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Items: 1 to 50 of 75

1.

Aldehyde oxidase and its role as a drug metabolizing enzyme.

Dalvie D, Di L.

Pharmacol Ther. 2019 May 24. pii: S0163-7258(19)30093-2. doi: 10.1016/j.pharmthera.2019.05.011. [Epub ahead of print] Review.

PMID:
31128989
2.

Characterization of the Selective Indoleamine 2,3-Dioxygenase-1 (IDO1) Catalytic Inhibitor EOS200271/PF-06840003 Supports IDO1 as a Critical Resistance Mechanism to PD-(L)1 Blockade Therapy.

Gomes B, Driessens G, Bartlett D, Cai D, Cauwenberghs S, Crosignani S, Dalvie D, Denies S, Dillon CP, Fantin VR, Guo J, Letellier MC, Li W, Maegley K, Marillier R, Miller N, Pirson R, Rabolli V, Ray C, Streiner N, Torti VR, Tsaparikos K, Van den Eynde BJ, Wythes M, Yao LC, Zheng X, Tumang J, Kraus M.

Mol Cancer Ther. 2018 Dec;17(12):2530-2542. doi: 10.1158/1535-7163.MCT-17-1104. Epub 2018 Sep 19.

PMID:
30232146
3.

Discovery of a Novel and Selective Indoleamine 2,3-Dioxygenase (IDO-1) Inhibitor 3-(5-Fluoro-1H-indol-3-yl)pyrrolidine-2,5-dione (EOS200271/PF-06840003) and Its Characterization as a Potential Clinical Candidate.

Crosignani S, Bingham P, Bottemanne P, Cannelle H, Cauwenberghs S, Cordonnier M, Dalvie D, Deroose F, Feng JL, Gomes B, Greasley S, Kaiser SE, Kraus M, Négrerie M, Maegley K, Miller N, Murray BW, Schneider M, Soloweij J, Stewart AE, Tumang J, Torti VR, Van Den Eynde B, Wythes M.

J Med Chem. 2017 Dec 14;60(23):9617-9629. doi: 10.1021/acs.jmedchem.7b00974. Epub 2017 Nov 21.

PMID:
29111717
4.

Glucuronides as Potential Anionic Substrates of Human Cytochrome P450 2C8 (CYP2C8).

Ma Y, Fu Y, Khojasteh SC, Dalvie D, Zhang D.

J Med Chem. 2017 Nov 9;60(21):8691-8705. doi: 10.1021/acs.jmedchem.7b00510. Epub 2017 Jun 27. Review.

PMID:
28653847
5.

Biotransformation and bioactivation reactions - 2016 literature highlights.

Khojasteh SC, Rietjens IMCM, Dalvie D, Miller G.

Drug Metab Rev. 2017 Aug;49(3):285-317. doi: 10.1080/03602532.2017.1326498. Epub 2017 May 31. Review.

PMID:
28468514
6.

Discovery of N-((3R,4R)-4-Fluoro-1-(6-((3-methoxy-1-methyl-1H-pyrazol-4-yl)amino)-9-methyl-9H-purin-2-yl)pyrrolidine-3-yl)acrylamide (PF-06747775) through Structure-Based Drug Design: A High Affinity Irreversible Inhibitor Targeting Oncogenic EGFR Mutants with Selectivity over Wild-Type EGFR.

Planken S, Behenna DC, Nair SK, Johnson TO, Nagata A, Almaden C, Bailey S, Ballard TE, Bernier L, Cheng H, Cho-Schultz S, Dalvie D, Deal JG, Dinh DM, Edwards MP, Ferre RA, Gajiwala KS, Hemkens M, Kania RS, Kath JC, Matthews J, Murray BW, Niessen S, Orr ST, Pairish M, Sach NW, Shen H, Shi M, Solowiej J, Tran K, Tseng E, Vicini P, Wang Y, Weinrich SL, Zhou R, Zientek M, Liu L, Luo Y, Xin S, Zhang C, Lafontaine J.

J Med Chem. 2017 Apr 13;60(7):3002-3019. doi: 10.1021/acs.jmedchem.6b01894. Epub 2017 Mar 29.

PMID:
28287730
7.

Biotransformation and bioactivation reactions - 2015 literature highlights.

Baillie TA, Dalvie D, Rietjens IM, Cyrus Khojasteh S.

Drug Metab Rev. 2016 May;48(2):113-38. doi: 10.1080/03602532.2016.1195404. Review.

PMID:
27362326
8.

