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Items: 24


Atropisomerism by Design: Discovery of a Selective and Stable Phosphoinositide 3-Kinase (PI3K) β Inhibitor.

Chandrasekhar J, Dick R, Van Veldhuizen J, Koditek D, Lepist EI, McGrath ME, Patel L, Phillips G, Sedillo K, Somoza JR, Therrien J, Till NA, Treiberg J, Villaseñor AG, Zherebina Y, Perreault S.

J Med Chem. 2018 Aug 9;61(15):6858-6868. doi: 10.1021/acs.jmedchem.8b00797. Epub 2018 Jul 30.


Beyond drug-drug interactions: effects of transporter inhibition on endobiotics, nutrients and toxins.

Lepist EI, Ray AS.

Expert Opin Drug Metab Toxicol. 2017 Oct;13(10):1075-1087. doi: 10.1080/17425255.2017.1372425. Epub 2017 Aug 29. Review.


Discovery of a Phosphoinositide 3-Kinase (PI3K) β/δ Inhibitor for the Treatment of Phosphatase and Tensin Homolog (PTEN) Deficient Tumors: Building PI3Kβ Potency in a PI3Kδ-Selective Template by Targeting Nonconserved Asp856.

Perreault S, Chandrasekhar J, Cui ZH, Evarts J, Hao J, Kaplan JA, Kashishian A, Keegan KS, Kenney T, Koditek D, Lad L, Lepist EI, McGrath ME, Patel L, Phillips B, Therrien J, Treiberg J, Yahiaoui A, Phillips G.

J Med Chem. 2017 Feb 23;60(4):1555-1567. doi: 10.1021/acs.jmedchem.6b01821. Epub 2017 Feb 7.


Interaction of 2,4-Diaminopyrimidine-Containing Drugs Including Fedratinib and Trimethoprim with Thiamine Transporters.

Giacomini MM, Hao J, Liang X, Chandrasekhar J, Twelves J, Whitney JA, Lepist EI, Ray AS.

Drug Metab Dispos. 2017 Jan;45(1):76-85. Epub 2016 Nov 1. Erratum in: Drug Metab Dispos. 2017 Nov;45(11):1146-1147.


Discovery of Dihydrobenzoxazepinone (GS-6615) Late Sodium Current Inhibitor (Late INai), a Phase II Agent with Demonstrated Preclinical Anti-Ischemic and Antiarrhythmic Properties.

Zablocki JA, Elzein E, Li X, Koltun DO, Parkhill EQ, Kobayashi T, Martinez R, Corkey B, Jiang H, Perry T, Kalla R, Notte GT, Saunders O, Graupe M, Lu Y, Venkataramani C, Guerrero J, Perry J, Osier M, Strickley R, Liu G, Wang WQ, Hu L, Li XJ, El-Bizri N, Hirakawa R, Kahlig K, Xie C, Li CH, Dhalla AK, Rajamani S, Mollova N, Soohoo D, Lepist EI, Murray B, Rhodes G, Belardinelli L, Desai MC.

J Med Chem. 2016 Oct 13;59(19):9005-9017. doi: 10.1021/acs.jmedchem.6b00939. Epub 2016 Oct 3.


Discovery of Orally Efficacious Phosphoinositide 3-Kinase δ Inhibitors with Improved Metabolic Stability.

Patel L, Chandrasekhar J, Evarts J, Forseth K, Haran AC, Ip C, Kashishian A, Kim M, Koditek D, Koppenol S, Lad L, Lepist EI, McGrath ME, Perreault S, Puri KD, Villaseñor AG, Somoza JR, Steiner BH, Therrien J, Treiberg J, Phillips G.

J Med Chem. 2016 Oct 13;59(19):9228-9242. doi: 10.1021/acs.jmedchem.6b01169. Epub 2016 Oct 3.


Renal Transporter-Mediated Drug-Drug Interactions: Are They Clinically Relevant?

Lepist EI, Ray AS.

J Clin Pharmacol. 2016 Jul;56 Suppl 7:S73-81. doi: 10.1002/jcph.735. Review.


2,4,6-Triaminopyrimidine as a Novel Hinge Binder in a Series of PI3Kδ Selective Inhibitors.

Patel L, Chandrasekhar J, Evarts J, Haran AC, Ip C, Kaplan JA, Kim M, Koditek D, Lad L, Lepist EI, McGrath ME, Novikov N, Perreault S, Puri KD, Somoza JR, Steiner BH, Stevens KL, Therrien J, Treiberg J, Villaseñor AG, Yeung A, Phillips G.

J Med Chem. 2016 Apr 14;59(7):3532-48. doi: 10.1021/acs.jmedchem.6b00213. Epub 2016 Mar 29.


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

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

Mol Pharm. 2015 Dec 7;12(12):4301-10. doi: 10.1021/acs.molpharmaceut.5b00501. Epub 2015 Nov 16.


Implications of efficient hepatic delivery by tenofovir alafenamide (GS-7340) for hepatitis B virus therapy.

Murakami E, Wang T, Park Y, Hao J, Lepist EI, Babusis D, Ray AS.

