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Expanding Precompetitive Multisector Collaborations to Advance Drug Development and Pharmacogenomics.

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

Clin Pharmacol Ther. 2019 Nov 27. doi: 10.1002/cpt.1691. [Epub ahead of print] No abstract available.


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

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

Am J Clin Nutr. 2019 Nov 25. pii: nqz255. doi: 10.1093/ajcn/nqz255. [Epub ahead of print]


Global Pharmacogenomics Within Precision Medicine: Challenges and Opportunities.

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

Clin Pharmacol Ther. 2019 Nov 6. doi: 10.1002/cpt.1664. [Epub ahead of print] No abstract available.


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

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.

PLoS Genet. 2019 Sep 25;15(9):e1008208. doi: 10.1371/journal.pgen.1008208. eCollection 2019 Sep.


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

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

Bioorg Med Chem Lett. 2019 Aug 15;29(16):2254-2258. doi: 10.1016/j.bmcl.2019.06.033. Epub 2019 Jun 20.


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

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.

Clin Pharmacol Ther. 2019 Nov;106(5):1083-1092. doi: 10.1002/cpt.1516. Epub 2019 Jul 3.


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

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

Clin Transl Sci. 2019 Jul;12(4):388-399. doi: 10.1111/cts.12625. Epub 2019 Apr 13.


Functional and structural analysis of rare SLC2A2 variants associated with Fanconi-Bickel syndrome and metabolic traits.

Enogieru OJ, Ung PMU, Yee SW, Schlessinger A, Giacomini KM.

Hum Mutat. 2019 Jul;40(7):983-995. doi: 10.1002/humu.23758. Epub 2019 Apr 25.


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

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

Clin Pharmacol Ther. 2019 Sep;106(3):623-631. doi: 10.1002/cpt.1439. Epub 2019 May 23.


Research Projects Supported by the University of California, San Francisco-Stanford Center of Excellence in Regulatory Science and Innovation.

Giacomini KM, Lin L, Altman RB.

Clin Pharmacol Ther. 2019 Apr;105(4):815-818. doi: 10.1002/cpt.1308. Epub 2019 Feb 17. No abstract available.


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

Zou L, Ni Z, Tsakalozou E, Giacomini KM.

Clin Pharmacol Ther. 2019 Feb;105(2):323-325. doi: 10.1002/cpt.1292. Epub 2019 Jan 20. No abstract available.


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

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.

PLoS Biol. 2019 Jan 17;17(1):e2006571. doi: 10.1371/journal.pbio.2006571. eCollection 2019 Jan.


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

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.

Clin Pharmacol Ther. 2018 Nov;104(5):836-864. doi: 10.1002/cpt.1216. Review.


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

Giacomini KM, Galetin A, Huang SM.

Clin Pharmacol Ther. 2018 Nov;104(5):766-771. doi: 10.1002/cpt.1224. No abstract available.


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

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.

Clin Pharmacol Ther. 2018 Nov;104(5):890-899. doi: 10.1002/cpt.1112. Epub 2018 Aug 8. Review.


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

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.

J Med Chem. 2018 Aug 23;61(16):7358-7373. doi: 10.1021/acs.jmedchem.8b01007. Epub 2018 Aug 10.


Pharmacogenetics of Antidiabetic Drugs.

Srinivasan S, Yee SW, Giacomini KM.

Adv Pharmacol. 2018;83:361-389. doi: 10.1016/bs.apha.2018.04.005. Epub 2018 May 14. Review.


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

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.

Clin Pharmacol Ther. 2018 Nov;104(5):781-784. doi: 10.1002/cpt.1082. Epub 2018 May 15.


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

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

Mol Pharmacol. 2018 Jul;94(1):689-699. doi: 10.1124/mol.117.111153. Epub 2018 May 2.


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

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

Clin Pharmacol Ther. 2018 Nov;104(5):803-817. doi: 10.1002/cpt.1098. Epub 2018 May 31. Review.


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

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.

PLoS Biol. 2018 Apr 16;16(4):e2002907. doi: 10.1371/journal.pbio.2002907. eCollection 2018 Apr.


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

Diabetes. 2018 Jul;67(7):1428-1440. doi: 10.2337/db17-1164. Epub 2018 Apr 12.


Emerging Clinical Importance of Hepatic Organic Cation Transporter 1 (OCT1) in Drug Pharmacokinetics, Dynamics, Pharmacogenetic Variability, and Drug Interactions.

Zamek-Gliszczynski MJ, Giacomini KM, Zhang L.

Clin Pharmacol Ther. 2018 May;103(5):758-760. doi: 10.1002/cpt.941. Epub 2017 Nov 28.


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

Brackman DJ, Giacomini KM.

Clin Pharmacol Ther. 2018 Feb;103(2):233-242. doi: 10.1002/cpt.903. Epub 2017 Nov 28. Review.


PharmGKB summary: very important pharmacogene information for ABCG2.

