Results 21 to 30 of about 56,913 (295)

CYP3A4 intronic SNP rs35599367 (CYP3A4*22) alters RNA splicing [PDF]

open access: yesPharmacogenetics and Genomics, 2016
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]

open access: yesBioorganic & Medicinal Chemistry, 2008
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]

open access: yes, 2012
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]

open access: yesBioorganic & Medicinal Chemistry Letters, 2012
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]

open access: yesAdvanced Pharmaceutical Bulletin, 2020
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

Enhanced oral bioavailability of nisoldipine-piperine-loaded poly-lactic-co-glycolic acid nanoparticles

open access: yesNanotechnology Reviews, 2017
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

open access: yesPharmaceutical Biology, 2018
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

Development of a highly reproducible system to evaluate inhibition of cytochrome P450 3A4 activity by natural medicines

open access: yesJournal of Pharmacy & Pharmaceutical Sciences, 2015
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 Vitro Model for a Drug Assessment of Cytochrome P450 Family 3 Subfamily A Member 4 Substrates Using Human Induced Pluripotent Stem Cells and Genome Editing Technology

open access: yesHepatology Communications, 2021
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]

open access: yesBritish Journal of Clinical Pharmacology, 2008
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

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