong LQ, Giacomini KM

Cloning and functional characterization of a rat renal organic cation transporter isoform (rOCT1A).

The Journal of biological chemistry

Zhang L, Dresser MJ, Chun JK, Babbitt PC, Giacomini KM

Cloning and functional expression of a human liver organic cation transporter.

Molecular pharmacology

Zhang L, Dresser MJ, Gray AT, Yost SC, Terashita S, Giacomini KM

Expression of human polyspecific renal organic cation transport activity in Xenopus laevis oocytes.

Journal of pharmaceutical sciences

Chun JK, Piquette-Miller M, Zhang L, Giacomini KM

Guanidine transport in a human choriocarcinoma cell line (JAR).

Pharmaceutical research

Zevin S, Schaner ME, Illsley NP, Giacomini KM

Taurine transport in cultured choroid plexus.

Pharmaceutical research

Ramanathan VK, Chung SJ, Giacomini KM, Brett CM

Saturable disposition of taurine in the rat cerebrospinal fluid.

The Journal of pharmacology and experimental therapeutics

Chung SJ, Ramanathan VK, Brett CM, Giacomini KM

Isolated renal brush border and basolateral membrane vesicles and cultured renal cells.

Pharmaceutical biotechnology

Gutierrez MM, Brett CM, Giacomini KM

Methods of study drug transport in isolated choroid plexus tissue and cultured cells.

Pharmaceutical biotechnology

Washington CB, Giacomini KM, Brett CM

The effect of N-ethylmaleimide on the Na(+)-dependent nucleoside transporter (N3) in rabbit choroid plexus.

The Journal of pharmacology and experimental therapeutics

Washington CB, Brett CM, Wu X, Giacomini KM

The effects of modulation of calcium influx through the voltage-sensitive calcium channel on cardiomyocyte hypertrophy.

Journal of molecular and cellular cardiology

Lubic SP, Giacomini KM, Giacomini JC

Increased 1,4-dihydropyridine binding sites in serum-stimulated cardiomyocyte hypertrophy.

The Journal of pharmacology and experimental therapeutics

Lubic SP, Giacomini KM, Giacomini JC

Characterization of a sodium-dependent taurine transporter in rabbit choroid plexus.

Biochimica et biophysica acta

Chung SJ, Ramanathan V, Giacomini KM, Brett CM

Expression of a renal Na(+)-nucleoside cotransport system (N2) in Xenopus laevis oocytes.

Pflugers Archiv : European journal of physiology

Giacomini KM, Markovich D, Werner A, Biber J, Wu X, Murer H

Effect of phenylisothiocyanate on organic cation transport in opossum kidney cells.

The Journal of pharmacology and experimental therapeutics

Ott RJ, Chan JK, Ramanathan VK, Hui AC, Giacomini KM

Chemical, enzymatic, and human enantioselective S-oxygenation of cimetidine.

Drug metabolism and disposition: the biological fate of chemicals

Cashman JR, Park SB, Yang ZC, Washington CB, Gomez DY, Giacomini KM, Brett CM

Formycin B elimination from the cerebrospinal fluid of the rat.

Pharmaceutical research

Wu X, Hui AC, Giacomini KM

Caring for the community

Caring.

Hayes K, Morgan B, Giacomini K, Dockal S.

Beta-adrenergic blockers as cardioprotective agents.

The American journal of cardiology

Frishman WH

Intact lung cytochrome P-450 is not required for hypoxic pulmonary vasoconstriction.

The American journal of physiology

Chang SW, Dutton D, Wang HL, He LS, Stearns R, Hui A, Giacomini KM, Ortiz de Montellano P, Voelkel NF

Nucleoside transport in brush border membrane vesicles from human kidney.

Biochimica et biophysica acta

Gutierrez MM, Brett CM, Ott RJ, Hui AC, Giacomini KM

Organic cation transport in human renal brush-border membrane vesicles.

The American journal of physiology

Ott RJ, Hui AC, Yuan G, Giacomini KM

Transport of organic cations by a renal epithelial cell line (OK).

The Journal of biological chemistry

Yuan G, Ott RJ, Salgado C, Giacomini KM

Effect of probenecid on the pharmacokinetics and pharmacodynamics of procainamide.

Journal of clinical pharmacology

Lam YW, Boyd RA, Chin SK, Chang D, Giacomini KM

Preparation of brush border membrane vesicles from bovine choroid plexus.

