Cytochrome P450 2A6

UniProt P11509 Organism Homo sapiens Gene CYP2A3, CYP2A6 EC 1.14.14.-

Also known as: CYP2A3, CYP2A6

Function

Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide, ifosphamide and tegafur. Competent in the metabolic activation of aflatoxin B1. Constitutes the major nicotine C-oxidase. Acts as a 1,4-cineole 2-exo-monooxygenase. Possesses low phenacetin O-deethylation activity.

Classification

Family (Pfam): PF00067 p450
InterPro: Cyt_P450, Cyt_P450_CS, Cyt_P450_E_grp-I, Cyt_P450_E_grp-I_CYP2A-like, Cyt_P450_sf, Cytochrome_P450_fam2
Functional cluster: Cytochrome P450 & Heme Enzymes

Experimental structures · PDB · 11

1Z10 X-ray 1.90A
1Z11 X-ray 2.05A
2FDU X-ray 1.85A
2FDV X-ray 1.65A
2FDW X-ray 2.05A
2FDY X-ray 1.95A
3EBS X-ray 2.15A
3T3Q X-ray 2.10A
3T3R X-ray 2.40A
4EJJ X-ray 2.30A
4RUI X-ray 2.61A

A predicted model is available from AlphaFold.

Gene Ontology · 15

Disease associations

OMIM:621426 RAW:OMIM_621426

Neighborhood · nearest proteins

Nearest neighbours of Cytochrome P450 2A6: 3 by sequence/function similarity (left); 3 co-cited in the literature (right).

Related proteins · sequence + function similarity

Co-cited proteins · studied together in the literature

Cytochrome P450 2A7 1 shared papers
Cytochrome P450 2A13 2 shared papers
Cytochrome P450 2B6 3 shared papers
Cytochrome P450 3A4 2 shared papers
S-formylglutathione hydrolase 1 shared papers
Arylacetamide deacetylase 1 shared papers
Cytochrome P450 7A1 1 shared papers
Cocaine esterase 1 shared papers
Thromboxane-A synthase 1 shared papers
Cytochrome P450 2E1 1 shared papers
Granzyme B 1 shared papers
Cytochrome P450 2D6 1 shared papers

Literature · 24 cited papers

An enzyme assisted RP-RPLC approach for in-depth analysis of human liver phosphoproteome. J. Proteomics · 2014
Key residues controlling phenacetin metabolism by human cytochrome P450 2A enzymes. Drug Metab. Dispos. · 2008
Novel and established CYP2A6 alleles impair in vivo nicotine metabolism in a population of Black African descent. Hum. Mutat. · 2008
A novel CYP2A6 allele, CYP2A6*23, impairs enzyme function in vitro and in vivo and decreases smoking in a population of Black-African descent. Pharmacogenet. Genomics · 2008
Synthetic inhibitors of cytochrome P-450 2A6: inhibitory activity, difference spectra, mechanism of inhibition, and protein cocrystallization. J. Med. Chem. · 2006
Structures of human microsomal cytochrome P450 2A6 complexed with coumarin and methoxsalen. Nat. Struct. Mol. Biol. · 2005
Twenty one novel single nucleotide polymorphisms (SNPs) of the CYP2A6 gene in Japanese and Caucasians. Drug Metab. Pharmacokinet. · 2002
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
The DNA sequence and biology of human chromosome 19. Nature · 2004
Complete sequencing and characterization of 21,243 full-length human cDNAs. Nat. Genet. · 2004
Catalog of 680 variations among eight cytochrome p450 (CYP) genes, nine esterase genes, and two other genes in the Japanese population. J. Hum. Genet. · 2003
… and 12 more in the literature graph

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