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Drug-Target Interaction

Drug

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PubChem ID:370
Structure:
Synonyms:
149-91-7
3,4,5-Trihydroxybenzoate
3,4,5-Trihydroxybenzoic acid
3-10-00-02070 (Beilstein Handbook Reference)
398225_SIAL
78563C7D-0E2D-4766-A8EA-670A03C78FCF
AB1002218
AC-1206
AC1L1934
AC1Q732X
AC1Q732Y
Acid, Gallic
AI3-16412
AIDS-001349
AIDS-059239
AIDS001349
AIDS059239
AKOS000119625
ARONIS23903
BB_SC-2795
Benzoic acid, 3,4,5-trihydroxy-
BIDD:ER0374
bmse000389
BRN 2050274
BSPBio_001668
C01424
CCG-38670
CCRIS 5523
CHEBI:30778
CHEMBL288114
CPD-183
D005707
DivK1c_006403
EINECS 205-749-9
G0011
G7384_SIGMA
Gallate
Gallic acid
GALLIC ACID ANHYDROUS
gallic acid for microelectronic industrial
Gallic Acid Hydrate
Gallic acid monohydrate
Gallic acid polymer
Gallic acid, tech
Gallic acid, tech.
GALOP
HMS1923K07
HMS2091A07
HSDB 2117
I14-9302
Jsp002851
KBio1_001347
KBio2_000822
KBio2_003390
KBio2_005958
KBio3_001168
KBioGR_002008
KBioSS_000822
Kyselina 3,4,5-trihydroxybenzoova
Kyselina 3,4,5-trihydroxybenzoova [Czech]
Kyselina gallova
Kyselina gallova [Czech]
LS-870
MolPort-000-881-260
NCGC00091125-01
NCGC00091125-02
NCGC00091125-03
NCGC00091125-04
NCGC00091125-05
nchembio.246-comp4
NSC 20103
NSC 674319
NSC20103
NSC674319
Oprea1_087792
Pyrogallol-5-carboxylic acid
SBB008781
SDCCGMLS-0066503.P001
SPBio_000617
SpecPlus_000307
SPECTRUM210369
Spectrum2_000399
Spectrum3_000254
Spectrum4_001544
Spectrum5_000108
Spectrum_000342
ST083487
STK298718
UNII-632XD903SP
WLN: QVR CQ DQ EQ

Target

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Uniprot ID:JUN_MOUSE
Synonyms:
Activator protein 1
AH119
AP1
Jun A
Proto-oncogene c-jun
Transcription factor AP-1
V-jun avian sarcoma virus 17 oncogene homolog
EC-Numbers:-
Organism:Mouse
Mus musculus
PDB IDs:-

Binding Affinities:

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

References:

10563991
Inhibition of TPA-induced protein kinase C and transcription activator protein-1 binding activities by theaflavin-3,3'-digallate from black tea in NIH3T3 cells.. Y C Chen; Y C Liang; S Y Lin-Shiau; C T Ho; J K Lin (1999) Journal of agricultural and food chemistry display abstract
Tea is one of the most popular beverages in the world. Several reports have shown that both green tea and black tea were able to inhibit tumor cell proliferation in animal models. In this study, we investigated the inhibitory effects of black tea polyphenols including theaflavin (TF-1), the mixture (TF-2) of theaflavin-3-gallate (TF-2a), and theaflavin-3'-gallate (TF-2b), theaflavin-3,3'-digallate (TF-3), thearubigin (TR), and a major green tea polyphenol (-)-epigallocatechin-3-gallate (EGCG) on 12-O-tetradecanoylphorbol 13-acetate (TPA)-induced protein kinase C (PKC) and transcription activator protein-1 (AP-1) binding activities in NIH3T3 cells. On analysis of PKC activity with partial purified preparation, TPA (100 ng/mL) treatment was able to elevate membrane-associated PKC activity approximately 3-fold, and treatment with TF-3 (20 microM) and EGCG (20 microM) showed 94.5% and 9.4% suppression on TPA-induced PKC activity, respectively. Translocation of PKCalpha protein from cytosol to membrane was detected in TPA-treated NIH3T3 cells, and TF-3 was able to block its translocation. By in vitro kinase assay using myelin basic protein (MBP) as a PKC-specific substrate, we found that TPA treatment was able to increase PKC kinase activity by detection of phosphorylated MBP protein and TF-3 showed strongest inhibitory effect on its phosphorylation while EGCG was shown to be less effective. We also analyzed the AP-1 binding activity by electrophoretic mobility shift assay and c-Jun gene expression by northern blot and western blot, the results showed that TF-3 is the most potent inhibitor on TPA-induced AP-1 binding activity and c-Jun gene expression among these five tea polyphenols. Our results might provide new molecular basis for understanding the inhibitory effects of tea polyphenols on TPA-mediated tumor promotion.