Journal of pharmacological methods

Whittico MT, Hui AC, Giacomini KM

Cimetidine transport in isolated brush border membrane vesicles from bovine choroid plexus.

The Journal of pharmacology and experimental therapeutics

Whittico MT, Gang YA, Giacomini KM

Computer-guided laser for neurosurgery.

Annales chirurgiae et gynaecologiae

Koivukangas J, Louhisalmi Y

The pharmacokinetics and pharmacodynamics of diltiazem and its metabolites in healthy adults after a single oral dose.

Clinical pharmacology and therapeutics

Boyd RA, Chin SK, Don-Pedro O, Verotta D, Sheiner LB, Williams RL, Giacomini KM

The effect of probenecid on the renal elimination of cimetidine.

Clinical pharmacology and therapeutics

Gisclon LG, Boyd RA, Williams RL, Giacomini KM

The pharmacokinetics of the enantiomers of atenolol.

Clinical pharmacology and therapeutics

Boyd RA, Chin SK, Don-Pedro O, Williams RL, Giacomini KM

Cimetidine elimination from the cerebrospinal fluid of the rat.

Pharmaceutical research

Whittico MT, Giacomini KM

Renal transport of drugs: an overview of methodology with application to cimetidine.

Pharmaceutical research

Giacomini KM, Hsyu PH, Gisclon LG

Stereoselective binding of disopyramide to plasma proteins.

Pharmaceutical research

Valdivieso L, Giacomini KM, Nelson WL, Pershe R, Blaschke TF

The effect of pindolol on the transport of L-lysine in renal brush border membrane vesicles.

Drug metabolism and disposition: the biological fate of chemicals

Hsyu PH, Wong FM, Giacomini KM

Inhibition of cimetidine transport by creatinine in luminal membrane vesicles prepared from rabbit kidney.

Drug metabolism and disposition: the biological fate of chemicals

Gisclon LG, Giacomini KM

Interactions of organic anions with the organic cation transporter in renal BBMV.

The American journal of physiology

Hsyu PH, Gisclon LG, Hui AC, Giacomini KM

Comparison of binding affinities and negative inotropic potencies of the 1,4-dihydropyridine calcium channel blockers in rabbit myocardium.

The Journal of pharmacology and experimental therapeutics

Boyd RA, Giacomini JC, Wong FM, Nelson WL, Giacomini KM

Cimetidine transport in isolated luminal membrane vesicles from rabbit kidney.

The American journal of physiology

Gisclon L, Wong FM, Giacomini KM

Essential tyrosine residues in transport of organic cations in renal BBMV.

The American journal of physiology

Hsyu PH, Giacomini KM

The interaction of phenylalkylamine calcium channel blockers with the 1,4-dihydropyridine binding site.

Journal of molecular and cellular cardiology

Zobrist RH, Giacomini KM, Nelson WL, Giacomini JC

In vivo interaction of the enantiomers of disopyramide in human subjects.

Journal of pharmacokinetics and biopharmaceutics

Giacomini KM, Nelson WL, Pershe RA, Valdivieso L, Turner-Tamiyasu K, Blaschke TF

Posttraumatic complications and inflammatory mediators.

Archives of surgery (Chicago, Ill. : 1960)

Nuytinck JK, Goris JA, Redl H, Schlag G, van Munster PJ

Stereoselective interactions of 2-[(2',6'-dimethoxyphenoxyethyl)aminomethyl]-1,4-benzodioxane (WB-4101) with the calcium channel.

Biochemical pharmacology

Giacomini JC, Nelson WL, Wong FM, Boyd R, Zobrist RH, Giacomini KM

Stereoselective renal clearance of pindolol in humans.

The Journal of clinical investigation

Hsyu PH, Giacomini KM

Electrophysiology of the enantiomers of disopyramide in dogs.

Journal of cardiovascular pharmacology

Giacomini JC, Giacomini KM, Nelson WL, Harrison DC, Blaschke TF

The pharmacokinetics and pharmacodynamics of d- and dl-verapamil in rabbits.

Journal of cardiovascular pharmacology

Giacomini JC, Nelson WL, Theodore L, Wong FM, Rood D, Giacomini KM

Verapamil interacts stereoselectively with the muscarinic receptor.

Pharmaceutical research

Giacomini JC, Zobrist RH, Dave B, Giacomini KM

Decreased binding of verapamil to plasma proteins in patients with liver disease.

