Search Results - "Kenaan, Cesar"

Mechanism-Based Inactivation of Human Cytochrome P450 2B6 by Chlorpyrifos by D’Agostino, Jaime, Zhang, Haoming, Kenaan, Cesar, Hollenberg, Paul F

“…Chlorpyrifos (CPS) is a commonly used pesticide which is metabolized by P450s into the toxic metabolite chlorpyrifos-oxon (CPO). Metabolism also results in the…”
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Polymorphic variants of cytochrome P450 2B6 (CYP2B6.4-CYP2B6.9) exhibit altered rates of metabolism for bupropion and efavirenz: a charge-reversal mutation in the K139E variant (CYP2B6.8) impairs formation of a functional cytochrome p450-reductase complex by Zhang, Haoming, Sridar, Chitra, Kenaan, Cesar, Amunugama, Hemali, Ballou, David P, Hollenberg, Paul F

“…In this study, metabolism of bupropion, efavirenz, and 7-ethoxy-4-trifluoromethylcoumarin (7-EFC) by CYP2B6 wild type (CYP2B6.1) and six polymorphic variants…”
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Inhibition of bupropion metabolism by selegiline: mechanism-based inactivation of human CYP2B6 and characterization of glutathione and peptide adducts by Sridar, Chitra, Kenaan, Cesar, Hollenberg, Paul F

“…Selegiline, the R-enantiomer of deprenyl, is used in the treatment of Parkinson's disease. Bupropion, an antidepressant, often used to treat patients in…”
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Uncovering the Role of Hydrophobic Residues in Cytochrome P450−Cytochrome P450 Reductase Interactions by Kenaan, Cesar, Zhang, Haoming, Shea, Erin V, Hollenberg, Paul F

“…Cytochrome P450 (CYP or P450)-mediated drug metabolism requires the interaction of P450s with their redox partner, cytochrome P450 reductase (CPR). In this…”
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Effect of Conformational Dynamics on Substrate Recognition and Specificity as Probed by the Introduction of a de Novo Disulfide Bond into Cytochrome P450 2B1 by Zhang, Haoming, Kenaan, Cesar, Hamdane, Djemel, Hoa, Gaston Hui Bon, Hollenberg, Paul F.

“…The conformational dynamics of cytochrome P450 2B1 (CYP2B1) were investigated through the introduction of a disulfide bond to link the I- and K-helices by…”
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Identification of the residue in human CYP3A4 that is covalently modified by bergamottin and the reactive intermediate that contributes to the grapefruit juice effect by Lin, Hsia-Lien, Kenaan, Cesar, Hollenberg, Paul F

“…Previous studies have demonstrated that bergamottin (BG), a component of grapefruit juice, is a mechanism-based inactivator of CYP3A4 and contributes, in part,…”
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The effect of ritonavir on human CYP2B6 catalytic activity: heme modification contributes to the mechanism-based inactivation of CYP2B6 and CYP3A4 by ritonavir by Lin, Hsia-lien, D'Agostino, Jaime, Kenaan, Cesar, Calinski, Diane, Hollenberg, Paul F

“…The mechanism-based inactivation of human CYP2B6 by ritonavir (RTV) in a reconstituted system was investigated. The inactivation is time, concentration, and…”
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Reaction of Human Cytochrome P450 3A4 with Peroxynitrite: Nitrotyrosine Formation on the Proximal Side Impairs Its Interaction with NADPH-Cytochrome P450 Reductase by Lin, Hsia-lien, Kenaan, Cesar, Zhang, Haoming, Hollenberg, Paul F

“…The reaction of peroxynitrite (PN) with purified human cytochrome P450 3A4 (CYP3A4) resulted in the loss of the reduced-CO difference spectrum, but the…”
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A quantitative high-throughput 96-well plate fluorescence assay for mechanism-based inactivators of cytochromes P450 exemplified using CYP2B6 by Hollenberg, Paul F, Kenaan, Cesar, Zhang, Haoming

“…Mechanism-based inactivators such as bergamottin are useful chemical tools for identifying the functions of specific active-site amino acid residues in the…”
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Roles of Residues F206 and V367 in Human CYP2B6: Effects of Mutations on Androgen Hydroxylation, Mechanism-Based Inactivation, and Reversible Inhibition by Lin, Hsia-Lien, Zhang, Haoming, Kenaan, Cesar, Hollenberg, Paul F

“…The crystal structures of human CYP2B6 indicate that Phe206 and Val367 are in close proximity to the substrate binding site and suggest that both residues may…”
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Targeting of the highly conserved threonine 302 residue of cytochromes P450 2B family during mechanism-based inactivation by aryl acetylenes by Zhang, Haoming, Lin, Hsia-lien, Kenaan, Cesar, Hollenberg, Paul F.

“…► Thr302 is susceptible to mechanism-based inactivation by aryl acetylenes. ► Thr302 forms an ester adduct with the reactive intermediate of tBPA, leading to…”
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Interactions between CYP2E1 and CYP2B4: effects on affinity for NADPH-cytochrome P450 reductase and substrate metabolism by Kenaan, Cesar, Shea, Erin V, Lin, Hsia-lien, Zhang, Haoming, Pratt-Hyatt, Matthew J, Hollenberg, Paul F

“…Studies in microsomal and reconstituted systems have shown that the presence of one cytochrome P450 isoform can significantly influence the catalytic activity…”
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CYP2E1 competes with CYP2B4 for limited NADPH‐Cytochrome P450 Reductase by Kenaan, Cesar, Shea, Erin V, Zhang, Haoming, Pratt‐Hyatt, Matthew, Hollenberg, Paul F

“…For efficient catalysis to occur, cytochromes P450 (CYPs or P450s) require an interaction with their physiological redox partner, cytochrome P450 reductase…”
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High-throughput fluorescence assay for cytochrome P450 mechanism-based inactivators by Kenaan, Cesar, Zhang, Haoming, Hollenberg, Paul F

“…The mechanism-based inactivation (MBI) of the human cytochrome P450 (P450 or CYP) drug-metabolizing enzymes may lead to adverse drug-drug interactions,…”
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Investigating the effects and mechanisms of interaction between cytochrome P450 2B4, cytochrome P450 2E1 and cytochrome P450 reductase by Kenaan, Cesar

“…A requirement for cytochrome P450 (CYP or P450)-mediated drug metabolism is the association of P450s with cytochrome P450 reductase (CPR). Although P450s form…”
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