Cytochrome P450 3A5

UniProt P20815 Organism Homo sapiens Gene CYP3A5 EC 1.14.14.1

Also known as: CYP3A5

Function

A cytochrome P450 monooxygenase involved in the metabolism of steroid hormones and vitamins. 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. Exhibits high catalytic activity for the formation of catechol estrogens from 17beta-estradiol (E2) and estrone (E1), namely 2-hydroxy E1 and E2. Catalyzes 6beta-hydroxylation of the steroid hormones testosterone, progesterone, and androstenedione. 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). Further metabolizes all trans-retinoic acid (atRA) to 4-hydroxyretinoate and may play a role in hepatic atRA clearance. Also involved in the oxidative metabolism of xenobiotics, including calcium channel blocking drug nifedipine and immunosuppressive drug cyclosporine.

Classification

Family (Pfam): PF00067 p450
InterPro: Cyt_P450, Cyt_P450_CS, Cyt_P450_E_CYP3A, Cyt_P450_E_grp-II, Cyt_P450_sf, Cytochrome_P450_3A
Functional cluster: Serine/Threonine Protein Kinases

Experimental structures · PDB · 6

5VEU X-ray 2.91A
6MJM X-ray 2.20A
7LAD X-ray 2.65A
7SV2 X-ray 2.46A
8SG5 X-ray 2.80A
9MS2 X-ray 2.25A

A predicted model is available from AlphaFold.

Gene Ontology · 21

Drugs targeting this protein · 2

RITONAVIR inhibitor
COBICISTAT inhibitor

Related proteins · sequence + function similarity

Co-cited proteins · studied together in the literature

Cytochrome P450 3A43 2 shared papers
Cytochrome P450 3A4 7 shared papers
Cytochrome P450 3A7 3 shared papers
Cytochrome P450 2C18 1 shared papers
Cytochrome P450 1A2 3 shared papers
Cytochrome P450 1A1 3 shared papers
Cytochrome P450 2D6 2 shared papers
Cytochrome P450 2C8 2 shared papers
Cytochrome P450 1B1 2 shared papers
Cytochrome P450 2B6 2 shared papers
Cytochrome P450 2C9 2 shared papers
Cytochrome P450 2E1 1 shared papers

Literature · 18 cited papers

An enzyme assisted RP-RPLC approach for in-depth analysis of human liver phosphoproteome. J. Proteomics · 2014
The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. · 2004
Genetic variation in eleven phase I drug metabolism genes in an ethnically diverse population. Pharmacogenomics · 2004
Complete sequencing and characterization of 21,243 full-length human cDNAs. Nat. Genet. · 2004
Genetic findings and functional studies of human CYP3A5 single nucleotide polymorphisms in different ethnic groups. Pharmacogenetics · 2003
Characterization of the oxidative metabolites of 17beta-estradiol and estrone formed by 15 selectively expressed human cytochrome p450 isoforms. Endocrinology · 2003
The DNA sequence of human chromosome 7. Nature · 2003
Human chromosome 7: DNA sequence and biology. Science · 2003
Intergenic mRNA molecules resulting from trans-splicing. J. Biol. Chem. · 2002
Genetic polymorphism of cytochrome P450 3A5 in Chinese. Drug Metab. Dispos. · 2001
Genomic organization of the human CYP3A locus: identification of a new, inducible CYP3A gene. Pharmacogenetics · 2001
Identification of human cytochrome P450s involved in the formation of all-trans-retinoic acid principal metabolites. Mol. Pharmacol. · 2000
… and 6 more in the literature graph

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