Search Results - "SRIDAR, Chitra"
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1
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
Published in The Journal of pharmacology and experimental therapeutics (01-09-2011)“…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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2
The inactivation of human CYP2E1 by phenethyl isothiocyanate, a naturally occurring chemopreventive agent, and its oxidative bioactivation
Published in Drug metabolism and disposition (01-04-2013)“…Phenethylisothiocyanate (PEITC), a naturally occurring isothiocyanate and potent cancer chemopreventive agent, works by multiple mechanisms, including the…”
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3
Inhibition of bupropion metabolism by selegiline: mechanism-based inactivation of human CYP2B6 and characterization of glutathione and peptide adducts
Published in Drug metabolism and disposition (01-12-2012)“…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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4
SILYBIN INACTIVATES CYTOCHROMES P450 3A4 AND 2C9 AND INHIBITS MAJOR HEPATIC GLUCURONOSYLTRANSFERASES
Published in Drug metabolism and disposition (01-06-2004)“…Silybin, a major constituent of the milk thistle, is used to treat several liver disorders. Silybin inactivated purified, recombinant cytochromes P450 (P450)…”
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5
The endocannabinoid anandamide is a substrate for the human polymorphic cytochrome P450 2D6
Published in The Journal of pharmacology and experimental therapeutics (01-11-2008)“…Members of the cytochrome P450 (P450) family of drug-metabolizing enzymes are present in the human brain, and they may have important roles in the oxidation of…”
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6
Differential Inhibition of Cytochromes P450 3A4 and 3A5 by the Newly Synthesized Coumarin Derivatives 7-Coumarin Propargyl Ether and 7-(4-Trifluoromethyl)coumarin Propargyl Ether
Published in Drug metabolism and disposition (01-11-2008)“…The abilities of 7-coumarin propargyl ether (CPE) and 7-(4-trifluoromethyl)coumarin propargyl ether (TFCPE) to act as mechanism-based inactivators of P450 3A4…”
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THE NATURALLY OCCURRING CYTOCHROME P450 (P450) 2B6 K262R MUTANT OF P450 2B6 EXHIBITS ALTERATIONS IN SUBSTRATE METABOLISM AND INACTIVATION
Published in Drug metabolism and disposition (01-06-2005)“…The polymorphic human cytochrome P450 (P450) 2B6 is primarily responsible for the metabolism of several clinically relevant drugs including bupropion,…”
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8
Effect of tamoxifen on the enzymatic activity of human cytochrome CYP2B6
Published in The Journal of pharmacology and experimental therapeutics (01-06-2002)“…Tamoxifen is primarily used in the treatment of breast cancer. It has been approved as a chemopreventive agent for individuals at high risk for this disease…”
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9
Identification of amino acid residues involved in the inactivation of cytochrome P450 2B1 by two acetylenic compounds: the role of three residues in nonsubstrate recognition Sites
Published in The Journal of pharmacology and experimental therapeutics (01-10-2004)“…The homologous rat cytochrome P450s 2B1 and 2B2 differ by 13 amino acids. A chimeric construct of P450 2B1/2B2 was used in conjunction with several…”
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10
Synthesis of Substituted Phenyl Diaziridines and Characterization as Mechanism-Based Inactivators of Human Cytochrome P450 2B6
Published in Drug metabolism and disposition (01-11-2006)“…The metabolism of arylhydrazines by cytochromes P450 (P450s) has previously been shown to yield aryl-iron complexes that inhibit P450 enzymes as a result of…”
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11
Structure-Activity Relationship and Elucidation of the Determinant Factor(s) Responsible for the Mechanism-Based Inactivation of Cytochrome P450 2B6 by Substituted Phenyl Diaziridines
Published in Drug metabolism and disposition (01-12-2006)“…It has been demonstrated previously that several 3-trifluoromethyl-3-(4-alkoxyphenyl)diaziridines inhibit the 7-ethoxy-4-(trifluoroethyl)coumarin (7-EFC) O…”
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12
Bioactivation of the cancer chemopreventive agent tamoxifen to quinone methides by cytochrome P4502B6 and identification of the modified residue on the apoprotein
Published in Drug metabolism and disposition (01-12-2012)“…The nonsteroidal antiestrogen tamoxifen was introduced as a treatment for breast cancer 3 decades ago. It has also been approved as a chemopreventive agent and…”
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13
Anandamide Oxidation by Wild-Type and Polymorphically Expressed CYP2B6 and CYP2D6
Published in Drug metabolism and disposition (01-05-2011)“…Anandamide is an arachidonic acid-derived endogenous cannabinoid that regulates normal physiological functions and pathophysiological responses within the…”
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14
Quantitation of UGT1A1 in human liver microsomes using stable isotope-labelled peptides and mass spectrometry based proteomic approaches
Published in Xenobiotica (01-04-2013)“…1. UDP-glucuronosyltransferases (UGTs) are a group of drug-metabolizing enzymes that catalyse the conjugation of endogeonous compounds and xenobiotics to yield…”
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15
Metabolism of Cyclophosphamide by the Human Cytochrome P450 2B6 Polymorphic Variants
Published in The FASEB journal (01-04-2012)“…Abstract only The alkylating agent, cyclophosphamide, is a common therapeutic agent used in the treatment of many cancers. Importantly, the efficacy and…”
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16
Anandamide Oxidation by Wild-Type and Polymorphically Expressed CYP2B6 and CYP2D6S
Published in Drug metabolism and disposition (01-05-2011)“…Anandamide is an arachidonic acid-derived endogenous cannabinoid that regulates normal physiological functions and pathophysiological responses within the…”
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17
The endocannabinoid anandamide is a substrate of cytochrome P450 2D6
Published in The FASEB journal (01-03-2008)“…Abstract only The endocannabinoid anandamide, an arachidonic acid derivative, activates the cannabinoid receptors CB1 and CB2. These receptors and the enzymes…”
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18
Modification of Serine 360 by a Reactive Intermediate of 17-a-Ethynylestradiol Results in Mechanism-Based Inactivation of Cytochrome P450s 2B1 and 2B6
Published in Chemical research in toxicology (01-10-2008)“…17-*a-Ethynylestradiol (17EE) is a mechanism-based inactivator of P450 2B1 and P450 2B6 in the reconstituted monooxygenase system. The loss in enzymatic…”
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Modification of Serine 360 by a Reactive Intermediate of 17-α-Ethynylestradiol Results in Mechanism-Based Inactivation of Cytochrome P450s 2B1 and 2B6
Published in Chemical research in toxicology (20-10-2008)“…17-α-Ethynylestradiol (17EE) is a mechanism-based inactivator of P450 2B1 and P450 2B6 in the reconstituted monooxygenase system. The loss in enzymatic…”
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20
Modification of Serine 360 by a Reactive Intermediate of 17-α-Ethynylestradiol Leads to Mechanism-based Inactivation of Cytochrome P450s 2B1 and 2B6
Published in Chemical research in toxicology (26-08-2008)“…17-α-Ethynylestradiole (17EE) is a mechanism-based inactivator of CYP 2B1 and CYP 2B6 in the reconstituted system. The loss in enzymatic activity was due to…”
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