Tchem CYP2A6 Cytochrome P450 2A6

Protein Summary

Description

Exhibits a high coumarin 7-hydroxylase activity. Can act in the hydroxylation of the anti-cancer drugs cyclophosphamide and ifosphamide. 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. This gene, CYP2A6, encodes a member of the cytochrome P450 superfamily of enzymes. The cytochrome P450 proteins are monooxygenases which catalyze many reactions involved in drug metabolism and synthesis of cholesterol, steroids and other lipids. This protein localizes to the endoplasmic reticulum and its expression is induced by phenobarbital. The enzyme is known to hydroxylate coumarin, and also metabolizes nicotine, aflatoxin B1, nitrosamines, and some pharmaceuticals. Individuals with certain allelic variants are said to have a poor metabolizer phenotype, meaning they do not efficiently metabolize coumarin or nicotine. This gene is part of a large cluster of cytochrome P450 genes from the CYP2A, CYP2B and CYP2F subfamilies on chromosome 19q. The gene was formerly referred to as CYP2A3; however, it has been renamed CYP2A6. [provided by RefSeq, Jul 2008]

Uniprot Accession IDs

• P11509
• A7YAE5
• B2R7F6
• P00190
• P10890
• Q16803
• Q4VAT9
• Q4VAU0
• Q4VAU1
• Q9H1Z7
• Q9UCU0
• Q9UK48

Gene Name

• CYP2A6

Ensembl ID

• ENST00000301141
• ENSP00000301141
• ENSG00000255974

Symbol

• CYP2A3
• CPA6
• CYP2A
• CYP2A3
• P450PB
• CYPIIA6
• P450C2A

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
drug	1
chemical	0.99
biological term	0.91
co-expressed gene	0.82
molecular function	0.79

Protein Classes

No PANTHER Classes or DTO Classes found

IDG Development Level Summary

Tdark

These are targets about which virtually nothing is known. They do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 1092.65   (req: < 5)

Gene RIFs: 217   (req: <= 3)

Antibodies: 407   (req: <= 50)

Tbio

These targets do not have known drug or small molecule activities
- AND - satisfy two or more of the following criteria:

Pubmed score: 1092.65   (req: >= 5)

Gene RIFs: 217   (req: > 3)

Antibodies: 407   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 16

Tchem

Target has at least one ChEMBL compound with an activity cutoff of < 30 nM - AND - satisfies the preceding conditions

Active Ligands: 106

Tclin

Target has at least one approved drug - AND - satisfies the preceding conditions

Active Drug: 1