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telomerase inhibitor GRN163L A synthetic lipid-conjugated, 13-mer oligonucleotide N3' P5'-thio-phosphoramidate with potential antineoplastic activity. Complementary to the template region of telomerase RNA (hTR), telomerase inhibitor GRN163L as a competitive enzyme inhibitor that binds and blocks the active site of the enzyme (a "telomerase template antagonist"), a mechanism of action which differs from that for the antisense oligonucleotide-mediated inhibition of telomerase activity through telomerase mRNA binding. Inhibition of telomerase activity in tumor cells by telomerase inhibitor GRN163L results in telomere shortening, which leads to cell cycle arrest or apoptosis. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus)
Code name: | | GRN163L | | |
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