Search Results - "Rushmore, Thomas H."
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Systematic genetic and genomic analysis of cytochrome P450 enzyme activities in human liver
Published in Genome research (01-08-2010)“…Liver cytochrome P450s (P450s) play critical roles in drug metabolism, toxicology, and metabolic processes. Despite rapid progress in the understanding of…”
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Pharmacogenomics, regulation and signaling pathways of phase I and II drug metabolizing enzymes
Published in Current drug metabolism (01-10-2002)“…Drug or xenobiotics metabolizing enzymes (DMEs or XMEs) play central roles in the biotransformation, metabolism and/or detoxification of xenobiotics or foreign…”
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Substrate Inhibition Kinetics for Cytochrome P450-Catalyzed Reactions
Published in Drug metabolism and disposition (01-04-2001)“…Most cytochrome P450 (P450 or CYP)-catalyzed reactions are adequately described by classical Michaelis-Menten kinetic parameters (e.g., K m and V max ), which…”
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4
Activators of the rat pregnane X receptor differentially modulate hepatic and intestinal gene expression
Published in Molecular pharmacology (01-05-2004)“…Ligand-mediated activation of the pregnane X receptor (PXR, NR1I2) is postulated to affect both hepatic and intestinal gene expression, because of the presence…”
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STEREO- AND REGIOSELECTIVITY ACCOUNT FOR THE DIVERSITY OF DEHYDROEPIANDROSTERONE (DHEA) METABOLITES PRODUCED BY LIVER MICROSOMAL CYTOCHROMES P450
Published in Drug metabolism and disposition (01-03-2004)“…The purpose of this study was to quantify the oxidative metabolism of dehydroepiandrosterone (3β-hydroxy-androst-5-ene-17-one; DHEA) by liver microsomal…”
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Mapping the genetic architecture of gene expression in human liver
Published in PLoS biology (01-05-2008)“…Genetic variants that are associated with common human diseases do not lead directly to disease, but instead act on intermediate, molecular phenotypes that in…”
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Toward a systems approach to the human cytochrome P450 ensemble: interactions between CYP2D6 and CYP2E1 and their functional consequences
Published in Biochemical journal (15-10-2017)“…Functional cross-talk among human drug-metabolizing cytochrome P450 through their association is a topic of emerging importance. Here, we studied the…”
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Selective inhibition of dog hepatic CYP2B11 and CYP3A12
Published in The Journal of pharmacology and experimental therapeutics (01-05-2005)“…In the present study, N-(alpha-methylbenzyl-)-1-aminobenzotriazole (MBA) and ketoconazole (KET) were identified as the inhibitors with selectivity toward dog…”
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Testosterone, 7-Benzyloxyquinoline, and 7-Benzyloxy-4-trifluoromethyl-coumarin Bind to Different Domains within the Active Site of Cytochrome P450 3A4
Published in Drug metabolism and disposition (01-11-2001)“…Testosterone, 7-benzyloxyquinoline, and 7-benzyloxy-4-trifluoromethyl-coumarin, marker substrates for cytochrome P450 3A4 are commonly used within the…”
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Electrospray Ionization Mass Spectrometric Analysis of Intact Cytochrome P450: Identification of Tienilic Acid Adducts to P450 2C9
Published in Biochemistry (Easton) (23-02-1999)“…A general scheme for the purification of baculovirus-expressed cytochrome P450s (P450s) from the crude insect cell pastes has been designed which renders the…”
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Halothane-Induced Liver Injury in Outbred Guinea Pigs: Role of Trifluoroacetylated Protein Adducts in Animal Susceptibility
Published in Chemical research in toxicology (01-04-2001)“…Halothane causes a mild form of liver injury in guinea pigs that appears to model the hepatotoxicity seen in approximately 20% of patients treated with this…”
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SUBSTRATE SPECIFICITY AND KINETIC PROPERTIES OF SEVEN HETEROLOGOUSLY EXPRESSED DOG CYTOCHROMES P450
Published in Drug metabolism and disposition (01-09-2003)“…Seven dog cytochromes P450 (P450s) were heterologously expressed in baculovirus-Sf21 insect cells. Of all enzymes examined, CYP1A1 exhibited high…”
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Inhibition Kinetics of Monoclonal Antibodies against Cytochromes P450
Published in Drug metabolism and disposition (01-06-2002)“…Monoclonal antibodies (MAbs) inhibitory to individual cytochromes P450 (P450s) are of tremendous utility in identification of P450s responsible for the…”
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Effect of quinidine on the 10-hydroxylation of R-warfarin: species differences and clearance projection
Published in The Journal of pharmacology and experimental therapeutics (01-10-2004)“…Stimulation by quinidine of warfarin metabolism in vitro was first demonstrated with liver microsomal preparations. We report herein that this drug interaction…”
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INDUCTION OF CYP1A IN THE BEAGLE DOG BY AN INHIBITOR OF KINASE INSERT DOMAIN-CONTAINING RECEPTOR: DIFFERENTIAL EFFECTS IN VITRO AND IN VIVO ON MRNA AND FUNCTIONAL ACTIVITY
Published in Drug metabolism and disposition (01-07-2005)“…Compound I [3-[5-(4-methanesulfonyl-piperazin-1-ylmethyl)-1 H -indol-2-yl]-1 H -quinolin-2-one] is a potent inhibitor of human kinase insert domain-containing…”
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Cytotoxicity of 3-(3,5-dichlorophenyl)-2,4-thiazolidinedione (DCPT) and analogues in wild type and CYP3A4 stably transfected HepG2 cells
Published in Toxicology in vitro (01-12-2011)“…[Display omitted] ► 3-(3,5-Dichlorophenyl)-2,4-thiazolidinedione (DCPT) was cytotoxic in HepG2 cells. ► Cytotoxicity was enhanced in HepG2 cells transfected…”
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Cytochrome P450 pharmacogenetics in drug development: in vitro studies and clinical consequences
Published in Current drug metabolism (01-06-2002)“…Members of the human cytochrome P450 (CYP) superfamily play a role in the metabolism of many drugs and several of them, CYP2D6, CYP2C9 and CYP2C19, have been…”
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Major role of human liver microsomal cytochrome P450 2C9 (CYP2C9) in the oxidative metabolism of celecoxib, a novel cyclooxygenase-II inhibitor
Published in The Journal of pharmacology and experimental therapeutics (01-05-2000)“…In vitro studies were conducted to identify the cytochromes P450 (CYP) involved in the oxidative metabolism of celecoxib. The hydroxylation of celecoxib…”
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A Kinetic Model for the Metabolic Interaction of Two Substrates at the Active Site of Cytochrome P450 3A4
Published in The Journal of biological chemistry (19-01-2001)“…In many cases, CYP3A4 exhibits unusual kinetic characteristics that result from the metabolism of multiple substrates that coexist at the active site. In the…”
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Sigmoidal kinetic model for two co-operative substrate-binding sites in a cytochrome P450 3A4 active site: an example of the metabolism of diazepam and its derivatives
Published in Biochemical journal (15-06-1999)“…Cytochrome P450 3A4 (CYP3A4) plays a prominent role in the metabolism of a vast array of drugs and xenobiotics and exhibits broad substrate specificities. Most…”
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