Tchem CYP1A2 Cytochrome P450 1A2

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 oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N3-demethylation. Also acts in the metabolism of aflatoxin B1 and acetaminophen. Participates in the bioactivation of carcinogenic aromatic and heterocyclic amines. Catalizes the N-hydroxylation of heterocyclic amines and the O-deethylation of phenacetin. This gene 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. The protein encoded by this gene localizes to the endoplasmic reticulum and its expression is induced by some polycyclic aromatic hydrocarbons (PAHs), some of which are found in cigarette smoke. The enzyme's endogenous substrate is unknown; however, it is able to metabolize some PAHs to carcinogenic intermediates. Other xenobiotic substrates for this enzyme include caffeine, aflatoxin B1, and acetaminophen. The transcript from this gene contains four Alu sequences flanked by direct repeats in the 3' untranslated region. [provided by RefSeq, Jul 2008]

Uniprot Accession IDs

• P05177
• Q16754
• Q6NWU3
• Q6NWU5
• Q9BXX7
• Q9UK49

Gene Name

• CYP1A2

Ensembl ID

• ENST00000343932
• ENSP00000342007
• ENSG00000140505

Symbol

• CP12
• CYPIA2
• P3-450
• P450(PA)

Knowledge Table

Most Knowledge About	Knowledge Value (0 to 1 scale)
chemical	1
drug	1
biological term	0.98
disease	0.85
molecular function	0.81

Protein Classes

PANTHER Classes

Protein / Oxidoreductase / Oxygenase / Cytochrome P450 1a2

DTO Classes

Protein / Enzyme / Oxidoreductase / Oxygenase / Cytochrome P450 1a2

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: 3211.69   (req: < 5)

Gene RIFs: 309   (req: <= 3)

Antibodies: 661   (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: 3211.69   (req: >= 5)

Gene RIFs: 309   (req: > 3)

Antibodies: 661   (req: > 50)

- OR - satisfy the following criterion:

Gene Ontology Terms: 39

Tchem

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

Active Ligands: 1907

Tclin

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

Active Drugs: 30