Search Results - "Wienkers, LC"

Factors confounding the successful extrapolation of in vitro CYP3A inhibition information to the in vivo condition by Wienkers, Larry C.

“…For the most part, the majority of adverse drug–drug interactions, which are pharmacokinetic in origin, can be understood in terms of alterations of cytochrome…”
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Predicting in vivo drug interactions from in vitro drug discovery data by Wienkers, Larry C, Heath, Timothy G

“…In vitro screening for drugs that inhibit cytochrome P450 enzymes is well established as a means for predicting potential metabolism-mediated drug interactions…”
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Pharmacology of AMG 181, a human anti‐α4β7 antibody that specifically alters trafficking of gut‐homing T cells by 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

“…Background and Purpose AMG 181 is a human anti‐α4β7 antibody currently in phase 1 and 2 trials in subjects with inflammatory bowel diseases. AMG 181…”
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Pyrene·Pyrene Complexes at the Active Site of Cytochrome P450 3A4:  Evidence for a Multiple Substrate Binding Site by Dabrowski, Michael J, Schrag, Michael L, Wienkers, Larry C, Atkins, William M

“…Cytochrome P450 monooxygenases (CYPs) metabolize nearly all drugs and toxins. Recently, it has become clear that CYPs exhibit both homotropic and heterotropic…”
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Pharmacology of AMG 181, a human anti-[alpha]4[beta]7 antibody that specifically alters trafficking of gut-homing T cells by 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

“…Background and Purpose AMG 181 is a human anti-[alpha]4[beta]7 antibody currently in phase 1 and 2 trials in subjects with inflammatory bowel diseases. AMG 181…”
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Pharmacology of AMG 181, a human anti‐α 4 β 7 antibody that specifically alters trafficking of gut‐homing T cells by 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

“…Background and Purpose AMG 181 is a human anti‐α 4 β 7 antibody currently in phase 1 and 2 trials in subjects with inflammatory bowel diseases. AMG 181…”
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Covalent Alteration of the CYP3A4 Active Site: Evidence for Multiple Substrate Binding Domains by Schrag, Michael L., Wienkers, Larry C.

“…The inhibition of CYP3A4-mediated oxidation of triazolam and testosterone was assessed in the presence of a selection of known CYP3A4 substrates and…”
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IN VITRO METABOLISM OF CLINDAMYCIN IN HUMAN LIVER AND INTESTINAL MICROSOMES by WYNALDA, Michael A, HUTZLER, J. Matthew, KOETS, Michael D, PODOLL, Terry, WIENKERS, Larry C

“…Incubations with human liver and gut microsomes revealed that the antibiotic, clindamycin, is primarily oxidized to form clindamycin sulfoxide. In this report,…”
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Topological Alteration of the CYP3A4 Active Site by the Divalent Cation Mg2 by SCHRAG, Michael L, WIENKERS, Larry C

“…Phenyldiazene reacted with lymphoblast-expressed CYP3A4 to give a stable phenyl-iron complex that could be induced to rearrange in situ producing approximately…”
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Inhibition of Cytochrome P450 2D6:  Structure−Activity Studies Using a Series of Quinidine and Quinine Analogues by Hutzler, J. Matthew, Walker, Gregory S, Wienkers, Larry C

“…Several pharmacophore models have suggested that substrates and inhibitors of cytochrome P450 2D6 (P450 2D6) possess a nitrogen with a positive charge that…”
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Bioactivation of the anticancer agent CPT-11 to SN-38 by human hepatic microsomal carboxylesterases and the in vitro assessment of potential drug interactions by SLATTER, J. G, SU, P, SAMS, J. P, SCHAAF, L. J, WIENKERS, L. C

“…Human hepatic microsomes were used to investigate the carboxylesterase-mediated bioactivation of CPT-11 to the active metabolite, SN-38. SN-38 formation…”
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Oxidation of the Novel Oxazolidinone Antibiotic Linezolid in Human Liver Microsomes by WYNALDA, M. A, HAUER, M. J, WIENKERS, L. C

