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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 cyt ...more
Illumination Graph
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


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: 733.85   (req: < 5)
Gene RIFs: 190   (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: 733.85   (req: >= 5)
Gene RIFs: 190   (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: 32
Tclin

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

Active Drug: 0
Protein Data Bank (11)
1 – 5 of 11
PDB Structure Id
Ligand
Method
Resolution (Å)
M.W. (kDa)
Pub Year
Title
PDB Structure Id
M.W.
Resolution
Pub Year
Pathways (59)
Biological oxidations (R-HSA-211859)

Click on a row in the table to change the structure displayed.

Items per page:
1 – 5 of 6
Data Source
Name
Explore in Pharos
Explore in Source
Reactome
Biological oxidations
Reactome
CYP2E1 reactions
Reactome
Cytochrome P450 - arranged by substrate type
Reactome
Metabolism
Reactome
Phase I - Functionalization of compounds
Name
Explore in Pharos
Explore in Source
Biological oxidations
CYP2E1 reactions
Cytochrome P450 - arranged by substrate type
Metabolism
Phase I - Functionalization of compounds
Gene Ontology Terms (21)
Items per page:
10
1 – 7 of 7
GO Term
Evidence
Assigned by
Inferred from Direct Assay (IDA)
UniProtKB
Inferred from Direct Assay (IDA)
UniProtKB
Inferred from Physical Interaction (IPI)
BHF-UCL
Inferred from Biological aspect of Ancestor (IBA)
GO_Central
Inferred from Biological aspect of Ancestor (IBA)
GO_Central
Inferred from Biological aspect of Ancestor (IBA)
GO_Central
Inferred from Electronic Annotation (IEA)
InterPro
Protein-Protein Interactions (114)
1 – 10 of 114
CYP2A7
Tbio
Novelty: 0.01122023
p_int: 1
Score: 0.943
Data Source: BioPlex,STRINGDB
RABAC1
Tbio
Novelty: 0.0162976
p_int: 0.761078473
p_ni: 0.00043792
p_wrong: 0.238483607
Score: 0.544
Data Source: BioPlex,STRINGDB
EPHX1
Tchem
Family: Enzyme
Novelty: 0.00210581
Score: 0.96
Data Source: STRINGDB
NAT2
Tbio
Family: Enzyme
Novelty: 0.00163877
Score: 0.955
Data Source: STRINGDB
AOX1
Tbio
Family: Enzyme
Novelty: 0.00323057
Score: 0.954
Data Source: STRINGDB
CYP3A4
Tclin
Family: Enzyme
Novelty: 0.00020884
Score: 0.949
Data Source: STRINGDB
DPYD
Tclin
Family: Enzyme
Novelty: 0.0022785
Score: 0.945
Data Source: STRINGDB
CYP4A11
Tbio
Novelty: 0.01325821
Score: 0.944
Data Source: STRINGDB
CYP3A5
Tclin
Family: Enzyme
Novelty: 0.00135473
Score: 0.942
Data Source: STRINGDB
CYP3A7
Tclin
Family: Enzyme
Novelty: 0.00963214
Score: 0.941
Data Source: STRINGDB
Publication Statistics
PubMed Score  733.85

PubMed score by year
PubTator Score  660.53

PubTator score by year
Amino Acid Sequence
Residue Counts
Sequence
MLASGMLLVALLVCLTVMVLMSVWQQRKSKGKLPPGPTPLPFIGNYLQLNTEQMYNSLMKISERYGPVFT
1-70
IHLGPRRVVVLCGHDAVREALVDQAEEFSGRGEQATFDWVFKGYGVVFSNGERAKQLRRFSIATLRDFGV
70-140
GKRGIEERIQEEAGFLIDALRGTGGANIDPTFFLSRTVSNVISSIVFGDRFDYKDKEFLSLLRMMLGIFQ
140-210
FTSTSTGQLYEMFSSVMKHLPGPQQQAFQLLQGLEDFIAKKVEHNQRTLDPNSPRDFIDSFLIRMQEEEK
210-280
NPNTEFYLKNLVMTTLNLFIGGTETVSTTLRYGFLLLMKHPEVEAKVHEEIDRVIGKNRQPKFEDRAKMP
280-350
YMEAVIHEIQRFGDVIPMSLARRVKKDTKFRDFFLPKGTEVFPMLGSVLRDPSFFSNPQDFNPQHFLNEK
350-420
GQFKKSDAFVPFSIGKRNCFGEGLARMELFLFFTTVMQNFRLKSSQSPKDIDVSPKHVGFATIPRNYTMS
420-490
FLPR
490-494
MLASGMLLVALLVCLTVMVLMSVWQQRKSKGKLPPGPTPLPFIGNYLQLNTEQMYNSLMKISERYGPVFTIHLGPRRVVVLCGHDAVREALVDQAEEFSGRGEQATFDWVFKGYGVVFSNGERAKQLRRFSIATLRDFGVGKRGIEERIQEEAGFLIDALRGTGGANIDPTFFLSRTVSNVISSIVFGDRFDYKDKEFLSLLRMMLGIFQFTSTSTGQLYEMFSSVMKHLPGPQQQAFQLLQGLEDFIAKKVEHNQRTLDPNSPRDFIDSFLIRMQEEEKNPNTEFYLKNLVMTTLNLFIGGTETVSTTLRYGFLLLMKHPEVEAKVHEEIDRVIGKNRQPKFEDRAKMPYMEAVIHEIQRFGDVIPMSLARRVKKDTKFRDFFLPKGTEVFPMLGSVLRDPSFFSNPQDFNPQHFLNEKGQFKKSDAFVPFSIGKRNCFGEGLARMELFLFFTTVMQNFRLKSSQSPKDIDVSPKHVGFATIPRNYTMSFLPR