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Items: 1 to 50 of 73

1.

Modeling the pharmacokinetic-pharmacodynamic relationship of the monoclonal anti-macaque-IL-15 antibody Hu714MuXHu in cynomolgus monkeys.

Pan WJ, Li H, Xiao JJ, Horner MJ, Lebrec HN, Butz EA, Kaliyaperumal A, Cheah TC, Ortiz RC, Prokop SP, Buntich SA, Boren BM, Wolford ST, Tsuji WH, Wienkers LC, Köck K.

Pharmacol Res Perspect. 2016 Jan 11;3(6):e00199. doi: 10.1002/prp2.199. eCollection 2015 Dec.

2.

Characterization of ritonavir-mediated inactivation of cytochrome P450 3A4.

Rock BM, Hengel SM, Rock DA, Wienkers LC, Kunze KL.

Mol Pharmacol. 2014 Dec;86(6):665-74. doi: 10.1124/mol.114.094862. Epub 2014 Oct 1.

PMID:
25274602
3.

Evaluation of near infrared fluorescent labeling of monoclonal antibodies as a tool for tissue distribution.

Conner KP, Rock BM, Kwon GK, Balthasar JP, Abuqayyas L, Wienkers LC, Rock DA.

Drug Metab Dispos. 2014 Nov;42(11):1906-13. doi: 10.1124/dmd.114.060319. Epub 2014 Sep 10. Erratum in: Drug Metab Dispos. 2015 Jan;43(1):53.

PMID:
25209366
4.

Characterization of the active site properties of CYP4F12.

Eksterowicz J, Rock DA, Rock BM, Wienkers LC, Foti RS.

Drug Metab Dispos. 2014 Oct;42(10):1698-707. doi: 10.1124/dmd.114.059626. Epub 2014 Jul 29.

PMID:
25074871
5.

Multienzyme kinetics and sequential metabolism.

Wienkers LC, Rock B.

Methods Mol Biol. 2014;1113:93-118. doi: 10.1007/978-1-62703-758-7_6. Review.

PMID:
24523110
6.

Cytochrome P450 Enzyme Metabolites in Lead Discovery and Development.

Kandel SE, Wienkers LC, Lampe JN.

Annu Rep Med Chem. 2014;49:347-359.

7.

An extended range generic immunoassay for total human therapeutic antibodies in preclinical pharmacokinetic studies.

Hall CM, Pearson JT, Patel V, Wienkers LC, Greene RJ.

J Immunol Methods. 2013 Jul 31;393(1-2):70-3. doi: 10.1016/j.jim.2013.03.011. Epub 2013 Apr 6.

PMID:
23570944
8.

Evaluation of UGT protein interactions in human hepatocytes: effect of siRNA down regulation of UGT1A9 and UGT2B7 on propofol glucuronidation in human hepatocytes.

Konopnicki CM, Dickmann LJ, Tracy JM, Tukey RH, Wienkers LC, Foti RS.

Arch Biochem Biophys. 2013 Jul 15;535(2):143-9. doi: 10.1016/j.abb.2013.03.012. Epub 2013 Apr 4.

9.

Pharmacology of AMG 181, a human anti-α4 β7 antibody that specifically alters trafficking of gut-homing T cells.

Pan WJ, Hsu H, Rees WA, Lear SP, Lee F, Foltz IN, Rathanaswami P, Manchulenko K, Chan BM, Zhang M, Xia XZ, Patel SK, Prince PJ, Doherty DR, Sheckler CM, Reynhardt KO, Krill CD, Harder BJ, Wisler JA, Brandvig JL, Lynch JL, Anderson AA, Wienkers LC, Borie DC.

Br J Pharmacol. 2013 May;169(1):51-68. doi: 10.1111/bph.12134.

10.

Predicting the drug interaction potential of AMG 853, a dual antagonist of the D-prostanoid and chemoattractant receptor-homologous molecule expressed on T helper 2 cells receptors.

Foti RS, Pearson JT, Wong SL, Zalikowski JA, Boudreaux MD, Prokop SP, Davis JA, Banfield C, Emery MG, Rock DA, Wahlstrom JL, Wienkers LC, Amore BM.

