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Drug-Target Interaction

Drug

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PubChem ID:88881
Structure:
Synonyms:
21392-57-4
4H-1-Benzopyran-4-one, 5,7-dimethoxy-2-phenyl-
5,7-Dimethoxy-2-phenyl-4H-chromen-4-one
5,7-dimethoxy-2-phenylchromen-4-one
5,7-Dimethoxyflavone
AC1L3GOM
AC1Q4EPT
AIDS-059328
AIDS059328
AKOS002255361
BRD-K81298036-001-02-1
BSPBio_002847
C060298
C10029
CCG-39297
CHEMBL275391
Chrysin 5,7-dimethyl ether
Chrysin dimethyl ether
Chrysin dimethylether
Chrysin DME
Dimethylchrysin
DivK1c_007009
Flavone, 5,7-dimethoxy-
HMS2269A24
KBio1_001953
KBio2_000844
KBio2_003412
KBio2_005980
KBio3_002067
KBioGR_001777
KBioSS_000844
LMPK12110188
MEGxp0_001682
MLS001049094
MolPort-001-835-896
NCGC00178436-01
NSC741743
Oprea1_482940
SMR000386927
SPBio_001577
SpecPlus_000913
Spectrum2_001359
Spectrum3_001034
Spectrum4_001169
Spectrum5_001712
Spectrum_000364
ST5309370
STK921429
STOCK1N-17980
ZINC00407231

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:

15661813
5,7-Dimethoxyflavone downregulates CYP1A1 expression and benzo[a]pyrene-induced DNA binding in Hep G2 cells.. Xia Wen; U Kristina Walle; Thomas Walle (2005) Carcinogenesis display abstract
The objective of this study was to examine the ability of dietary polyphenols to inhibit cytochrome P450 (CYP) 1A1 expression and activity and benzo[a]pyrene (BaP) DNA binding, with the main emphasis on prevention of chemical-induced hepatic carcinogenesis. For this purpose we used Hep G2 cells, a good model of the normal human hepatocyte for CYP1A1 cell signaling. First, when these cells were exposed to a low concentration (1 microM) of BaP, DNA binding occurred, which dramatically increased after 6 h of treatment. BaP also dramatically induced CYP1A1 activity, protein expression and mRNA levels, the likely reason for the marked increase in DNA binding. Second, we screened 25 polyphenols with highly varying chemical structures for maximum ability to inhibit CYP1A1 activity in the Hep G2 cells. Highly varying responses were obtained, ranging from a 10-fold induction by some polyphenols to almost complete inhibition, in particular by 5,7-dimethoxyflavone (DMF), a flavonoid found in some tropical plants. Third, we examined the ability of DMF to inhibit DNA binding of BaP and the mechanisms involved. DMF (2-20 microM) inhibited BaP-induced DNA binding. DMF also inhibited BaP-induced CYP1A1 activity, CYP1A1 protein expression and mRNA levels. Moreover, DMF directly inhibited the catalytic activity of recombinant CYP1A1 with an IC50 of 0.8 microM. In conclusion, DMF was a highly potent inhibitor of BaP-induced DNA binding and CYP1A1 protein expression and activity in the Hep G2 cells. These properties may make DMF an effective chemoprotectant in chemical-induced liver cancer.