Journal of cardiovascular pharmacology

Giacomini KM, Massoud N, Wong FM, Giacomini JC

High-performance liquid chromatographic analysis of hypoxanthine arabinoside in plasma.

Journal of chromatography

Smith GA, Giacomini KM, Smith CT, Gregory PB, Robinson WS, Merigan TC, Blaschke TF

Amitriptyline disposition in young and elderly normal men.

Clinical pharmacology and therapeutics

Schulz P, Turner-Tamiyasu K, Smith G, Giacomini KM, Blaschke TF

Effect of heparin on the red blood cell-to-plasma concentration ratio of diphenylhydantoin and prazosin.

Therapeutic drug monitoring

Schulz P, Abang A, Giacomini JC, Blaschke TF, Giacomini KM

Effect of low doses of heparin on the plasma binding of phenytoin and prazosin in normal man.

European journal of clinical pharmacology

Schulz P, Giacomini KM, Luttrell S, Turner-Tamiyasu K, Blaschke TF

Calculation of drug concentration in plasma after equilibrium dialysis.

British journal of clinical pharmacology

Giacomini KM, Abang A, Blaschke TF

The cardiac effects of d- and l-disopyramide in normal subjects: a noninvasive study.

Circulation

Pollick C, Giacomini KM, Blaschke TF, Nelson WL, Turner-Tamiyasu K, Briskin V, Popp RL

High-pressure liquid chromatographic determination of amitriptyline and its major metabolites in human whole blood.

Journal of pharmaceutical sciences

Smith GA, Schulz P, Giacomini KM, Blaschke TF

Measurement of ketoconazole, a new antifungal agent, by high-performance liquid chromatography.

Journal of chromatography

Swezey SF, Giacomini KM, Abang A, Brass C, Stevens DA, Blaschke TF

The effect of saturable binding to plasma proteins on the pharmacokinetic properties of disopyramide.

Journal of pharmacokinetics and biopharmaceutics

Giacomini KM, Swezey SE, Turner-Tamiyasu K, Blaschke TF

Synthesis and anticholinergic properties of the enantiomers of 4-(isopropylamino)-2-(2-pyridyl)-2-phenylbutyramide, the mono-N-dealkylated metabolite of disopyramide.

Journal of medicinal chemistry

Nelson WL, Sneed CK, Giacomini KM, Giacomini JC, Stauss J, Blaschke TF, Cox BM

Evaluation of methods for producing renal dysfunction in rats.

Journal of pharmaceutical sciences

Giacomini KM, Roberts SM, Levy G

Absence of effect of heparin on the binding of prazosin and phenytoin to plasma proteins.

Biochemical pharmacology

Giacomini KM, Giacomini JC, Blaschke TF

The stereoselective disposition of disopyramide in the dog.

Journal of cardiovascular pharmacology

Giacomini KM, Giacomini JC, Swezey SE, Harrison DC, Nelson WL, Burke TR, Blaschke TF

Administration of heparin causes in vitro release of non-esterified fatty acids in human plasma.

Life sciences

Giacomini KM, Swezey SE, Giacomini JC, Blaschke TF

Pharmacokinetic studies of propoxyphene I:Effect of portacaval shunt on systemic availability in dogs.

Journal of pharmaceutical sciences

Giacomini KM, Nakeeb SM, Levy G

Propoxyphene and norpropoxyphene plasma concentrations in the anephric patient.

Clinical pharmacology and therapeutics

Gibson TP, Giacomini KM, Briggs WA, Whitman W, Levy G

Effect of hemodialysis on propoxyphene and norpropoxyphene concentrations in blood of anephric patients.

Clinical pharmacology and therapeutics

Giacomini KM, Gibson TP, Levy G

Phenylalanine metabolism in uremic and normal man.

Kidney international

Jones MR, Kopple JD, Swendseid ME

Rational aspirin dosage regimens.

Clinical pharmacology and therapeutics

Levy G, Giacomini KM

Plasma protein binding of d-propoxyphene in normal subjects and anephric patients.

Journal of clinical pharmacology

Giacomini KM, Gibson TP, Levy G

A Convenient Method for Repetitive Blood Sampling in the Dog

J. Pharmacol. Meth.

Soles C, Giacomini KM, Roberts SM, Giacomini JC. Soles C, Giacomini KM, Roberts SM, Giacomini JC.