Cytochrome P450 and Non-Cytochrome P450 Oxidative Metabolism: Contributions to the Pharmacokinetics, Safety, and Efficacy of Xenobiotics.

Foti RS, Dalvie DK.

Drug Metab Dispos. 2016 Aug;44(8):1229-45. doi: 10.1124/dmd.116.071753. Epub 2016 Jun 13. Erratum in: Drug Metab Dispos. 2016 Sep;44(9):1516.

PMID:
27298339
9.

Species Differences in the Oxidative Desulfurization of a Thiouracil-Based Irreversible Myeloperoxidase Inactivator by Flavin-Containing Monooxygenase Enzymes.

Eng H, Sharma R, Wolford A, Di L, Ruggeri RB, Buckbinder L, Conn EL, Dalvie DK, Kalgutkar AS.

Drug Metab Dispos. 2016 Aug;44(8):1262-9. doi: 10.1124/dmd.116.070185. Epub 2016 Apr 14.

PMID:
27079250
10.

Discovery of 1-{(3R,4R)-3-[({5-Chloro-2-[(1-methyl-1H-pyrazol-4-yl)amino]-7H-pyrrolo[2,3-d]pyrimidin-4-yl}oxy)methyl]-4-methoxypyrrolidin-1-yl}prop-2-en-1-one (PF-06459988), a Potent, WT Sparing, Irreversible Inhibitor of T790M-Containing EGFR Mutants.

Cheng H, Nair SK, Murray BW, Almaden C, Bailey S, Baxi S, Behenna D, Cho-Schultz S, Dalvie D, Dinh DM, Edwards MP, Feng JL, Ferre RA, Gajiwala KS, Hemkens MD, Jackson-Fisher A, Jalaie M, Johnson TO, Kania RS, Kephart S, Lafontaine J, Lunney B, Liu KK, Liu Z, Matthews J, Nagata A, Niessen S, Ornelas MA, Orr ST, Pairish M, Planken S, Ren S, Richter D, Ryan K, Sach N, Shen H, Smeal T, Solowiej J, Sutton S, Tran K, Tseng E, Vernier W, Walls M, Wang S, Weinrich SL, Xin S, Xu H, Yin MJ, Zientek M, Zhou R, Kath JC.

J Med Chem. 2016 Mar 10;59(5):2005-24. doi: 10.1021/acs.jmedchem.5b01633. Epub 2016 Jan 28.

PMID:
26756222
11.

Contribution of membrane trafficking perturbation to retinal toxicity.

Khoh-Reiter S, Sokolowski SA, Jessen B, Evans M, Dalvie D, Lu S.

Toxicol Sci. 2015 Jun;145(2):383-95. doi: 10.1093/toxsci/kfv059. Epub 2015 Mar 13.

PMID:
25771199
12.

Metabolism of xenobiotics by aldehyde oxidase.

Dalvie D, Zientek M.

Curr Protoc Toxicol. 2015 Feb 2;63:4.41.1-13. doi: 10.1002/0471140856.tx0441s63.

PMID:
25645247
13.

Practical approaches to resolving reactive metabolite liabilities in early discovery.

Dalvie D, Kalgutkar AS, Chen W.

Drug Metab Rev. 2015 Feb;47(1):56-70. doi: 10.3109/03602532.2014.984813. Epub 2014 Nov 20. Review.

PMID:
25410913
14.

Predicting toxicities of reactive metabolite-positive drug candidates.

Kalgutkar AS, Dalvie D.

Annu Rev Pharmacol Toxicol. 2015;55:35-54. doi: 10.1146/annurev-pharmtox-010814-124720. Epub 2014 Oct 6. Review.

PMID:
25292426
15.

Metabolites in safety testing assessment in early clinical development: a case study with a glucokinase activator.

Sharma R, Litchfield J, Atkinson K, Eng H, Amin NB, Denney WS, Pettersen JC, Goosen TC, Di L, Lee E, Pfefferkorn JA, Dalvie DK, Kalgutkar AS.

Drug Metab Dispos. 2014 Nov;42(11):1926-39. doi: 10.1124/dmd.114.060087. Epub 2014 Aug 20.

PMID:
25142735
16.

Metabolism, excretion and pharmacokinetics of [14C]crizotinib following oral administration to healthy subjects.

Johnson TR, Tan W, Goulet L, Smith EB, Yamazaki S, Walker GS, O'Gorman MT, Bedarida G, Zou HY, Christensen JG, Nguyen LN, Shen Z, Dalvie D, Bello A, Smith BJ.

