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Items: 36

1.

Identification of novel glutathione conjugates of terbinafine in liver microsomes and hepatocytes across species.

Patil A, Ladumor MK, Kamble SH, Johnson BM, Subramanian M, Sinz MW, Singh DK, Putlur S, Bhutani P, Ahire DS, Singh S.

Xenobiotica. 2019 Dec;49(12):1403-1413. doi: 10.1080/00498254.2019.1581959. Epub 2019 Mar 7.

PMID:
30747549
2.

Preface.

Sinz MW.

Curr Drug Metab. 2017;18(1):1. doi: 10.2174/138920021801170119202545. No abstract available.

PMID:
28889795
3.

Discovery of a Potent Acyclic, Tripeptidic, Acyl Sulfonamide Inhibitor of Hepatitis C Virus NS3 Protease as a Back-up to Asunaprevir with the Potential for Once-Daily Dosing.

Sun LQ, Mull E, Zheng B, D'Andrea S, Zhao Q, Wang AX, Sin N, Venables BL, Sit SY, Chen Y, Chen J, Cocuzza A, Bilder DM, Mathur A, Rampulla R, Chen BC, Palani T, Ganesan S, Arunachalam PN, Falk P, Levine S, Chen C, Friborg J, Yu F, Hernandez D, Sheaffer AK, Knipe JO, Han YH, Schartman R, Donoso M, Mosure K, Sinz MW, Zvyaga T, Rajamani R, Kish K, Tredup J, Klei HE, Gao Q, Ng A, Mueller L, Grasela DM, Adams S, Loy J, Levesque PC, Sun H, Shi H, Sun L, Warner W, Li D, Zhu J, Wang YK, Fang H, Cockett MI, Meanwell NA, McPhee F, Scola PM.

J Med Chem. 2016 Sep 8;59(17):8042-60. doi: 10.1021/acs.jmedchem.6b00821. Epub 2016 Aug 26.

PMID:
27564532
4.

Evaluation of CYP2B6 Induction and Prediction of Clinical Drug-Drug Interactions: Considerations from the IQ Consortium Induction Working Group-An Industry Perspective.

Fahmi OA, Shebley M, Palamanda J, Sinz MW, Ramsden D, Einolf HJ, Chen L, Wang H.

Drug Metab Dispos. 2016 Oct;44(10):1720-30. doi: 10.1124/dmd.116.071076. Epub 2016 Jul 15.

PMID:
27422672
5.

The discovery of asunaprevir (BMS-650032), an orally efficacious NS3 protease inhibitor for the treatment of hepatitis C virus infection.

Scola PM, Sun LQ, Wang AX, Chen J, Sin N, Venables BL, Sit SY, Chen Y, Cocuzza A, Bilder DM, D'Andrea SV, Zheng B, Hewawasam P, Tu Y, Friborg J, Falk P, Hernandez D, Levine S, Chen C, Yu F, Sheaffer AK, Zhai G, Barry D, Knipe JO, Han YH, Schartman R, Donoso M, Mosure K, Sinz MW, Zvyaga T, Good AC, Rajamani R, Kish K, Tredup J, Klei HE, Gao Q, Mueller L, Colonno RJ, Grasela DM, Adams SP, Loy J, Levesque PC, Sun H, Shi H, Sun L, Warner W, Li D, Zhu J, Meanwell NA, McPhee F.

J Med Chem. 2014 Mar 13;57(5):1730-52. doi: 10.1021/jm500297k. Epub 2014 Mar 5.

PMID:
24564672
6.

Discovery and early clinical evaluation of BMS-605339, a potent and orally efficacious tripeptidic acylsulfonamide NS3 protease inhibitor for the treatment of hepatitis C virus infection.

Scola PM, Wang AX, Good AC, Sun LQ, Combrink KD, Campbell JA, Chen J, Tu Y, Sin N, Venables BL, Sit SY, Chen Y, Cocuzza A, Bilder DM, D'Andrea S, Zheng B, Hewawasam P, Ding M, Thuring J, Li J, Hernandez D, Yu F, Falk P, Zhai G, Sheaffer AK, Chen C, Lee MS, Barry D, Knipe JO, Li W, Han YH, Jenkins S, Gesenberg C, Gao Q, Sinz MW, Santone KS, Zvyaga T, Rajamani R, Klei HE, Colonno RJ, Grasela DM, Hughes E, Chien C, Adams S, Levesque PC, Li D, Zhu J, Meanwell NA, McPhee F.

J Med Chem. 2014 Mar 13;57(5):1708-29. doi: 10.1021/jm401840s. Epub 2014 Feb 20.

PMID:
24555570
7.

