Details of the Biological Target of DIG (DBT)

General Information of DBT (ID: ET0AF1R)
Name
Coumarin 7-hydroxylase (CYP2A6)
Synonyms    Click to Show/Hide the Synonyms of This DBT
Cytochrome P450 2A6; 1,4-cineole 2-exo-monooxygenase; CYP2A3; CYP2A6; CYPIIA6; Cytochrome P450 IIA3; Cytochrome P450(I)
Family Oxidoreductase (ORase)  >>  Oxygen paired donor oxidoreductase (EC 1.14)
Organism
Homo sapiens (Human)
Gene Name CYP2A6 Gene ID
1548
UniProt ID CP2A6_HUMAN (click to find more protein-related data of this DBT)
TTD ID T06455 (click to find more therapeutic target data of this DBT)
INTEDE ID DME0005 (click to find more drug-metabolizing enzyme data of this DBT)
   Click to Show/Hide the Molecular/Function Data (Sequence/Function) of This Target
Sequence
MLASGMLLVALLVCLTVMVLMSVWQQRKSKGKLPPGPTPLPFIGNYLQLNTEQMYNSLMK
ISERYGPVFTIHLGPRRVVVLCGHDAVREALVDQAEEFSGRGEQATFDWVFKGYGVVFSN
GERAKQLRRFSIATLRDFGVGKRGIEERIQEEAGFLIDALRGTGGANIDPTFFLSRTVSN
VISSIVFGDRFDYKDKEFLSLLRMMLGIFQFTSTSTGQLYEMFSSVMKHLPGPQQQAFQL
LQGLEDFIAKKVEHNQRTLDPNSPRDFIDSFLIRMQEEEKNPNTEFYLKNLVMTTLNLFI
GGTETVSTTLRYGFLLLMKHPEVEAKVHEEIDRVIGKNRQPKFEDRAKMPYMEAVIHEIQ
RFGDVIPMSLARRVKKDTKFRDFFLPKGTEVYPMLGSVLRDPSFFSNPQDFNPQHFLNEK
GQFKKSDAFVPFSIGKRNCFGEGLARMELFLFFTTVMQNFRLKSSQSPKDIDVSPKHVGF
ATIPRNYTMSFLPR
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. Possesses low phenacetin O-deethylation activity.
Full List of Drug Inactive Ingredients (DIGs) Regulating This DBT
          DIG Name: Benzaldehyde Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Antimicrobial preservative
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 3920 nM (tested by experiment) [1]
                   Tested Species Homo sapiens (Human)
                   UniProt ID CP2A6_HUMAN
          DIG Name: Beta-naphthol Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Antimicrobial preservative
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 139958.73 nM (tested by experiment) [2]
                   Tested Species Homo sapiens (Human)
                   UniProt ID CP2A6_HUMAN
          DIG Name: Polyoxyl 40 stearate Click to Show/Hide
             Detailed Information DIG Info click to show the detail info of this DIG
             Functional Class    Click to Show/Hide the Functional Class of This DIG
Emulsifying agent; Surfactant
             Experiment for Assessing the Biological Activity of This DIG on the Studied DBT
                   Biological Activity IC50 = 950.1 uM (tested by experiment) [3]
                   Tested Species Homo sapiens (Human)
                   UniProt ID CP2A6_HUMAN
References
1 Quantitative structure-activity relationship analysis of inhibitors of the nicotine metabolizing CYP2A6 enzyme. J Med Chem. 2005 Jan 27; 48(2):440-9.
2 Exploring QSAR and QAAR for inhibitors of cytochrome P450 2A6 and 2A5 enzymes using GFA and G/PLS techniques. Eur J Med Chem. 2009 May; 44(5):1941-51.
3 Effects of polyoxyethylene (40) stearate on the activity of P-glycoprotein and cytochrome P450. Eur J Pharm Sci. 2009 Jul 12;37(5):573-80.

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