Drug Metab Dispos. 2012 Dec;40(12):2239-49. doi: 10.1124/dmd.112.047928. Epub 2012 Aug 28.

PMID:
22930276
11.

Impact of organic solvents on cytochrome P450 probe reactions: filling the gap with (S)-Warfarin and midazolam hydroxylation.

González-Pérez V, Connolly EA, Bridges AS, Wienkers LC, Paine MF.

Drug Metab Dispos. 2012 Nov;40(11):2136-42. doi: 10.1124/dmd.112.047134. Epub 2012 Aug 15.

12.

Cytochrome p450 architecture and cysteine nucleophile placement impact raloxifene-mediated mechanism-based inactivation.

VandenBrink BM, Davis JA, Pearson JT, Foti RS, Wienkers LC, Rock DA.

Mol Pharmacol. 2012 Nov;82(5):835-42. doi: 10.1124/mol.112.080739. Epub 2012 Aug 2.

PMID:
22859722
13.

In vitro characterization of the drug-drug interaction potential of catabolites of antibody-maytansinoid conjugates.

Davis JA, Rock DA, Wienkers LC, Pearson JT.

Drug Metab Dispos. 2012 Oct;40(10):1927-34. doi: 10.1124/dmd.112.046169. Epub 2012 Jun 29.

PMID:
22752008
14.

Effects of interleukin 1β (IL-1β) and IL-1β/interleukin 6 (IL-6) combinations on drug metabolizing enzymes in human hepatocyte culture.

Dickmann LJ, Patel SK, Wienkers LC, Slatter JG.

Curr Drug Metab. 2012 Sep 1;13(7):930-7.

PMID:
22475267
15.

Murine collagen antibody induced arthritis (CAIA) and primary mouse hepatocyte culture as models to study cytochrome P450 suppression.

Dickmann LJ, McBride HJ, Patel SK, Miner K, Wienkers LC, Slatter JG.

Biochem Pharmacol. 2012 Jun 15;83(12):1682-9. doi: 10.1016/j.bcp.2012.03.001. Epub 2012 Mar 10.

PMID:
22425536
16.

Ligand-based design of a potent and selective inhibitor of cytochrome P450 2C19.

Foti RS, Rock DA, Han X, Flowers RA, Wienkers LC, Wahlstrom JL.

J Med Chem. 2012 Feb 9;55(3):1205-14. doi: 10.1021/jm201346g. Epub 2012 Jan 31.

PMID:
22239545
17.

Prediction of CYP2D6 drug interactions from in vitro data: evidence for substrate-dependent inhibition.

VandenBrink BM, Foti RS, Rock DA, Wienkers LC, Wahlstrom JL.

Drug Metab Dispos. 2012 Jan;40(1):47-53. doi: 10.1124/dmd.111.041210. Epub 2011 Oct 5.

PMID:
21976621
18.

Formation of raloxifene homo-dimer in CYP3A4, evidence for multi-substrate binding in a single catalytically competent P450 active site.

Davis JA, Greene RJ, Han S, Rock DA, Wienkers LC.

Arch Biochem Biophys. 2011 Sep 15;513(2):110-8. doi: 10.1016/j.abb.2011.06.016. Epub 2011 Jul 13.

PMID:
21767526
19.

Evaluation of CYP2C8 inhibition in vitro: utility of montelukast as a selective CYP2C8 probe substrate.

VandenBrink BM, Foti RS, Rock DA, Wienkers LC, Wahlstrom JL.

Drug Metab Dispos. 2011 Sep;39(9):1546-54. doi: 10.1124/dmd.111.039065. Epub 2011 Jun 22.

PMID:
21697463
20.

Effects of interleukin-6 (IL-6) and an anti-IL-6 monoclonal antibody on drug-metabolizing enzymes in human hepatocyte culture.

Dickmann LJ, Patel SK, Rock DA, Wienkers LC, Slatter JG.

Drug Metab Dispos. 2011 Aug;39(8):1415-22. doi: 10.1124/dmd.111.038679. Epub 2011 May 9.

PMID:
21555507
21.

