Results 21 to 30 of about 56,913 (295)
CYP3A4 intronic SNP rs35599367 (CYP3A4*22) alters RNA splicing [PDF]
Cytochrome P450 3A4 (CYP3A4) metabolizes 30-50% of clinically used drugs. Large interperson variability in CYP3A4 activity affects response to CYP3A4 substrate drugs. We had demonstrated that an intronic single nucleotide polymorphism rs35599367 (CYP3A4*22, located in intron 6) reduces mRNA/protein expression; however, the underlying mechanism remained
Danxin, Wang, Wolfgang, Sadee
openaire +2 more sources
An epoxidation mechanism of carbamazepine by CYP3A4 [PDF]
Human CYP3A4 catalyzes the 10,11-epoxidation of carbamazepine (CBZ). However, the epoxide is less stable in terms of potential energy than hydroxides of the six-membered aromatic ring. To clarify the reason why CYP3A4 produces such an energetically unfavorable compound, the mechanism of epoxidation of CBZ by CYP3A4 was investigated by theoretical ...
Hata, Masayuki +8 more
openaire +2 more sources
Enantioselective capillary electrophoresis : fundamental aspects and application to the "in vitro" assessment of CYP3A4 mediated ketamine N-demethylation [PDF]
A large number of pharmaceutical substances are administered as racemates, consisting of two enantiomers with typically different pharmacodynamic and pharmacokinetic profiles.
Kwan, Hiu Ying
core +1 more source
Imidazopyridines as selective CYP3A4 inhibitors [PDF]
Cytochrome P450s are the major family of enzymes responsible for the oxidative metabolism of pharmaceuticals and xenobiotics. CYP3A4 and CYP3A5 have been shown to have overlapping substrate and inhibitor profiles and their inhibition has been demonstrated to be involved in numerous pharmacokinetic drug-drug interactions. Here we report the first highly
Xinyi, Song +6 more
openaire +2 more sources
Lipid Drug Carriers for Cancer Therapeutics: An Insight into Lymphatic Targeting, P-gp, CYP3A4 Modulation and Bioavailability Enhancement [PDF]
In the treatment of cancer, chemotherapy plays an important role though the efficacy of anti-cancer drug administered orally is limited, due to their poor solubility in physiological medium, inability to cross biological membrane, high Para-glycoprotein (
Shashank Chaturvedi +2 more
doaj +1 more source
Piperine helps in the improvement of bioavailability through pharmacokinetic interaction by modulating metabolism when administered with other drugs. Nisoldipine is a substrate for cytochrome P4503A4 enzymes.
Rathee Permender +2 more
doaj +1 more source
In vitro inhibitory effects of Friedelin on human liver cytochrome P450 enzymes
Context: Friedelin is a triterpenoid with several biological activities. However, the affects of Friedelin on the activity of human liver cytochrome P450 (CYP) enzymes remains unclear.
Jinlan Wei +2 more
doaj +1 more source
PURPOSE: In recent years, a number of natural medicines have been reported to have inductive or inhibitive effects on the activity of drug metabolizing enzymes, upon co-administration with prescribed medicines.
Yu Sato +4 more
doaj +1 more source
In drug development, a system for predicting drug metabolism and drug‐induced toxicity is necessary to ensure drug safety. Cytochrome P450 family 3 subfamily A member 4 (CYP3A4) is an important drug‐metabolizing enzyme expressed in the liver and small ...
Sayaka Deguchi +8 more
doaj +1 more source
Effects of CYP3A4 inducers with and without CYP3A4 inhibitors on the pharmacokinetics of maraviroc in healthy volunteers [PDF]
AIMSTo assess the potential of known CYP3A4 inducers, with and without CYP3A4 inhibitors, to alter the pharmacokinetic profile of maraviroc.METHODSTwo separate, open, randomized, placebo‐controlled studies were conducted in healthy subjects. Study 1 was a 28‐day parallel‐group study with three treatment groups of 12 subjects each.
Samantha, Abel +4 more
openaire +2 more sources

