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Drug-Target Interaction

Drug

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PubChem ID:6001
Structure:
Synonyms:
1,4-Dimethyl-2,3-benzophenanthrene
1,4-Dimethyl-2,3-benzphenanthrene
4-05-00-02587 (Beilstein Handbook Reference)
40567_SUPELCO
442425_SUPELCO
45780_FLUKA
45780_RIEDEL
56-56-4
57-97-6
6,7-Dimethyl-1,2-benzanthracene
7,12 Dimethylbenzanthracene
7,12-Dimethyl-1,2-benzanthracene
7,12-Dimethyl-1:2-benz(a)anthracene
7,12-DIMETHYLBENZ(A)ANTHRACENE
7,12-Dimethylbenz(a)anthracene [Polycyclic aromatic compounds]
7,12-Dimethylbenz-[a]-anthracene
7,12-Dimethylbenzanthracene
7,12-DIMETHYLBENZANTHRACENE (SEE ALSO DMBA/TPA/BPO, CAS 57-97-6 AND
7,12-DIMETHYLBENZANTHRACENE (SEE ALSO DMBA/TPA/BPO, CAS 57-97-6 AND DMBA/TPA)
7,12-Dimethylbenzanthrancene
7,12-Dimethylbenzo(a)anthracene
7,12-Dimethylbenzo[a]anthracene
7,12-Dimethylbenz[a]anthracene
7,12-Dimethylbenz[a]anthracene solution
7,12-dimethyltetraphene
7,12-DMBA
9,10-Dimethyl-1,2-benzanthracene
9,10-Dimethyl-1,2-benzanthrazen
9,10-Dimethyl-1,2-benzanthrazen [German]
9,10-dimethyl-benzanthracene
9,10-Dimethylbenz(a)anthracene
9,10-Dimethylbenz[a]anthracene
AC1L1LL0
AG-G-05032
AI3-50460
Benz(a)anthracene, 7,12-dimethyl-
Benz(a)anthracene, 9,10-dimethyl-
Benz[a]anthracene, 7,12-dimethyl-
Benz[a]anthracene, 9,10-dimethyl-
BRN 1912135
C19488
CCRIS 274
CHEBI:254496
CHEMBL329673
D015127
D0677
D3254_SIGMA
DBA
Dimethylbenzanthracene
Dimethylbenzanthrene
Dimethylbenz[a]anthracene
DMBA
DMBA/TPA/BPO/MNNG
EINECS 200-359-5
Ethyl acetate
HMS2232O09
HSDB 2938
LS-235
MLS001333155
MLS001333156
MLS002454381
MolPort-001-789-814
NCGC00091518-01
NCGC00091518-02
NCGC00091518-03
NCGC00091518-04
NCGC00091518-05
NCGC00091518-06
NCGC00091518-07
nchembio.90-comp12
NCI-C03918
NSC 408823
NSC408823
RCRA waste no. U094
RCRA waste number U094
SMR000857253
ST50307413
ST5307413
WLN: L D6 B666J C1 J1
WLN: L D6 B666J F1 G1
ZINC01600920

Target

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Uniprot ID:CP1A1_HUMAN
Synonyms:
CYPIA1
Cytochrome P450 1A1
P450 form 6
P450-C
P450-P1
EC-Numbers:1.14.14.1
Organism:Homo sapiens
Human
PDB IDs:-

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----

References:

10496959
Inhibition of aryl hydrocarbon-induced cytochrome P-450 1A1 enzyme activity and CYP1A1 expression by resveratrol.. H P Ciolino; G C Yeh (1999) Molecular pharmacology display abstract
We investigated the effect of resveratrol, a constituent of the human diet that has been shown to inhibit aryl hydrocarbon-induced carcinogenesis in animals, on the carcinogen activation pathway regulated by the aryl hydrocarbon receptor. Resveratrol inhibited the metabolism of the environmental aryl hydrocarbon benzo[a]pyrene (B[a]P) catalyzed by microsomes isolated from B[a]P-treated human hepatoma HepG2 cells. Resveratrol competitively inhibited, in a concentration-dependent manner, the activity of the carcinogen activating enzymes cytochrome P-450 (CYP)1A1/CYP1A2 in microsomes and intact HepG2 cells. Resveratrol inhibited the B[a]P-induced expression of the CYP1A1 gene, as measured at the mRNA and transcriptional levels. Resveratrol abolished the binding of B[a]P-activated nuclear aryl hydrocarbon receptor to the xenobiotic-responsive element of the CYP1A1 promoter but did not itself bind to the receptor. Resveratrol was also effective in inhibiting CYP1A1 transcription induced by the aryl hydrocarbon dimethylbenz[a]anthracene in human mammary carcinoma MCF-7 cells. These data demonstrate that resveratrol inhibits aryl hydrocarbon-induced CYP1A activity in vitro by directly inhibiting CYP1A1/1A2 enzyme activity and by inhibiting the signal transduction pathway that up-regulates the expression of carcinogen activating enzymes. These activities may be an important part of the chemopreventive activity of resveratrol in vivo.