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dc.contributor.authorDikmen, ZG
dc.contributor.authorGellert, GC
dc.contributor.authorJackson, S
dc.contributor.authorGryaznov, S
dc.contributor.authorTressler, R
dc.contributor.authorDogan, P
dc.contributor.authorWright, WE
dc.contributor.authorShay, JW
dc.date.accessioned2019-12-16T10:29:23Z
dc.date.available2019-12-16T10:29:23Z
dc.date.issued2005
dc.identifier.issn0008-5472
dc.identifier.urihttps://doi.org/10.1158/0008-5472.CAN-05-1215
dc.identifier.urihttp://hdl.handle.net/11655/20109
dc.description.abstractDifferential regulation of telomerase activity in normal and tumor cells provides a rationale for the design of new classes of telomerase inhibitors. The telomerase enzyme complex presents multiple potential sites for the development of inhibitors. GRN163L, a telomerase enzyme antagonist, is a lipid-modified 13-mer oligonucleotide N3' -> P5'-thiophosphoramidate, complementary to the template region of telomerase RNA (hTR). We evaluated both the in vitro and in vivo effects of GRN163L using A549-luciferase (A549-Luc) human lung cancer cells expressing a luciferase reporter. GRN163L (1 mu mol/L) effectively inhibits telomerase activity of A549-Luc cells, resulting in progressive telomere shortening. GRN163L treatment also reduces colony formation in soft agar assays. Surprisingly, after only I week of treatment with GRN163L, A549-Luc cells were unable to form robust colonies in the clonal. efficiency assay, whereas the mismatch control compound had no effect. Finally, we show that in vivo treatment with GRN163L is effective in preventing lung metastases in xenograft animal models. These in vitro and in vivo data support the development of GRN163L as a therapeutic for the treatment of cancer.
dc.language.isoen
dc.publisherAmer Assoc Cancer Research
dc.relation.isversionof10.1158/0008-5472.CAN-05-1215
dc.rightsinfo:eu-repo/semantics/openAccess
dc.subjectOncology
dc.titleIn Vivo Inhibition Of Lung Cancer By Grn163L: A Novel Human Telomerase Inhibitor
dc.typeinfo:eu-repo/semantics/article
dc.typeinfo:eu-repo/semantics/publishedVersion
dc.relation.journalCancer Research
dc.contributor.departmentBiyokimya
dc.identifier.volume65
dc.identifier.issue17
dc.identifier.startpage7866
dc.identifier.endpage7873
dc.description.indexWoS
dc.description.indexScopus


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