Xenobiotica. 2015 Jan;45(1):45-59. doi: 10.3109/00498254.2014.941964. Epub 2014 Jul 18.

PMID:
25034009
17.

Pharmacokinetics, metabolism, and excretion of [14C]axitinib, a vascular endothelial growth factor receptor tyrosine kinase inhibitor, in humans.

Smith BJ, Pithavala Y, Bu HZ, Kang P, Hee B, Deese AJ, Pool WF, Klamerus KJ, Wu EY, Dalvie DK.

Drug Metab Dispos. 2014 May;42(5):918-31. doi: 10.1124/dmd.113.056531. Epub 2014 Mar 7.

PMID:
24608633
18.

A simple litmus test for aldehyde oxidase metabolism of heteroarenes.

O'Hara F, Burns AC, Collins MR, Dalvie D, Ornelas MA, Vaz AD, Fujiwara Y, Baran PS.

J Med Chem. 2014 Feb 27;57(4):1616-20. doi: 10.1021/jm4017976. Epub 2014 Feb 5.

19.

Covalent EGFR inhibitor analysis reveals importance of reversible interactions to potency and mechanisms of drug resistance.

Schwartz PA, Kuzmic P, Solowiej J, Bergqvist S, Bolanos B, Almaden C, Nagata A, Ryan K, Feng J, Dalvie D, Kath JC, Xu M, Wani R, Murray BW.

Proc Natl Acad Sci U S A. 2014 Jan 7;111(1):173-8. doi: 10.1073/pnas.1313733111. Epub 2013 Dec 17.

20.

Structure-based design, SAR analysis and antitumor activity of PI3K/mTOR dual inhibitors from 4-methylpyridopyrimidinone series.

Cheng H, Hoffman JE, Le PT, Pairish M, Kania R, Farrell W, Bagrodia S, Yuan J, Sun S, Zhang E, Xiang C, Dalvie D, Rahavendran SV.

Bioorg Med Chem Lett. 2013 May 1;23(9):2787-92. doi: 10.1016/j.bmcl.2013.02.020. Epub 2013 Feb 13.

PMID:
23506825
21.

N-(Pyridin-2-yl) arylsulfonamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1: strategies to eliminate reactive metabolites.

Nair SK, Matthews JJ, Cripps SJ, Cheng H, Hoffman JE, Smith C, Kupchinsky S, Siu M, Taylor WD, Wang Y, Johnson TO, Dress KR, Edwards MP, Zhou S, Hosea NA, Lapaglia A, Kang P, Castro A, Ermolieff J, Fanjul A, Vogel JE, Rejto P, Dalvie D.

Bioorg Med Chem Lett. 2013 Apr 15;23(8):2344-8. doi: 10.1016/j.bmcl.2013.02.066. Epub 2013 Feb 24.

PMID:
23489629
22.

Which metabolites circulate?

Loi CM, Smith DA, Dalvie D.

Drug Metab Dispos. 2013 May;41(5):933-51. doi: 10.1124/dmd.112.050278. Epub 2013 Mar 1.

PMID:
23454828
23.

Pharmacokinetics and metabolism of 2-aminothiazoles with antiprion activity in mice.

Silber BM, Rao S, Fife KL, Gallardo-Godoy A, Renslo AR, Dalvie DK, Giles K, Freyman Y, Elepano M, Gever JR, Li Z, Jacobson MP, Huang Y, Benet LZ, Prusiner SB.

Pharm Res. 2013 Apr;30(4):932-50. doi: 10.1007/s11095-012-0912-4. Epub 2013 Feb 16.

24.

Strategies for a comprehensive understanding of metabolism by aldehyde oxidase.

Hutzler JM, Obach RS, Dalvie D, Zientek MA.

Expert Opin Drug Metab Toxicol. 2013 Feb;9(2):153-68. doi: 10.1517/17425255.2013.738668. Epub 2012 Dec 12. Review.

PMID:
23231678
25.

The generation, detection, and effects of reactive drug metabolites.

Stachulski AV, Baillie TA, Park BK, Obach RS, Dalvie DK, Williams DP, Srivastava A, Regan SL, Antoine DJ, Goldring CE, Chia AJ, Kitteringham NR, Randle LE, Callan H, Castrejon JL, Farrell J, Naisbitt DJ, Lennard MS.

Med Res Rev. 2013 Sep;33(5):985-1080. doi: 10.1002/med.21273. Epub 2012 Oct 22. Review.

