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Items: 13


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 effect of laquinimod, a novel immuno-modulator in development to treat Huntington disease, on the pharmacokinetics of ethinylestradiol and levonorgestrel in healthy young women.

Elgart A, Zur AA, Mimrod D, Dror V, Bar-Ilan O, Korver T, Spiegelstein O.

Eur J Clin Pharmacol. 2019 Jan;75(1):41-49. doi: 10.1007/s00228-018-2549-7. Epub 2018 Sep 6.


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.


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.


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.


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.


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.


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.


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.


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

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.

Proc Natl Acad Sci U S A. 2014 Jul 8;111(27):9983-8. doi: 10.1073/pnas.1314939111. Epub 2014 Jun 24.


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

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

Clin Pharmacol Ther. 2013 Jul;94(1):52-63. doi: 10.1038/clpt.2013.74. Epub 2013 Apr 8. Review.


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

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

J Med Chem. 2013 Feb 14;56(3):781-795. doi: 10.1021/jm301302s. Epub 2013 Jan 22.


The challenge of pain management in patients with myasthenia gravis.

Haroutiunian S, Lecht S, Zur AA, Hoffman A, Davidson E.

J Pain Palliat Care Pharmacother. 2009;23(3):242-60. doi: 10.1080/15360280903098523. Review.


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