| Target Validation Information | |||||
|---|---|---|---|---|---|
| Target ID | T86052 | ||||
| Target Name | Telomerase reverse transcriptase | ||||
| Target Type | Clinical Trial |
||||
| Drug Potency against Target | GRN163 | Drug Info | IC50 = 0.1 nM | [527581] | |
| Action against Disease Model | Imetelstat | GRN163 has been shown to inhibit telomerase activity in 19 t uMor cell lines, with an average IC50 of 0.5-1.0 uM. | [552542] | Drug Info | |
| The Effect of Target Knockout, Knockdown or Genetic Variations | Late generation telomerase knockout mice exhibited impaired exocrine pancreatic regeneration after acute pancreatitis as seen by persistence of metaplastic acinar cells and markedly reduced proliferation. The expression levels of p53 and p21 were not significantly increased in regenerating pancreas of late generation telomerase knockout mice compared to wild-type mice. | [552542] | |||
| References | |||||
| Ref 552542 | Telomerase antagonists GRN163 and GRN163L inhibit tumor growth and increase chemosensitivity of human hepatoma. Hepatology. 2005 Nov;42(5):1127-36. | ||||
| Ref 527581 | Oncogene. 2005 Aug 4;24(33):5262-8.Lipid modification of GRN163, an N3'-->P5' thio-phosphoramidate oligonucleotide, enhances the potency of telomerase inhibition. | ||||
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