Antimicrob Agents Chemother. 2015;59(6):3563-9. doi: 10.1128/AAC.00128-15. Epub 2015 Apr 13.


Contribution of the organic anion transporter OAT2 to the renal active tubular secretion of creatinine and mechanism for serum creatinine elevations caused by cobicistat.

Lepist EI, Zhang X, Hao J, Huang J, Kosaka A, Birkus G, Murray BP, Bannister R, Cihlar T, Huang Y, Ray AS.

Kidney Int. 2014 Aug;86(2):350-7. doi: 10.1038/ki.2014.66. Epub 2014 Mar 19.


Evaluation of the endothelin receptor antagonists ambrisentan, bosentan, macitentan, and sitaxsentan as hepatobiliary transporter inhibitors and substrates in sandwich-cultured human hepatocytes.

Lepist EI, Gillies H, Smith W, Hao J, Hubert C, St Claire RL 3rd, Brouwer KR, Ray AS.

PLoS One. 2014 Jan 30;9(1):e87548. doi: 10.1371/journal.pone.0087548. eCollection 2014.


Metabolism and pharmacokinetics of the anti-hepatitis C virus nucleotide prodrug GS-6620.

Murakami E, Wang T, Babusis D, Lepist EI, Sauer D, Park Y, Vela JE, Shih R, Birkus G, Stefanidis D, Kim CU, Cho A, Ray AS.

Antimicrob Agents Chemother. 2014;58(4):1943-51. doi: 10.1128/AAC.02350-13. Epub 2014 Jan 13.


Pharmacokinetics of cobicistat boosted-elvitegravir administered in combination with rosuvastatin.

Custodio JM, Wang H, Hao J, Lepist EI, Ray AS, Andrews J, Ling KH, Cheng A, Kearney BP, Ramanathan S.

J Clin Pharmacol. 2014 Jun;54(6):649-56. doi: 10.1002/jcph.256. Epub 2014 Jan 17.


Evaluation of the effect of cobicistat on the in vitro renal transport and cytotoxicity potential of tenofovir.

Stray KM, Bam RA, Birkus G, Hao J, Lepist EI, Yant SR, Ray AS, Cihlar T.

Antimicrob Agents Chemother. 2013 Oct;57(10):4982-9. doi: 10.1128/AAC.00712-13. Epub 2013 Jul 29.


Transport of A1 adenosine receptor agonist tecadenoson by human and mouse nucleoside transporters: evidence for blood-brain barrier transport by murine equilibrative nucleoside transporter 1 mENT1.

Lepist EI, Damaraju VL, Zhang J, Gati WP, Yao SY, Smith KM, Karpinski E, Young JD, Leung KH, Cass CE.

Drug Metab Dispos. 2013 Apr;41(4):916-22. doi: 10.1124/dmd.112.049858. Epub 2013 Feb 6.


Cobicistat boosts the intestinal absorption of transport substrates, including HIV protease inhibitors and GS-7340, in vitro.

Lepist EI, Phan TK, Roy A, Tong L, Maclennan K, Murray B, Ray AS.

Antimicrob Agents Chemother. 2012 Oct;56(10):5409-13. doi: 10.1128/AAC.01089-12. Epub 2012 Jul 30.


Pharmacokinetic/pharmacodynamic modeling of methylprednisolone effects on iNOS mRNA expression and nitric oxide during LPS-induced inflammation in rats.

Sukumaran S, Lepist EI, DuBois DC, Almon RR, Jusko WJ.

Pharm Res. 2012 Aug;29(8):2060-9. doi: 10.1007/s11095-012-0733-5. Epub 2012 Mar 16.


Renal drug-drug interactions: what we have learned and where we are going.

Lepist EI, Ray AS.

Expert Opin Drug Metab Toxicol. 2012 Apr;8(4):433-48. doi: 10.1517/17425255.2012.667401. Epub 2012 Feb 29. Review.


Artemisinin derivatives: toxic for laboratory animals, safe for humans?

Gordi T, Lepist EI.

Toxicol Lett. 2004 Mar 1;147(2):99-107. Review.


Stability and in vitro metabolism of dipeptide model prodrugs with affinity for the oligopeptide transporter.

Lepist EI, Kusk T, Larsen DH, Andersen D, Frokjaer S, Taub ME, Veski P, Lennernäs H, Friedrichsen G, Steffansen B.

Eur J Pharm Sci. 2000 Jul;11(1):43-50.


Stability and perfusion studies of Desmopressin (dDAVP) and prodrugs in the rat jejunum.

Lepist EI, Ostergaard J, Fredholt K, Lennernäs H, Friis GJ.

Exp Toxicol Pathol. 1999 Jul;51(4-5):363-8.


Stability, metabolism and transport of D-Asp(OBzl)-Ala--a model prodrug with affinity for the oligopeptide transporter.

Steffansen B, Lepist EI, Taub ME, Larsen BD, Frokjaer S, Lennernäs H.

Eur J Pharm Sci. 1999 Apr;8(1):67-73.


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