CYP3A5

Cytochrome P450 3A5 • UniProt accession P20815

A cytochrome P450 monooxygenase involved in the metabolism of steroid hormones and vitamins (PubMed:10681376, PubMed:11093772, PubMed:12865317, PubMed:2732228). Mechanistically, uses molecular oxygen inserting one oxygen atom into a substrate, and reducing the second into a water molecule, with two electrons provided by NADPH via cytochrome P450 reductase (NADPH--hemoprotein reductase). Catalyzes the hydroxylation of carbon-hydrogen bonds (PubMed:10681376, PubMed:11093772, PubMed:12865317, PubMed:2732228).

Exhibits high catalytic activity for the formation of catechol estrogens from 17beta-estradiol (E2) and estrone (E1), namely 2-hydroxy E1 and E2 (PubMed:12865317). Catalyzes 6beta-hydroxylation of the steroid hormones testosterone, progesterone, and androstenedione (PubMed:2732228). Catalyzes the oxidative conversion of all-trans-retinol to all-trans-retinal, a rate-limiting step for the biosynthesis of all-trans-retinoic acid (atRA) (PubMed:10681376).

Further metabolizes all trans-retinoic acid (atRA) to 4-hydroxyretinoate and may play a role in hepatic atRA clearance (PubMed:11093772). Also involved in the oxidative metabolism of xenobiotics, including calcium channel blocking drug nifedipine and immunosuppressive drug cyclosporine (PubMed:2732228)

Source: UniProt
Endoplasmic reticulum membrane — Peripheral membrane protein, Microsome membrane — Peripheral membrane protein
Source: UniProt
  • Xenobiotics
  • Aflatoxin activation and detoxification
Source: Reactome via UniProt

Mutations

No mutation information available.

Synthetic Lethal Network

Genes with an experimentally identified or computationally predicted synthetic-lethal relationship to CYP3A5, aggregated across our SSL data sources. Click any partner node to view that gene’s page.

Nodes and edges are coloured by the SSL data source. Partners appearing in more than one source are shown in grey.

BioGRID SLOrth SynLethDB MexDrugs Multi-source
Sources: BioGRID, SLOrth, SynLethDB, MexDrugs

Clinical Trials

Total Trials Found: 39

NCT ID Condition Brief Title Phase Status
NCT02377791 Kidney Transplant Impact of CYP3A5 Gene Polymorphisms on Tacrolimus Concentrations and Outcomes in Thai Transplant Recipients N/A UNKNOWN
NCT00552201 Kidney Transplantation TACrolimus in Renal Transplantation: Individualization by Pharmacogenetic PHASE4 COMPLETED
NCT02077556 Drug Interaction Potentiation Effect of Everolimus on the Pharmacokinetics of Tacrolimus in Renal Transplant Patients PHASE4 COMPLETED
NCT00411944 Renal Transplantation Long-Term Pharmacokinetics of Tacrolimus in Renal Recipients N/A COMPLETED
NCT06044558 Kidney Transplant Patients Effect of Azole/Echinocandin Use on Tacrolimus Pharmacokinetics N/A COMPLETED
NCT00902460 Healthy Volunteer CP-690,550 and Midazolam Drug-Drug Interaction Study PHASE1 COMPLETED
NCT00139035 Chronic Renal Failure Effects of Cyclosporine A on Pancreatic Insulin Secretion PHASE4 COMPLETED
NCT02311010 Kidney Diseases Practical Use of Advagraf de Novo After Kidney Transplantation According to Recipient Genetic Polymorphism PHASE4 UNKNOWN
NCT00767598 Pharmacokinetics of Three PDE5Is, Healthy Subjects, Genetic Polymorphic CYP3A5 The Effect of CYP3A Genetic Polymorphism on the Pharmacokinetics of Phosphodiesterase type5 Inhibitors in Male Subjects PHASE1 COMPLETED
NCT02625207 Healthy Subjects THE EFFECT OF CYP3A5 GENOTYPE ON THE PHARMACOKINETICS OF MARAVIROC PHASE1 COMPLETED