CYP3A is an enzyme subfamily in the cytochrome P450 (CYP) superfamily and includes isoforms CYP3A4, CYP3A5, CYP3A7, and CYP3A43. CYP3A enzymes are indiscriminate toward substrates and are unique in that these enzymes metabolize both endogenous compounds and diverse xenobiotics (including drugs); almost the only common characteristic of these compounds is lipophilicity and a relatively large molecular weight. CYP3A enzymes are widely expressed in human organs and tissues, and consequences of these enzymes' activities play a major role both in normal regulation of physiological levels of endogenous compounds and in various pathological conditions. This review addresses these aspects of regulation of CYP3A enzymes under physiological conditions and their involvement in the initiation and progression of diseases.
Download full-text PDF |
Source |
---|---|
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC9687714 | PMC |
http://dx.doi.org/10.3390/biomedicines10112686 | DOI Listing |
Cell Biol Toxicol
January 2025
Department of Environmental Toxicology, Swiss Federal Institute of Aquatic Science and Technology, Eawag, 8600, Dübendorf, Switzerland.
Advancing in vitro systems to address the effects of chemical pollution requires a thorough characterization of their functionalities, such as their repertoire of biotransformation enzymes. Currently, knowledge regarding the presence, activity magnitudes, and inducibility of different biotransformation pathways in vitro is scarce, particularly across organs. We report organ-specific kinetics for phase I and II biotransformation enzymes, under basal and induced conditions, in two in vitro systems using salmonid fish: S9 sub-cellular fractions from brown trout (Salmo trutta) and rainbow trout (Oncorhynchus mykiss) were compared with rainbow trout cell lines.
View Article and Find Full Text PDFJ Nanobiotechnology
January 2025
Key Laboratory of Human Genetics and Environmental Medicine, Xuzhou Medical University, Xuzhou, 221004, China.
Fullerenols, a water-soluble polyhydroxy derivative of fullerene, hold promise in medical and materials science due to their unique properties. However, concerns about their potential embryotoxicity remain. Using a pregnancy mouse model and metabolomics analysis, our findings reveal that fullerenols exposure during pregnancy not only significantly reduced mice placental weight and villi thickness, but also altered the classes and concentrations of metabolites in the mouse placenta.
View Article and Find Full Text PDFSci Rep
January 2025
Institute for Breath Research, University of Innsbruck, Innrain 80/82, Innsbruck, 6020, Austria.
Cytochrome P450 (CYP) 3A4 plays a major role in drug metabolism. Its activity could be determined by non-invasive and cost-effective assays, such as breath analysis, for the personalised monitoring of drug response. For the first time, we identify an isotopically unlabelled CYP3A4 substrate, tolterodine that leads to the formation of a non-toxic volatile metabolite, acetone, which could potentially be applied to monitor CYP3A4 activity in humans.
View Article and Find Full Text PDFSci Rep
January 2025
Bioinformatics Program, School of Biotechnology, Nile University, Giza, Egypt.
Single nucleotide polymorphisms (SNPs) represent the prevailing form of genetic variations observed in the human population. Such variations could alter the encoded enzymes' activities. CYP3A4/5 enzymes are involved in metabolizing drugs, notably antivirals against SARS-CoV-2.
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!