PMID:
23090860
26.

Interspecies variation in the metabolism of zoniporide by aldehyde oxidase.

Dalvie D, Xiang C, Kang P, Zhou S.

Xenobiotica. 2013 May;43(5):399-408. doi: 10.3109/00498254.2012.727499. Epub 2012 Oct 10.

PMID:
23046389
27.

Design and synthesis of a novel pyrrolidinyl pyrido pyrimidinone derivative as a potent inhibitor of PI3Kα and mTOR.

Le PT, Cheng H, Ninkovic S, Plewe M, Huang X, Wang H, Bagrodia S, Sun S, Knighton DR, LaFleur Rogers CM, Pannifer A, Greasley S, Dalvie D, Zhang E.

Bioorg Med Chem Lett. 2012 Aug 1;22(15):5098-103. doi: 10.1016/j.bmcl.2012.05.100. Epub 2012 Jun 6. Erratum in: Bioorg Med Chem Lett. 2012 Nov 1;22(21):6774.

PMID:
22749419
28.

Drug discovery for a new generation of covalent drugs.

Kalgutkar AS, Dalvie DK.

Expert Opin Drug Discov. 2012 Jul;7(7):561-81. doi: 10.1517/17460441.2012.688744. Epub 2012 May 19. Review. Erratum in: Expert Opin Drug Discov. 2012 Sep;7(9):861.

PMID:
22607458
29.

Effect of structural variation on aldehyde oxidase-catalyzed oxidation of zoniporide.

Dalvie D, Sun H, Xiang C, Hu Q, Jiang Y, Kang P.

Drug Metab Dispos. 2012 Aug;40(8):1575-87. doi: 10.1124/dmd.112.045823. Epub 2012 May 15.

PMID:
22587988
30.

Boston Society's 7th Applied Pharmaceutical Analysis.

Kumar G, Weiner R, Vick A, Xia C, Dalvie D, Bateman K, Ramanathan R.

Bioanalysis. 2012 Jan;4(1):9-12. doi: 10.4155/bio.11.292. No abstract available.

31.

Why do metabolites circulate?

Smith DA, Dalvie D.

Xenobiotica. 2012 Jan;42(1):107-26. doi: 10.3109/00498254.2011.630110. Epub 2011 Nov 24. Review.

PMID:
22115420
32.

Use of a multistaged time-dependent inhibition assay to assess the impact of intestinal metabolism on drug-drug interaction potential.

Zientek M, Dalvie D.

Drug Metab Dispos. 2012 Mar;40(3):467-73. doi: 10.1124/dmd.111.043257. Epub 2011 Nov 23.

PMID:
22112384
33.

Myeloperoxidase-mediated bioactivation of 5-hydroxythiabendazole: a possible mechanism of thiabendazole toxicity.

Jamieson JD, Smith EB, Dalvie DK, Stevens GJ, Yanochko GM.

Toxicol In Vitro. 2011 Aug;25(5):1061-6. doi: 10.1016/j.tiv.2011.04.007. Epub 2011 Apr 12.

PMID:
21513789
34.

Design and synthesis of novel N-hydroxy-dihydronaphthyridinones as potent and orally bioavailable HIV-1 integrase inhibitors.

Johnson TW, Tanis SP, Butler SL, Dalvie D, Delisle DM, Dress KR, Flahive EJ, Hu Q, Kuehler JE, Kuki A, Liu W, McClellan GA, Peng Q, Plewe MB, Richardson PF, Smith GL, Solowiej J, Tran KT, Wang H, Yu X, Zhang J, Zhu H.

J Med Chem. 2011 May 12;54(9):3393-417. doi: 10.1021/jm200208d. Epub 2011 Apr 13.

PMID:
21446745
35.

Comparison of in vitro metabolism of ticlopidine by human cytochrome P450 2B6 and rabbit cytochrome P450 2B4.

Talakad JC, Shah MB, Walker GS, Xiang C, Halpert JR, Dalvie D.

Drug Metab Dispos. 2011 Mar;39(3):539-50. doi: 10.1124/dmd.110.037101. Epub 2010 Dec 14.

36.

Azaindole N-methyl hydroxamic acids as HIV-1 integrase inhibitors-II. The impact of physicochemical properties on ADME and PK.

Tanis SP, Plewe MB, Johnson TW, Butler SL, Dalvie D, DeLisle D, Dress KR, Hu Q, Huang B, Kuehler JE, Kuki A, Liu W, Peng Q, Smith GL, Solowiej J, Tran KT, Wang H, Yang A, Yin C, Yu X, Zhang J, Zhu H.