Expression and characterization of cynomolgus monkey cytochrome CYP3A4 in a novel human embryonic kidney cell-based mammalian system.

Selvakumar S, Bhutani P, Ghosh K, Krishnamurthy P, Kallipatti S, Selvam S, Ramarao M, Mandlekar S, Sinz MW, Rodrigues AD, Subramanian M.

Drug Metab Dispos. 2014 Mar;42(3):369-76. doi: 10.1124/dmd.113.055491. Epub 2013 Dec 13.

PMID:
24335510
8.

Evaluation of various static and dynamic modeling methods to predict clinical CYP3A induction using in vitro CYP3A4 mRNA induction data.

Einolf HJ, Chen L, Fahmi OA, Gibson CR, Obach RS, Shebley M, Silva J, Sinz MW, Unadkat JD, Zhang L, Zhao P.

Clin Pharmacol Ther. 2014 Feb;95(2):179-88. doi: 10.1038/clpt.2013.170. Epub 2013 Aug 29.

PMID:
23995268
9.

Induction of xenobiotic receptors, transporters, and drug metabolizing enzymes by oxycodone.

Hassan HE, Myers AL, Lee IJ, Mason CW, Wang D, Sinz MW, Wang H, Eddington ND.

Drug Metab Dispos. 2013 May;41(5):1060-9. doi: 10.1124/dmd.112.050401. Epub 2013 Feb 25.

PMID:
23439660
10.

Evaluation of pregnane X receptor (PXR)-mediated CYP3A4 drug-drug interactions in drug development.

Sinz MW.

Drug Metab Rev. 2013 Feb;45(1):3-14. doi: 10.3109/03602532.2012.743560. Review.

PMID:
23330538
11.

An insulin-like growth factor 1 receptor inhibitor induces CYP3A4 expression through a pregnane X receptor-independent, noncanonical constitutive androstane receptor-related mechanism.

Li L, Sinz MW, Zimmermann K, Wang H.

J Pharmacol Exp Ther. 2012 Mar;340(3):688-97. doi: 10.1124/jpet.111.188854. Epub 2011 Dec 9.

12.

Phenacetin pharmacokinetics in CYP1A2-deficient beagle dogs.

Whiterock VJ, Morgan DG, Lentz KA, Orcutt TL, Sinz MW.

Drug Metab Dispos. 2012 Feb;40(2):228-31. doi: 10.1124/dmd.111.041848. Epub 2011 Nov 10.

PMID:
22074769
13.

Quantitative relationship between rifampicin exposure and induction of Cyp3a11 in SXR humanized mice: extrapolation to human CYP3A4 induction potential.

Kim S, Pray D, Zheng M, Morgan DG, Pizzano JG, Zoeckler ME, Chimalakonda A, Sinz MW.

Drug Metab Lett. 2008 Aug;2(3):169-75.

PMID:
19356089
14.

Discovery and evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperidin-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an orally efficacious inhibitor of insulin-like growth factor-1 receptor kinase with broad spectrum in vivo antitumor activity.

Velaparthi U, Wittman M, Liu P, Carboni JM, Lee FY, Attar R, Balimane P, Clarke W, Sinz MW, Hurlburt W, Patel K, Discenza L, Kim S, Gottardis M, Greer A, Li A, Saulnier M, Yang Z, Zimmermann K, Trainor G, Vyas D.

J Med Chem. 2008 Oct 9;51(19):5897-900. doi: 10.1021/jm800832q. Epub 2008 Sep 3.

PMID:
18763755
15.

Machine learning methods and docking for predicting human pregnane X receptor activation.

Khandelwal A, Krasowski MD, Reschly EJ, Sinz MW, Swaan PW, Ekins S.

Chem Res Toxicol. 2008 Jul;21(7):1457-67. doi: 10.1021/tx800102e. Epub 2008 Jun 12.

16.

Cytochrome P450 reaction-phenotyping: an industrial perspective.

Zhang H, Davis CD, Sinz MW, Rodrigues AD.

Expert Opin Drug Metab Toxicol. 2007 Oct;3(5):667-87. Review.

PMID:
17916054
17.

Development and full validation of six inhibition assays for five major cytochrome P450 enzymes in human liver microsomes using an automated 96-well microplate incubation format and LC-MS/MS analysis.

Yao M, Zhu M, Sinz MW, Zhang H, Humphreys WG, Rodrigues AD, Dai R.

J Pharm Biomed Anal. 2007 May 9;44(1):211-23. Epub 2007 Mar 3.

PMID:
17418993
18.

Frequency of CYP1A2 polymorphism in beagle dogs.

