Search Results - "VAZ, Alfin D. N"
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Deuterium isotope effects in drug pharmacokinetics II: Substrate-dependence of the reaction mechanism influences outcome for cytochrome P450 cleared drugs
Published in PloS one (14-11-2018)“…Two chemotypes were examined in vitro with CYPs 3A4 and 2C19 by molecular docking, metabolic profiles, and intrinsic clearance deuterium isotope effects with…”
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2
A tag-free collisionally induced fragmentation approach to detect drug-adducted proteins by mass spectrometry
Published in Rapid communications in mass spectrometry (30-11-2015)“…Rationale The covalent modification of proteins by toxicants, new chemical entities or drug molecules, either by metabolic activation or the presence of…”
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3
Molecular etiology of atherogenesis--in vitro induction of lipidosis in macrophages with a new LDL model
Published in PloS one (13-04-2012)“…Atherosclerosis starts by lipid accumulation in the arterial intima and progresses into a chronic vascular inflammatory disease. A major atherogenic process is…”
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IN VITRO DRUG INTERACTIONS OF CYTOCHROME P450: AN EVALUATION OF FLUOROGENIC TO CONVENTIONAL SUBSTRATES
Published in Drug metabolism and disposition (01-08-2003)“…Clinically observed drug interactions with cytochrome P450 (P450) enzymes have increased the need to assess drug interactions of new chemical entities early in…”
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5
A Simple Litmus Test for Aldehyde Oxidase Metabolism of Heteroarenes
Published in Journal of medicinal chemistry (27-02-2014)“…The bioavailability of aromatic azaheterocyclic drugs can be affected by the activity of aldehyde oxidase (AO). Susceptibility to AO metabolism is difficult to…”
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6
BIOACTIVATION OF THE NONTRICYCLIC ANTIDEPRESSANT NEFAZODONE TO A REACTIVE QUINONE-IMINE SPECIES IN HUMAN LIVER MICROSOMES AND RECOMBINANT CYTOCHROME P450 3A4
Published in Drug metabolism and disposition (01-02-2005)“…The therapeutic benefits of the antidepressant nefazodone have been hampered by several cases of acute hepatotoxicity/liver failure. Although the mechanism of…”
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7
Epoxidation of Olefins by Cytochrome P450: Evidence from Site-Specific Mutagenesis for Hydroperoxo-Iron as an Electrophilic Oxidant
Published in Proceedings of the National Academy of Sciences - PNAS (31-03-1998)“…P450 cytochromes (P450) catalyze many types of oxidative reactions, including the conversion of olefinic substrates to epoxides by oxygen insertion. In some…”
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Deuterium isotope effects on drug pharmacokinetics. I. System-dependent effects of specific deuteration with aldehyde oxidase cleared drugs
Published in Drug metabolism and disposition (01-03-2012)“…The pharmacokinetic properties of drugs may be altered by kinetic deuterium isotope effects. With specifically deuterated model substrates and drugs…”
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9
On the Mechanism of Action of Cytochrome P450: Evaluation of Hydrogen Abstraction in Oxygen-Dependent Alcohol Oxidation
Published in Biochemistry (Easton) (01-05-1994)“…The mechanisms of oxidation of primary and secondary benzylic alcohols to the corresponding carbonyl compounds by purified rabbit liver cytochrome P450 forms…”
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10
Discrete Species of Activated Oxygen Yield Different Cytochrome P450 Heme Adducts from Aldehydes
Published in Biochemistry (Easton) (10-08-1999)“…Aldehydes are known to inactivate cytochrome P450 in the reconstituted enzyme system containing NADPH and NADPH−cytochrome P450 reductase under aerobic…”
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11
A rapid and specific derivatization procedure to identify acyl-glucuronides by mass spectrometry
Published in Rapid communications in mass spectrometry (30-07-2010)“…A simple procedure is described to identify acyl‐glucuronides by coupled liquid chromatography/mass spectrometry after derivatization to a hydroxamic acid with…”
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12
Cytochrome P450-Catalyzed Hydroxylation of Mechanistic Probes that Distinguish between Radicals and Cations. Evidence for Cationic but Not for Radical Intermediates
Published in Journal of the American Chemical Society (29-03-2000)“…Oxidation of the mechanistic probes trans,trans-2-methoxy-3-phenylmethylcyclopropane and methylcubane by six cytochrome P450 isozymes has been studied. The…”
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13
In vitro metabolism studies on the isoxazole ring scission in the anti-inflammatory agent leflunomide to its active α-cyanoenol metabolite A771726: Mechanistic similarities with the cytochrome P450-catalyzed dehydration of aldoximes
Published in Drug metabolism and disposition (01-10-2003)Get full text
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14
Discovery of Azetidinyl Ketolides for the Treatment of Susceptible and Multidrug Resistant Community-Acquired Respiratory Tract Infections
Published in Journal of medicinal chemistry (10-12-2009)“…Respiratory tract bacterial strains are becoming increasingly resistant to currently marketed macrolide antibiotics. The current alternative telithromycin (1)…”
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15
Olefin formation in the oxidative deformylation of aldehydes by cytochrome P-450. Mechanistic implications for catalysis by oxygen-derived peroxide
Published in Journal of the American Chemical Society (01-07-1991)“…We describe the cytochrome P-450 mediated oxidative deformylation of a xenobiotic aldehyde with introduction of unsaturation into the residual carbon framework…”
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16
Aromatization of a Bicyclic Steroid Analog, 3-Oxodecalin-4-ene-10-carboxaldehyde, by Liver Microsomal Cytochrome P450 2B4
Published in Biochemistry (Easton) (01-11-1994)“…Several purified isoforms of microsomal cytochrome P450 were previously shown in this laboratory to catalyze the oxidative deformylation of a variety of alpha-…”
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17
The use of 18O-exchange and base-catalyzed N-dealkylation with liquid chromatography/tandem mass spectrometry to identify carbinolamide metabolites
Published in Rapid communications in mass spectrometry (30-07-2010)“…Oxidation of N‐alkyl‐substituted amides is a common transformation observed in metabolism studies of drugs and other chemicals. Metabolism at the alpha carbon…”
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18
Peroxo-Iron and Oxenoid-Iron Species as Alternative Oxygenating Agents in Cytochrome P450-Catalyzed Reactions: Switching by Threonine-302 to Alanine Mutagenesis of Cytochrome P450 2B4
Published in Proceedings of the National Academy of Sciences - PNAS (14-05-1996)“…Among biological catalysts, cytochrome P450 is unmatched in its multiplicity of isoforms, inducers, substrates, and types of chemical reactions catalyzed. In…”
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19
Two Distinct Electrophilic Oxidants Effect Hydroxyl- ation in Cytochrome P-450-Catalyzed Reactions
Published in Journal of the American Chemical Society (23-09-1998)Get full text
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20
Old yellow enzyme: Aromatization of cyclic enones and the mechanism of a novel dismutation reaction
Published in Biochemistry (Easton) (04-04-1995)“…The origin of charge transfer bands that develop on reaction of Old Yellow Enzyme with alpha,beta-unsaturated cyclic ketones such as 3-oxodecalin-4-ene (ODE,…”
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