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

Pharmacogenet Genomics. 2017 Nov;27(11):420-427. doi: 10.1097/FPC.0000000000000305. Review. No abstract available. Erratum in: Pharmacogenet Genomics. 2018 May;28(5):138.


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

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.

Clin Pharmacol Ther. 2017 Dec;102(6):897-902. doi: 10.1002/cpt.755. Epub 2017 Aug 10.


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

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

Clin Pharmacol Ther. 2018 Mar;103(3):485-492. doi: 10.1002/cpt.750. Epub 2017 Jul 24.


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

Stecula A, Schlessinger A, Giacomini KM, Sali A.

Biochemistry. 2017 Jul 11;56(27):3475-3483. doi: 10.1021/acs.biochem.7b00339. Epub 2017 Jun 29.


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

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

J Chem Inf Model. 2017 Jun 26;57(6):1402-1413. doi: 10.1021/acs.jcim.6b00720. Epub 2017 Jun 15.


Transporters Involved in Metformin Pharmacokinetics and Treatment Response.

Liang X, Giacomini KM.

J Pharm Sci. 2017 Sep;106(9):2245-2250. doi: 10.1016/j.xphs.2017.04.078. Epub 2017 May 8. Review.


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

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

J Pharm Sci. 2017 Sep;106(9):2551-2557. doi: 10.1016/j.xphs.2017.04.076. Epub 2017 May 5.


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

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

J Med Chem. 2017 Apr 13;60(7):2685-2696. doi: 10.1021/acs.jmedchem.6b01317. Epub 2017 Mar 15.


The use of drug transporters as therapeutic targets.

Giacomini KM.

Clin Adv Hematol Oncol. 2016 Nov;14(11):869-871. No abstract available.


Genomic Characterization of Metformin Hepatic Response.

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.

PLoS Genet. 2016 Nov 30;12(11):e1006449. doi: 10.1371/journal.pgen.1006449. eCollection 2016 Nov.


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

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

Nat Rev Drug Discov. 2017 Jan;16(1):1. doi: 10.1038/nrd.2016.234. Epub 2016 Nov 25. No abstract available.


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

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, Klimčáková L, Pirags V, Kooy A, Brøsen K, Klovins J, Semiz S, Tkáč I, Stricker BH, Palmer C, 't Hart LM, Giacomini KM, Pearson ER.

Clin Pharmacol Ther. 2017 Jun;101(6):763-772. doi: 10.1002/cpt.567. Epub 2017 Feb 3.


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

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.

Bioorg Med Chem Lett. 2016 Oct 15;26(20):5000-5006. doi: 10.1016/j.bmcl.2016.09.001. Epub 2016 Sep 3.


A Molecular Basis for Innovation in Drug Excipients.

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

Clin Pharmacol Ther. 2017 Mar;101(3):320-323. doi: 10.1002/cpt.458. Epub 2016 Sep 28. Review.


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

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, Tkáč 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.

Nat Genet. 2016 Sep;48(9):1055-1059. doi: 10.1038/ng.3632. Epub 2016 Aug 8.


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

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

Mol Pharm. 2016 Sep 6;13(9):3130-40. doi: 10.1021/acs.molpharmaceut.6b00332. Epub 2016 Aug 9. Review.


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

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.

Clin Pharmacol Ther. 2016 Nov;100(5):524-536. doi: 10.1002/cpt.434. Epub 2016 Sep 20.


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

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.

Clin Pharmacol Ther. 2016 Nov;100(5):537-547. doi: 10.1002/cpt.428. Epub 2016 Sep 23.


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

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

Front Pharmacol. 2016 Jun 14;7:135. doi: 10.3389/fphar.2016.00135. eCollection 2016.


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

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

Clin Pharmacol Ther. 2016 Nov;100(5):423-426. doi: 10.1002/cpt.405. Epub 2016 Jul 21.


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

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

Bioorg Med Chem Lett. 2016 Jun 1;26(11):2616-2621. doi: 10.1016/j.bmcl.2016.04.023. Epub 2016 Apr 11.


A research roadmap for next-generation sequencing informatics.

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.

Sci Transl Med. 2016 Apr 20;8(335):335ps10. doi: 10.1126/scitranslmed.aaf7314. Review.


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

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.

Pharmacogenomics J. 2017 Mar;17(2):137-145. doi: 10.1038/tpj.2015.93. Epub 2016 Feb 9.


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.

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

Drug Metab Dispos. 2016 Mar;44(3):356-64. doi: 10.1124/dmd.115.066647. Epub 2015 Dec 23.


Unmet needs: Research helps regulators do their jobs.

Altman RB, Khuri N, Salit M, Giacomini KM.

Sci Transl Med. 2015 Nov 25;7(315):315ps22. doi: 10.1126/scitranslmed.aac4369. Review.


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

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.

Clin Pharmacokinet. 2016 Jun;55(6):711-21. doi: 10.1007/s40262-015-0346-3.

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