Names & Taxonomy

Uniprot ID:
P11509
Entry Name:
CP2A6_HUMAN
Status:
reviewed
Protein Names:
Cytochrome P450 2A6 (EC 1.14.13.-) (1,4-cineole 2-exo-monooxygenase) (CYPIIA6) (Coumarin 7-hydroxylase) (Cytochrome P450 IIA3) (Cytochrome P450(I))
Gene Names:
CYP2A6 CYP2A3
Gene Names Primary:
CYP2A6
Organism:
Homo sapiens (Human)

Structure

Length:
494
Sequence:
MLASGMLLVALLVCLTVMVLMSVWQQRKSKGKLPPGPTPLPFIGNYLQLNTEQMYNSLMKISERYGPVFTIHLGPRRVVVLCGHDAVREALVDQAEEFSGRGEQATFDWVFKGYGVVFSNGERAKQLRRFSIATLRDFGVGKRGIEERIQEEAGFLIDALRGTGGANIDPTFFLSRTVSNVISSIVFGDRFDYKDKEFLSLLRMMLGIFQFTSTSTGQLYEMFSSVMKHLPGPQQQAFQLLQGLEDFIAKKVEHNQRTLDPNSPRDFIDSFLIRMQEEEKNPNTEFYLKNLVMTTLNLFIGGTETVSTTLRYGFLLLMKHPEVEAKVHEEIDRVIGKNRQPKFEDRAKMPYMEAVIHEIQRFGDVIPMSLARRVKKDTKFRDFFLPKGTEVFPMLGSVLRDPSFFSNPQDFNPQHFLNEKGQFKKSDAFVPFSIGKRNCFGEGLARMELFLFFTTVMQNFRLKSSQSPKDIDVSPKHVGFATIPRNYTMSFLPR
Proteomes:
UP000005640

Subcellular location

Subcellular Location:
Endoplasmic reticulum membrane; Peripheral membrane protein. Microsome membrane; Peripheral membrane protein.

Function

Function:
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.
Catalytic Activity:
1,4-cineole + NADPH + O(2) = 2-exo-hydroxy-1,4-cineole + NADP(+) + H(2)O.
Cofactor:
COFACTOR: Name=heme; Xref=ChEBI:CHEBI:30413;
Kinetics:
BIOPHYSICOCHEMICAL PROPERTIES: Kinetic parameters: KM=0.23 uM for coumarin
Cross Reference Drug Bank:
DB00316 DB01118 DB00381 DB01351 DB00182 DB01435 DB01274 DB00972 DB00207 DB00921 DB01156 DB00356 DB00568 DB00604 DB00636 DB00882 DB00257 DB00363 DB00531 DB06292 DB01151 DB01234 DB01191 DB00255 DB00470 DB00216 DB04953 DB04841 DB01544 DB00544 DB00690 DB01213 DB00983 DB01159 DB01181 DB00951 DB01026 DB01006 DB00281 DB04871 DB01043 DB00170 DB00763 DB00553 DB01028 DB01011 DB01110 DB00471 DB00238 DB00184 DB01115 DB06712 DB01059 DB00312 DB01174 DB01085 DB00860 DB00396 DB00818 DB01045 DB00412 DB01037 DB01236 DB06729 DB00675 DB00752 DB00755 DB01361 DB00313 DB09068 DB00495
Gene Ontology Go:
cytoplasmic microtubule
endoplasmic reticulum membrane
arachidonic acid epoxygenase activity
coumarin 7-hydroxylase activity
enzyme binding
heme binding
iron ion binding
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
steroid hydroxylase activity
coumarin catabolic process
coumarin metabolic process
drug metabolic process
epoxygenase P450 pathway
exogenous drug catabolic process
small molecule metabolic process
steroid metabolic process
xenobiotic metabolic process
Gene Ontology Biological Process:
coumarin catabolic process
coumarin metabolic process
drug metabolic process
epoxygenase P450 pathway
exogenous drug catabolic process
small molecule metabolic process
steroid metabolic process
xenobiotic metabolic process
Gene Ontology Molecular Function:
arachidonic acid epoxygenase activity
coumarin 7-hydroxylase activity
enzyme binding
heme binding
iron ion binding
oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
steroid hydroxylase activity
Gene Ontology Cellular Component:
cytoplasmic microtubule
endoplasmic reticulum membrane
Keywords:
3D-structure
Complete proteome
Direct protein sequencing
Endoplasmic reticulum
Heme
Iron
Membrane
Metal-binding
Microsome
Monooxygenase
NADP
Oxidoreductase
Phosphoprotein
Polymorphism
Reference proteome

Publication

PubMed ID:
2726448 2748347 2322567 14702039 15057824 15489334 1889415 1944238 11278503 3856261 11695850 24275569 16086027 17125252 18779312 9409631 10544257 11237731 15618701 12721789 15469410 18360915 18216723