Mechanism-based inactivation of cytochrome P450 3A4 by mibefradil through heme destruction.

Foti RS, Rock DA, Pearson JT, Wahlstrom JL, Wienkers LC.

Drug Metab Dispos. 2011 Jul;39(7):1188-95. doi: 10.1124/dmd.111.038505. Epub 2011 Mar 29.

PMID:
21447734
22.

Preclinical profiling in drug discovery. Editorial.

Wienkers LC.

Comb Chem High Throughput Screen. 2010 Feb;13(2):88-9. No abstract available.

PMID:
20344828
23.

Selection of alternative CYP3A4 probe substrates for clinical drug interaction studies using in vitro data and in vivo simulation.

Foti RS, Rock DA, Wienkers LC, Wahlstrom JL.

Drug Metab Dispos. 2010 Jun;38(6):981-7. doi: 10.1124/dmd.110.032094. Epub 2010 Mar 4.

PMID:
20203109
24.

In vitro modulation of cytochrome P450 reductase supported indoleamine 2,3-dioxygenase activity by allosteric effectors cytochrome b(5) and methylene blue.

Pearson JT, Siu S, Meininger DP, Wienkers LC, Rock DA.

Biochemistry. 2010 Mar 30;49(12):2647-56. doi: 10.1021/bi100022c.

PMID:
20178337
25.

Application of cytochrome P450 drug interaction screening in drug discovery.

Foti RS, Wienkers LC, Wahlstrom JL.

Comb Chem High Throughput Screen. 2010 Feb;13(2):145-58. Review.

PMID:
20053168
26.

In vitro inhibition of multiple cytochrome P450 isoforms by xanthone derivatives from mangosteen extract.

Foti RS, Pearson JT, Rock DA, Wahlstrom JL, Wienkers LC.

Drug Metab Dispos. 2009 Sep;37(9):1848-55. doi: 10.1124/dmd.109.028043. Epub 2009 Jun 18.

PMID:
19541824
27.

Assessment of the metabolism and intrinsic reactivity of a novel catechol metabolite.

Hutzler JM, Melton RJ, Rumsey JM, Thompson DC, Rock DA, Wienkers LC.

Chem Res Toxicol. 2008 May;21(5):1125-33. doi: 10.1021/tx700429v. Epub 2008 Apr 12.

PMID:
18407675
28.

Differential time-dependent inactivation of P450 3A4 and P450 3A5 by raloxifene: a key role for C239 in quenching reactive intermediates.

Pearson JT, Wahlstrom JL, Dickmann LJ, Kumar S, Halpert JR, Wienkers LC, Foti RS, Rock DA.

Chem Res Toxicol. 2007 Dec;20(12):1778-86. Epub 2007 Nov 15.

PMID:
18001057
29.

Time-dependent inactivation of P450 3A4 by raloxifene: identification of Cys239 as the site of apoprotein alkylation.

Baer BR, Wienkers LC, Rock DA.

Chem Res Toxicol. 2007 Jun;20(6):954-64. Epub 2007 May 12.

PMID:
17497897
30.

CYP2C9 protein interactions with cytochrome b(5): effects on the coupling of catalysis.

Locuson CW, Wienkers LC, Jones JP, Tracy TS.

Drug Metab Dispos. 2007 Jul;35(7):1174-81. Epub 2007 Apr 19.

31.

Inhibition of cytochrome P450 3A4 by a pyrimidineimidazole: Evidence for complex heme interactions.

Hutzler JM, Melton RJ, Rumsey JM, Schnute ME, Locuson CW, Wienkers LC.

Chem Res Toxicol. 2006 Dec;19(12):1650-9.

PMID:
17173379
32.

Advances in predicting CYP-mediated drug interactions in the drug discovery setting.

Wahlstrom JL, Rock DA, Slatter JG, Wienkers LC.

Expert Opin Drug Discov. 2006 Dec;1(7):677-91. doi: 10.1517/17460441.1.7.677.

PMID:
23495993
33.

The in vitro drug interaction potential of dietary supplements containing multiple herbal components.

Foti RS, Wahlstrom JL, Wienkers LC.

