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Drug-Target Interaction

Drug

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PubChem ID:3501
Structure:
Synonyms:
"gö 6976"
"insolution™ gö 6976"
12-(2-Cyanoethyl)-6,7,12,13-tetrahydro-13-methyl-5-oxo-5H-indolo(2,3-a)pyrrolo(3,4-c)-carbazole
12-(2-cyanoethyl)-6,7,12,13-tetrahydro-13-methyl-5-oxo-5H-indolo[2,3-a]pyrolo[3,4-c]carbazole
12H-Indolo(2,3-a)pyrrolo(3,4-c)carbazole-12-propanenitrile,
12H-Indolo(2,3-a)pyrrolo(3,4-c)carbazole-12-propanenitrile, 5,6,7,13-tetrahydro-13-methyl-5-oxo-
12H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-12-propanenitrile, 5,6,7,13-tetrahydro-13-methyl-5-oxo-
13-Methyl-5-oxo-5,6,7,13-tetrahydro-12H-indolo(2,3-a)pyrrolo(3,4-c)carbazole-12-propanenitrile
136194-77-9
3-(13-methyl-5-oxo-5,6,7,13-tetrahydro-12H-indolo[2,3-a]pyrrolo[3,4-c]carbazol-12-yl)propanenitrile
3-(13-Methyl-5-oxo-6,7-dihydro-5H-indolo[2,3-a]pyrrolo[3,4-c]carbazol-12(13H)-yl)propanenitrile
AIDS-044729
AIDS044729
BCBcMAP01_000156
Bio1_000157
Bio1_000646
Bio1_001135
Bio2_000381
Bio2_000861
BSPBio_001101
C081021
C24H20N4O
CBiol_001871
CHEBI:51913
Gö 6976
G? 6976
Go 6976
Go 6976, Solution
Go-6976
Go6976
Goe 6976
IDI1_002136
InSolution™ Gö 6976
KBio2_000441
KBio2_003009
KBio2_005577
KBio3_000821
KBio3_000822
KBioGR_000441
KBioSS_000441
LS-172954
NCGC00163451-01
NCGC00163451-02
nchembio.154-comp7
nchembio.95-comp18

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.