Tclin CYP3A4 Cytochrome P450 3A4

Protein Summary

Description

Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,8-cineole 2-exo-monooxygenase. The enzyme also hydroxylates etoposide (PubMed:11159812). Catalyzes 4-beta-hydroxylation of cholesterol. May catalyze 25-hydroxylation of cholesterol in vitro (PubMed:21576599). This gene encodes a member of the cytochrome P450 superfamily of enzymes. The cytochrome P450 proteins are monooxygenases that 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 glucocorticoids and some pharmacological agents. This enzyme is involved in the metabolism of approximately half the drugs in use today, including acetaminophen, codeine, cyclosporin A, diazepam and erythromycin. The enzyme also metabolizes some steroids and carcinogens. This gene is part of a cluster of cytochrome P450 genes on chromosome 7q21.1. Previously another CYP3A gene, CYP3A3, was thought to exist; however, it is now thought that this sequence represents a transcript variant of CYP3A4. Alternatively spliced transcript variants encoding different isoforms have been identified. [provided by RefSeq, Feb 2011]

Uniprot Accession IDs

• P08684
• P05184
• Q16757
• Q9UK50

Gene Name

• CYP3A4

Ensembl ID

• ENST00000336411
• ENSP00000337915
• ENSG00000160868

Symbol

• CYP3A3
• HLP
• CP33
• CP34
• CYP3A
• NF-25
• CYP3A3
• P450C3
• CYPIIIA3
• CYPIIIA4
• P450PCN1

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
chemical	1
drug	1
molecular function	0.96
disease	0.85
pathway	0.81

Protein Classes

PANTHER Classes

Protein / Oxidoreductase / Oxygenase / Cytochrome P450 3a4

DTO Classes

Protein / Enzyme / Oxidoreductase / Oxygenase / Cytochrome P450 3a4

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: 8043.8   (req: < 5)

Gene RIFs: 683   (req: <= 3)

Antibodies: 551   (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: 8043.8   (req: >= 5)

Gene RIFs: 683   (req: > 3)

Antibodies: 551   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 30

Tchem

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

Active Ligands: 1814

Tclin

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

Active Drugs: 40