“…In vitro studies were conducted to identify the hepatic enzyme(s) responsible for the oxidative metabolism of linezolid. In human liver microsomes, linezolid…”
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Triazolam Substrate Inhibition: Evidence of Competition for Heme-Bound Reactive Oxygen Within the CYP3A4 Active Site by SCHRAG, Michael L, WIENKERS, Larry C

“…In human liver microsomes, triazolam is principally metabolized by CYP3A4 to form two metabolites, 1′-hydroxytriazolam (1′OHTz) and 4-hydroxytriazolam…”
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Effect of carbonate anion on cytochrome P450 2D6-mediated metabolism in vitro: the potential role of multiple oxygenating species by Hutzler, J.Matthew, Powers, Frank J, Wynalda, Michael A, Wienkers, Larry C

“…Studies were designed to investigate various anions and their effects on cytochrome P450 2D6-mediated metabolism in vitro. Incubations were initially performed…”
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Cytochrome P-450-Mediated Metabolism of the Individual Enantiomers of the Antidepressant Agent Reboxetine in Human Liver Microsomes by WIENKERS, L. C, ALLIEVI, C, HAUER, M. J, WYNALDA, M. A

“…In vitro studies were conducted to identify the hepatic cytochrome P-450 (CYP) enzymes responsible for the oxidative metabolism of the individual enantiomers…”
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Mechanism-Based Inactivation of Cytochrome P450 2D6 by 1-[(2-Ethyl-4-methyl-1H-imidazol-5-yl)methyl]- 4-[4-(trifluoromethyl)-2-pyridinyl]piperazine:  Kinetic Characterization and Evidence for Apoprotein Adduction by Hutzler, J. Matthew, Steenwyk, Rick C, Smith, Evan B, Walker, Gregory S, Wienkers, Larry C

“…The kinetics for inactivation of cytochrome P450 2D6 by (1-[(2-ethyl-4-methyl-1H-imidazol-5-yl)methyl]-4-[4-(trifluoromethyl)-2-pyridinyl]piperazine (EMTPP)…”
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Assessment of Potential Interactions Between Dopamine Receptor Agonists and Various Human Cytochrome P450 Enzymes Using a Simple In Vitro Inhibition Screen by WYNALDA, M. A, WIENKERS, L. C

“…The selectivity of inhibition for four dopamine receptor agonists (pramipexole, ropinirole, pergolide, and bromocriptine) on six human cytochrome P450 enzyme…”
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Multiple Cytochrome P450 Enzymes Responsible for the Oxidative Metabolism of the Substituted (S)-3-Phenylpiperidine, (S,S)-3-[3-(Methylsulfonyl)phenyl]-1-propylpiperidine Hydrochloride, in Human Liver Microsomes by WIENKERS, Larry C, WYNALDA, Michael A

“…( S , S )-3-[3-(Methylsulfonyl)phenyl]-1-propylpiperidine hydrochloride [(−)-OSU6162] is a weak dopamine D2 receptor modulator that possesses potential for…”
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Formation of (R)-8-hydroxywarfarin in human liver microsomes. A new metabolic marker for the (S)-mephenytoin hydroxylase, P4502C19 by Wienkers, L C, Wurden, C J, Storch, E, Kunze, K L, Rettie, A E, Trager, W F

“…Kinetic studies demonstrate that two forms of human liver cytochrome P450 are responsible for the formation of (R)-8-hydroxywarfarin: a low-affinity enzyme (KM…”
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Problems associated with in vitro assessment of drug inhibition of CYP3A4 and other P-450 enzymes and its impact on drug discovery by Wienkers, Larry C

“…The cytochromes P-450 recognize and metabolize a broad range of structurally diverse therapeutic agents. As a consequence, many clinically relevant drug–drug…”
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