Drug Metab Dispos. 2007 Feb;35(2):185-8. Epub 2006 Nov 8.

PMID:
17093003
34.

Mechanism of inactivation of human cytochrome P450 2B6 by phencyclidine.

Jushchyshyn MI, Wahlstrom JL, Hollenberg PF, Wienkers LC.

Drug Metab Dispos. 2006 Sep;34(9):1523-9. Epub 2006 Jun 16.

PMID:
16782764
35.

Predicting in vivo drug interactions from in vitro drug discovery data.

Wienkers LC, Heath TG.

Nat Rev Drug Discov. 2005 Oct;4(10):825-33. Review.

PMID:
16224454
36.

Catalytic turnover of pyrene by CYP3A4: evidence that cytochrome b5 directly induces positive cooperativity.

Jushchyshyn MI, Hutzler JM, Schrag ML, Wienkers LC.

Arch Biochem Biophys. 2005 Jun 1;438(1):21-8. Epub 2005 Mar 5.

PMID:
15910734
37.

Predicting drug-drug interactions in drug discovery: where are we now and where are we going?

Hutzler M, Messing DM, Wienkers LC.

Curr Opin Drug Discov Devel. 2005 Jan;8(1):51-8. Review.

PMID:
15679172
39.

Characterization of bropirimine O-glucuronidation in human liver microsomes.

Wynalda MA, Wynalda KM, Amore BM, Fagerness PE, Wienkers LC.

Xenobiotica. 2003 Oct;33(10):999-1011.

PMID:
14555337
40.

Effect of carbonate anion on cytochrome P450 2D6-mediated metabolism in vitro: the potential role of multiple oxygenating species.

Hutzler JM, Powers FJ, Wynalda MA, Wienkers LC.

Arch Biochem Biophys. 2003 Sep 15;417(2):165-75.

PMID:
12941298
41.

In vitro metabolism of clindamycin in human liver and intestinal microsomes.

Wynalda MA, Hutzler JM, Koets MD, Podoll T, Wienkers LC.

Drug Metab Dispos. 2003 Jul;31(7):878-87.

PMID:
12814964
42.

Inhibition of cytochrome P450 2D6: structure-activity studies using a series of quinidine and quinine analogues.

Hutzler JM, Walker GS, Wienkers LC.

Chem Res Toxicol. 2003 Apr;16(4):450-9.

PMID:
12703961
43.

Activation of cytochrome P450 2C9-mediated metabolism: mechanistic evidence in support of kinetic observations.

Hutzler JM, Wienkers LC, Wahlstrom JL, Carlson TJ, Tracy TS.

Arch Biochem Biophys. 2003 Feb 1;410(1):16-24.

PMID:
12559973
44.

Identification of phenylisoxazolines as novel and viable antibacterial agents active against Gram-positive pathogens.

Barbachyn MR, Cleek GJ, Dolak LA, Garmon SA, Morris J, Seest EP, Thomas RC, Toops DS, Watt W, Wishka DG, Ford CW, Zurenko GE, Hamel JC, Schaadt RD, Stapert D, Yagi BH, Adams WJ, Friis JM, Slatter JG, Sams JP, Oien NL, Zaya MJ, Wienkers LC, Wynalda MA.

J Med Chem. 2003 Jan 16;46(2):284-302.

PMID:
12519066
46.

Pyrene.pyrene complexes at the active site of cytochrome P450 3A4: evidence for a multiple substrate binding site.

Dabrowski MJ, Schrag ML, Wienkers LC, Atkins WM.

J Am Chem Soc. 2002 Oct 9;124(40):11866-7.

PMID:
12358527
47.
48.

Triazolam substrate inhibition: evidence of competition for heme-bound reactive oxygen within the CYP3A4 active site.

Schrag ML, Wienkers LC.

Adv Exp Med Biol. 2001;500:347-50. No abstract available.

PMID:
11764967
49.
50.

Covalent alteration of the CYP3A4 active site: evidence for multiple substrate binding domains.

Schrag ML, Wienkers LC.

Arch Biochem Biophys. 2001 Jul 1;391(1):49-55.

PMID:
11414684

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