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Results: 1 to 10 of 81

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In Vitro Activation of Cytochrome P450 46A1 (CYP46A1) by Efavirenz-Related Compounds.
Mast N, Verwilst P, Wilkey CJ, Guengerich FP, Pikuleva IA
(2020) J Med Chem 63: 6477-6488
MeSH Terms: Alkynes, Allosteric Site, Benzoxazines, Catalytic Domain, Cholesterol, Cholesterol 24-Hydroxylase, Cyclopropanes, Cytochrome P-450 CYP3A Inducers, Humans, Hydroxylation, In Vitro Techniques, Pharmaceutical Preparations, Protein Conformation
Added March 3, 2020
0 Communities
1 Members
0 Resources
13 MeSH Terms
Human cytochrome P450 enzymes bind drugs and other substrates mainly through conformational-selection modes.
Guengerich FP, Wilkey CJ, Phan TTN
(2019) J Biol Chem 294: 10928-10941
MeSH Terms: Catalysis, Cytochrome P-450 CYP2D6, Cytochrome P-450 CYP2E1, Cytochrome P-450 CYP3A, Cytochrome P-450 Enzyme Inhibitors, Cytochrome P-450 Enzyme System, Humans, Kinetics, Lauric Acids, Ligands, Molecular Conformation, Oxidation-Reduction, Palmitic Acid, Protein Binding, Protein Conformation, Spiro Compounds, Substrate Specificity
Added March 3, 2020
0 Communities
1 Members
0 Resources
17 MeSH Terms
Induction of human cytochrome P450 3A enzymes in cultured placental cells by thalidomide and relevance to bioactivation and toxicity.
Murayama N, Kazuki Y, Satoh D, Arata K, Harada T, Shibata N, Guengerich FP, Yamazaki H
(2017) J Toxicol Sci 42: 343-348
MeSH Terms: Cells, Cultured, Cytochrome P-450 CYP3A, Enzyme Induction, Female, Humans, Liver, Oxidation-Reduction, Placenta, Pregnancy, Pregnane X Receptor, RNA, Messenger, Receptors, Steroid, Rifampin, Thalidomide
Added March 14, 2018
0 Communities
1 Members
0 Resources
14 MeSH Terms
7,8-benzoflavone binding to human cytochrome P450 3A4 reveals complex fluorescence quenching, suggesting binding at multiple protein sites.
Marsch GA, Carlson BT, Guengerich FP
(2018) J Biomol Struct Dyn 36: 841-860
MeSH Terms: Benzoflavones, Binding Sites, Cytochrome P-450 CYP3A, Fluorescence, Humans, Kinetics, Ligands, Models, Chemical, Oxidation-Reduction, Protein Binding, Spectrometry, Fluorescence, Substrate Specificity
Added March 14, 2018
0 Communities
1 Members
0 Resources
12 MeSH Terms
Simulation of Human Plasma Concentrations of Thalidomide and Primary 5-Hydroxylated Metabolites Explored with Pharmacokinetic Data in Humanized TK-NOG Mice.
Nishiyama S, Suemizu H, Shibata N, Guengerich FP, Yamazaki H
(2015) Chem Res Toxicol 28: 2088-90
MeSH Terms: Animals, Cytochrome P-450 CYP3A, Glutathione, Hepatocytes, Humans, Hydroxylation, Liver, Mice, Teratogens, Thalidomide
Added March 14, 2018
0 Communities
1 Members
0 Resources
10 MeSH Terms
Dual drug delivery of tamoxifen and quercetin: Regulated metabolism for anticancer treatment with nanosponges.
Lockhart JN, Stevens DM, Beezer DB, Kravitz A, Harth E
(2015) J Control Release 220: 751-7
MeSH Terms: Animals, Antineoplastic Combined Chemotherapy Protocols, Biological Availability, Biotransformation, Breast Neoplasms, Cell Line, Tumor, Cell Survival, Chemistry, Pharmaceutical, Cross-Linking Reagents, Cytochrome P-450 CYP3A, Delayed-Action Preparations, Dose-Response Relationship, Drug, Drug Carriers, Drug Stability, Female, Gastric Juice, Glucuronosyltransferase, Intestinal Secretions, Kinetics, Mice, Nanomedicine, Nanoparticles, Particle Size, Polyesters, Quercetin, Solubility, Tamoxifen
Added February 15, 2016
0 Communities
1 Members
0 Resources
27 MeSH Terms
A Screen of Approved Drugs Identifies the Androgen Receptor Antagonist Flutamide and Its Pharmacologically Active Metabolite 2-Hydroxy-Flutamide as Heterotropic Activators of Cytochrome P450 3A In Vitro and In Vivo.
Blobaum AL, Byers FW, Bridges TM, Locuson CW, Conn PJ, Lindsley CW, Daniels JS
(2015) Drug Metab Dispos 43: 1718-26
MeSH Terms: Androgen Receptor Antagonists, Animals, Cytochrome P-450 CYP3A, Drug Evaluation, Preclinical, Enzyme Activators, Female, Flutamide, Guinea Pigs, Humans, Male, Mice, Microsomes, Liver, Rats, Rats, Sprague-Dawley, Swine, Swine, Miniature
Added February 18, 2016
0 Communities
1 Members
0 Resources
16 MeSH Terms
Role of pharmacogenomics in dialysis and transplantation.
Birdwell K
(2014) Curr Opin Nephrol Hypertens 23: 570-7
MeSH Terms: Calcineurin Inhibitors, Cytochrome P-450 CYP3A, Genotype, Humans, Immunosuppressive Agents, Kidney Transplantation, Pharmacogenetics, Phenotype, Renal Dialysis, Renal Insufficiency, Chronic
Added October 27, 2014
0 Communities
1 Members
0 Resources
10 MeSH Terms
Time- and NADPH-dependent inhibition of cytochrome P450 3A4 by the cyclopentapeptide cilengitide: significance of the guanidine group and accompanying spectral changes.
Bojić M, Barbero L, Dolgos H, Freisleben A, Gallemann D, Riva S, Guengerich FP
(2014) Drug Metab Dispos 42: 1438-46
MeSH Terms: Adult, Cytochrome P-450 CYP3A, Enzyme Inhibitors, Female, Guanidine, Heme, Humans, Male, Microsomes, Liver, NADP, Oxidation-Reduction, Snake Venoms
Added January 20, 2015
0 Communities
1 Members
0 Resources
12 MeSH Terms
Functional CYP2B6 variants and virologic response to an efavirenz-containing regimen in Port-au-Prince, Haiti.
Haas DW, Severe P, Jean Juste MA, Pape JW, Fitzgerald DW
(2014) J Antimicrob Chemother 69: 2187-90
MeSH Terms: ATP Binding Cassette Transporter, Subfamily B, Adult, Alkynes, Anti-HIV Agents, Benzoxazines, Cyclopropanes, Cytochrome P-450 CYP2A6, Cytochrome P-450 CYP2B6, Cytochrome P-450 CYP2B6 Inducers, Cytochrome P-450 CYP3A, Female, Genetic Association Studies, HIV Infections, HIV-1, Haiti, Humans, Male, Middle Aged, Polymorphism, Single Nucleotide, Prospective Studies, RNA, Viral, Reverse Transcriptase Inhibitors, Secondary Metabolism, Treatment Outcome
Added March 13, 2015
0 Communities
1 Members
0 Resources
24 MeSH Terms