Results 281 to 290 of about 61,480 (319)

Discovery and Characterization of Potent Dual P-Glycoprotein and CYP3A4 Inhibitors: Design, Synthesis, Cryo-EM Analysis, and Biological Evaluations.

Journal of Medicinal Chemistry, 2021
Targeted concurrent inhibition of intestinal drug efflux transporter P-glycoprotein (P-gp) and drug metabolizing enzyme cytochrome P450 3A4 (CYP3A4) is a promising approach to improve oral bioavailability of their common substrates such as docetaxel ...
S. Urgaonkar, K. Nosol, A. Said, Nader N Nasief, Yahao Bu, K. Locher, J. Lau, M. Smolinski   +7 more
semanticscholar   +1 more source

Carbon Monoxide Inhibits Cytochrome P450 Enzymes CYP3A4/2C8 in Human Breast Cancer Cells, Increasing Sensitivity to Paclitaxel.

Journal of Medicinal Chemistry, 2021
Paclitaxel (PTX) is a first-line treatment in breast cancer, though resistance develops quickly and frequently. Cytochrome P450 enzymes CYP3A4 and CYP2C8, which metabolically inactivate PTX in hepatic tissue, are overexpressed in malignant breast tissues.
Brian Kawahara, K. Faull, C. Janzen, P. Mascharak   +3 more
semanticscholar   +1 more source

Functional Gene Variants of CYP3A4

Clinical Pharmacology & Therapeutics, 2014
Cytochrome P450 3A4 (CYP3A4) is involved in the metabolism of more drugs in clinical use than any other foreign compound-metabolizing enzyme in humans. Recently, increasing evidence has been found showing that variants in the CYP3A4 gene have functional significance and--in rare cases--lead to loss of activity, implying tremendous consequences for ...
A. Werk, I. Cascorbi
semanticscholar   +3 more sources

Anion-Dependent Stimulation of CYP3A4 Monooxygenase. [PDF]

Biochemistry, 2015
We co-crystallized human cytochrome P450 3A4 (CYP3A4) with progesterone (PRG) under two different conditions, but the resulting complexes contained only one PRG molecule bound to the previously identified peripheral site. A novel feature in one of our structures is a citrate ion, originating from the crystallization solution.
I. Sevrioukova, T. Poulos
semanticscholar   +4 more sources

Pioglitazone: Effect on CYP3A4 Activity

The Journal of Clinical Pharmacology, 2002
Clinical studies demonstrate CYP3A4 enzyme induction with troglitazone, a thiazolidinedione derivative structurally related to pioglitazone. The objective of this prospective, open‐label study conducted in healthy volunteers was to evaluate the influence of multiple‐dose pioglitazone therapy on the urinary excretion ratio of 6‐β‐hydroxycortisol to ...
Sandra N, Nowak, David J, Edwards, Anthony, Clarke, Gail D, Anderson, Linda A, Jaber   +4 more
openaire   +2 more sources

CYP3A4*16 and CYP3A4*18 Alleles Found in East Asians Exhibit Differential Catalytic Activities for Seven CYP3A4 Substrate Drugs

Drug Metabolism and Disposition, 2010
CYP3A4, the major form of cytochrome P450 (P450) expressed in the adult human liver, is involved in the metabolism of approximately 50% of commonly prescribed drugs. Several genetic polymorphisms in CYP3A4 are known to affect its catalytic activity and to contribute in part to interindividual differences in the pharmacokinetics and pharmacodynamics of ...
Keiko, Maekawa, Noriko, Harakawa, Takuya, Yoshimura, Su-Ryang, Kim, Yoshiyuki, Fujimura, Fumika, Aohara, Kimie, Sai, Noriko, Katori, Masahiro, Tohkin, Mikihiko, Naito, Ryuichi, Hasegawa, Haruhiro, Okuda, Jun-ichi, Sawada, Takuro, Niwa, Yoshiro, Saito   +14 more
openaire   +2 more sources

CYP3A4*22: Promising Newly IdentifiedCYP3A4Variant Allele for Personalizing Pharmacotherapy

Pharmacogenomics, 2012
Many studies have attempted to explain the interindividual variability observed in drug metabolism by assessing the impact of SNPs in genes implicated in drug absorption, distribution, metabolism and excretion pathways. Particular attention has been paid to the CYP450s.
Elens, Laure, Gelder, Teun, Hesselink, Dennis, Haufroid, V, van Schaik, Ron   +4 more
openaire   +3 more sources

CYP3A4 and CYP3A5: the crucial roles in clinical drug metabolism and the significant implications of genetic polymorphisms

PeerJ
CYP3A, a key member of the cytochrome P450 (CYP450) superfamily, is integral to drug metabolism, processing a substantial portion of medications. Their role in drug metabolism is particularly prominent, as CYP3A4 and CYP3A5 metabolize approximately 30–50%
Yuqing Zhang, Ziying Wang, Yuchao Wang, Weikai Jin, Zhe-yan Zhang, Lehao Jin, Jian-chang Qian, Long Zheng   +7 more
semanticscholar   +1 more source

Drug-drug interaction (DDI) assessments of ruxolitinib, a dual substrate of CYP3A4 and CYP2C9, using a verified physiologically based pharmacokinetic (PBPK) model to support regulatory submissions

Drug Metabolism and Personalized Therapy, 2019
Ruxolitinib is mainly metabolized by cytochrome P450 (CYP) enzymes CYP3A4 and CYP2C9 followed by minor contributions of other hepatic CYP enzymes in vitro.
K. Umehara, F. Huth, Yi Jin, Hilmar Schiller, V. Aslanis, T. Heimbach, Handan He   +6 more
semanticscholar   +1 more source

CYP3A4 variant alleles in white individuals with low CYP3A4 enzyme activity

Clinical Pharmacology & Therapeutics, 2002
ObjectiveOur objective was to evaluate the presence of CYP3A4 gene variants in white individualswith low CYP3A4 enzyme activity.MethodsPersons with extremely low enzyme activity, either in vitro or in vivo, were selected in a panel of 97 healthy subjects. Genetic analyses for CYP3A4 variant alleles present in white subjects, including CYP3A4*1B, CYP3A4*
Elena, García-Martín, Carmen, Martínez, Rosa M, Pizarro, Francisco J, García-Gamito, Harriet, Gullsten, Hannu, Raunio, José A G, Agúndez   +6 more
openaire   +2 more sources