Bioorg Med Chem Lett. 2010 Dec 15;20(24):7429-34. doi: 10.1016/j.bmcl.2010.10.022. Epub 2010 Oct 13.

PMID:
21036042
37.

Aldehyde oxidase: an enzyme of emerging importance in drug discovery.

Pryde DC, Dalvie D, Hu Q, Jones P, Obach RS, Tran TD.

J Med Chem. 2010 Dec 23;53(24):8441-60. doi: 10.1021/jm100888d. Epub 2010 Sep 20. No abstract available.

PMID:
20853847
38.

Cross-species comparison of the metabolism and excretion of zoniporide: contribution of aldehyde oxidase to interspecies differences.

Dalvie D, Zhang C, Chen W, Smolarek T, Obach RS, Loi CM.

Drug Metab Dispos. 2010 Apr;38(4):641-54. doi: 10.1124/dmd.109.030783. Epub 2009 Dec 29.

PMID:
20040581
39.

Identification of novel substrates for human cytochrome P450 2J2.

Lee CA, Neul D, Clouser-Roche A, Dalvie D, Wester MR, Jiang Y, Jones JP 3rd, Freiwald S, Zientek M, Totah RA.

Drug Metab Dispos. 2010 Feb;38(2):347-56. doi: 10.1124/dmd.109.030270. Epub 2009 Nov 18.

PMID:
19923256
40.

A holistic strategy for characterizing the safety of metabolites through drug discovery and development.

Walker D, Brady J, Dalvie D, Davis J, Dowty M, Duncan JN, Nedderman A, Obach RS, Wright P.

Chem Res Toxicol. 2009 Oct;22(10):1653-62. doi: 10.1021/tx900213j. Review.

PMID:
19715349
41.

Effect of intestinal glucuronidation in limiting hepatic exposure and bioactivation of raloxifene in humans and rats.

Dalvie D, Kang P, Zientek M, Xiang C, Zhou S, Obach RS.

Chem Res Toxicol. 2008 Dec;21(12):2260-71. doi: 10.1021/tx800323w.

PMID:
19548350
42.

Assessment of three human in vitro systems in the generation of major human excretory and circulating metabolites.

Dalvie D, Obach RS, Kang P, Prakash C, Loi CM, Hurst S, Nedderman A, Goulet L, Smith E, Bu HZ, Smith DA.

Chem Res Toxicol. 2009 Feb;22(2):357-68. doi: 10.1021/tx8004357.

PMID:
19146377
43.

Bioactivation of lumiracoxib by peroxidases and human liver microsomes: identification of multiple quinone imine intermediates and GSH adducts.

Kang P, Dalvie D, Smith E, Renner M.

Chem Res Toxicol. 2009 Jan;22(1):106-17. doi: 10.1021/tx8002356.

PMID:
19063590
44.

Pharmacokinetics, metabolism, and excretion of torcetrapib, a cholesteryl ester transfer protein inhibitor, in humans.

Dalvie D, Chen W, Zhang C, Vaz AD, Smolarek TA, Cox LM, Lin J, Obach RS.

Drug Metab Dispos. 2008 Nov;36(11):2185-98. doi: 10.1124/dmd.108.023176. Epub 2008 Aug 11.

PMID:
18694908
45.
47.

Bioactivation of flutamide metabolites by human liver microsomes.

Kang P, Dalvie D, Smith E, Zhou S, Deese A, Nieman JA.

Drug Metab Dispos. 2008 Jul;36(7):1425-37. doi: 10.1124/dmd.108.020370. Epub 2008 Apr 14.

PMID:
18411402
48.

NADPH-dependent covalent binding of [3H]paroxetine to human liver microsomes and S-9 fractions: identification of an electrophilic quinone metabolite of paroxetine.

Zhao SX, Dalvie DK, Kelly JM, Soglia JR, Frederick KS, Smith EB, Obach RS, Kalgutkar AS.

Chem Res Toxicol. 2007 Nov;20(11):1649-57. Epub 2007 Oct 2.

PMID:
17907785
49.
50.

Identification of a novel glutathione conjugate of flutamide in incubations with human liver microsomes.

Kang P, Dalvie D, Smith E, Zhou S, Deese A.

Drug Metab Dispos. 2007 Jul;35(7):1081-8. Epub 2007 Apr 2.

PMID:
17403914

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