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Drug-Target Interaction

Drug

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PubChem ID:2396
Structure:
Synonyms:
"gö 6850"
"insolution™ bisindolylmaleimide i"
133052-90-1
1H-Pyrrole-2,5-dione,
1H-Pyrrole-2,5-dione, 3-(1-(3-(dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-indol-3-yl)-
1uu8
1zrz
2-(1-(3-Dimethylaminopropyl)indol-3-yl)-3-(indol-3-yl)maleimide
2-[1-(3-Dimethylaminopropyl)-1H-indol-3-yl]-3-(1H-indol-3-yl)-maleimide
3-(1-(3-(Dimethylamino)propyl)-1H-indol-3-yl)-4-(1H-indol-3-yl)-1H-pyrrole-2,5-dione
3-{1-[3-(DIMETHYLAMINO)PROPYL]-1H-INDOL-3-YL}-4-(1H-INDOL-3-YL)-1H-PYRROLE-2,5-DIONE
6850
BI1
BIM-1
Bio2_000420
Bio2_000900
BiomolKI2_000039
BiomolKI_000031
BIS-1 cpd
Bisindolylmaleimide I
bisindoylmaleimide I
BSPBio_001160
C070515
C11238
C25H24N4O2
Gö 6850
GF 109203X
GF-109203X
GF109203X
GFX 203290
Go 6850
Go-6850
HSCI1_000290
IDI1_002175
IN1033
IN1518
IN1521
InSolution™ Bisindolylmaleimide I
KBio2_000500
KBio2_003068
KBio2_005636
KBio3_000919
KBio3_000920
KBioGR_000500
KBioSS_000500
LS-172856
NCGC00024760-01
NCGC00024760-02
NCGC00024760-03
NCGC00024760-04
nchembio.154-comp5
RBT205 INHIBITOR
Tocris-0741

Target

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Uniprot ID:POKL_HUMAN
Synonyms:
Putative HERV-K_Xq28 provirus ancestral Pol protein
EC-Numbers:2.7.7.49
Organism:Homo sapiens
Human
PDB IDs:-

Binding Affinities:

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

References:

11642552
Protein kinase C modulates telomerase activity in human cervical cancer cells.. Y W Kim; S Y Hur; T E Kim; J M Lee; S E Namkoong; I K Ki; J W Kim (2001) Experimental & molecular medicine display abstract
Telomerase, a ribonucleoprotein reverse transcriptase that extends telomeres of eukaryotic chromosomes is repressed in normal somatic cells but is activated during development and neoplasia. The regulation mechanism of telomerase activity in cancer cells is not clearly known. In this report, a possible affect of PKC on telomerase activity was examined using HeLa and CUMC-6 cervical cancer cell lines. Exposure of cells to PKC inhibitor, bisindolylmaleimide I and G6976, and high levels of PKC activator, 12-O-tetradecanoyl phorbol 13-acetate (TPA) resulted in the inhibition of PKC activity in both cells. Telomerase activities were also inhibited by bisindolyl-maleimide I and G6976, respectively, in a time-dependent manner. As PKC activity changes in TPA-treated cervical cancer cells, telomerase activities were increased at low dose of TPA and decreased at high dose. The expression levels of human telomerase subunits, human telomerase RNA (hTR) were not influenced by PKC modulating drugs. In contrast, the expression of full-length human telomerase reverse transcriptase (hTERT) was decreased after exposure to bisindolylmaleimide I and G6976 in a time-dependent manner. hTERT expression was not affected by low dose of TPA. In contrast, high dose of TPA inhibited hTERT expression level. But the expression patterns of beta-deletion transcript of hTERT after 72 h of treatment with PKC inhibitors or high dose of TPA exposure were not discernable as compared with those of full-length hTERT transcripts to PKC modulating drugs. These results suggest that PKC-modulating drugs altered telomerase activities by affecting full-length hTERT expression profile in human cervical cancers.