Whiterock VJ, Delmonte TA, Hui LE, Orcutt TL, Sinz MW.

Drug Metab Lett. 2007 Apr;1(2):163-5.

PMID:
19356037
19.

The utility of stable cell lines to assess species differences in PXR transactivation.

Sinz MW, Pray D, Raucy J.

Drug Metab Lett. 2007 Apr;1(2):147-52.

PMID:
19356035
20.

Stem cells, immortalized cells and primary cells in ADMET assays.

Sinz MW, Kim S.

Drug Discov Today Technol. 2006 Spring;3(1):79-85. doi: 10.1016/j.ddtec.2006.03.006.

PMID:
24980105
21.

Animal models of xenobiotic receptors in drug metabolism and diseases.

Gong H, Sinz MW, Feng Y, Chen T, Venkataramanan R, Xie W.

Methods Enzymol. 2005;400:598-618. Review.

PMID:
16399373
22.

Metabolism and transporter-mediated drug-drug interactions of the endothelin-A receptor antagonist CI-1034.

Sahi J, Sinz MW, Campbell S, Mireles R, Zheng X, Rose KA, Raeissi S, Hashim MF, Ye Y, de Morais SM, Black C, Tugnait M, Keller LH.

Chem Biol Interact. 2006 Feb 1;159(2):156-68. Epub 2005 Dec 13.

PMID:
16356485
23.

Fluorine substitution can block CYP3A4 metabolism-dependent inhibition: identification of (S)-N-[1-(4-fluoro-3- morpholin-4-ylphenyl)ethyl]-3- (4-fluorophenyl)acrylamide as an orally bioavailable KCNQ2 opener devoid of CYP3A4 metabolism-dependent inhibition.

Wu YJ, Davis CD, Dworetzky S, Fitzpatrick WC, Harden D, He H, Knox RJ, Newton AE, Philip T, Polson C, Sivarao DV, Sun LQ, Tertyshnikova S, Weaver D, Yeola S, Zoeckler M, Sinz MW.

J Med Chem. 2003 Aug 28;46(18):3778-81.

PMID:
12930139
24.

(S)-N-[1-(3-morpholin-4-ylphenyl)ethyl]- 3-phenylacrylamide: an orally bioavailable KCNQ2 opener with significant activity in a cortical spreading depression model of migraine.

Wu YJ, Boissard CG, Greco C, Gribkoff VK, Harden DG, He H, L'Heureux A, Kang SH, Kinney GG, Knox RJ, Natale J, Newton AE, Lehtinen-Oboma S, Sinz MW, Sivarao DV, Starrett JE Jr, Sun LQ, Tertyshnikova S, Thompson MW, Weaver D, Wong HS, Zhang L, Dworetzky SI.

J Med Chem. 2003 Jul 17;46(15):3197-200.

PMID:
12852750
25.

Comparative effects of thiazolidinediones on in vitro P450 enzyme induction and inhibition.

Sahi J, Black CB, Hamilton GA, Zheng X, Jolley S, Rose KA, Gilbert D, LeCluyse EL, Sinz MW.

Drug Metab Dispos. 2003 Apr;31(4):439-46.

PMID:
12642470
26.

The effect of troglitazone biliary excretion on metabolite distribution and cholestasis in transporter-deficient rats.

Kostrubsky VE, Vore M, Kindt E, Burliegh J, Rogers K, Peter G, Altrogge D, Sinz MW.

Drug Metab Dispos. 2001 Dec;29(12):1561-6.

PMID:
11717175
27.
28.
29.

Inactivation of cytochrome P450 3A4 by bergamottin, a component of grapefruit juice.

He K, Iyer KR, Hayes RN, Sinz MW, Woolf TF, Hollenberg PF.

Chem Res Toxicol. 1998 Apr;11(4):252-9.

PMID:
9548795
30.

Characterization of the induction of rat microsomal cytochrome P450 by tacrine.

Sinz MW, Woolf TF.

Biochem Pharmacol. 1997 Aug 1;54(3):425-7.

PMID:
9278102
31.
32.

Distribution of tacrine and metabolites in rat brain and plasma after single- and multiple-dose regimens. Evidence for accumulation of tacrine in brain tissue.

McNally WP, Pool WF, Sinz MW, Dehart P, Ortwine DF, Huang CC, Chang T, Woolf TF.

Drug Metab Dispos. 1996 Jun;24(6):628-33.

PMID:
8781777
34.
35.

Isolation and characterization of a novel quaternary ammonium-linked glucuronide of lamotrigine.

Sinz MW, Remmel RP.

Drug Metab Dispos. 1991 Jan-Feb;19(1):149-53.

PMID:
1673389

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