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Telomerase inhibitors--oligonucleotide phosphoramidates as potential therapeutic agents.
Gryaznov, S; Pongracz, K; Matray, T; Schultz, R; Pruzan, R; Aimi, J; Chin, A; Harley, C; Shea-Herbert, B; Shay, J; Oshima, Y; Asai, A; Yamashita, Y.
Affiliation
  • Gryaznov S; Geron Corporation, 230 Constitution Drive, Menlo Park, California 94025, USA.
Nucleosides Nucleotides Nucleic Acids ; 20(4-7): 401-10, 2001.
Article in En | MEDLINE | ID: mdl-11563055
ABSTRACT
We have designed, synthesized, and evaluated using physical, chemical and biochemical assays various oligonucleotide N3'-->P5' phosphoramidates, as potential telomerase inhibitors. Among the prepared compounds were 2'-deoxy, 2'-hydroxy, 2'-methoxy, 2'-ribo-fluoro, and 2'-arabino-fluoro oligonucleotide phosphoramidates, as well as novel N3'-->P5' thio-phosphoramidates. The compounds demonstrated sequence specific and dose dependent activity with IC50 values in the sub-nM to pM concentration range.
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Collection: 01-internacional Database: MEDLINE Main subject: Oligonucleotides / Phosphoric Acids / Telomerase / Enzyme Inhibitors / Amides Limits: Humans Language: En Journal: Nucleosides Nucleotides Nucleic Acids Journal subject: BIOQUIMICA Year: 2001 Document type: Article Affiliation country: United States
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Collection: 01-internacional Database: MEDLINE Main subject: Oligonucleotides / Phosphoric Acids / Telomerase / Enzyme Inhibitors / Amides Limits: Humans Language: En Journal: Nucleosides Nucleotides Nucleic Acids Journal subject: BIOQUIMICA Year: 2001 Document type: Article Affiliation country: United States