PMID- 12836339 OWN - NLM STAT- MEDLINE DCOM- 20030815 LR - 20201208 IP - 1 DP - 2001 TI - Telomerase-inhibitory effects of the triphosphate derivatives of some biologically active nucleosides. PG - 211-2 AB - Telomerase is a ribonucleoprotein reverse transcriptase that uses its internal RNA moiety as a template for synthesis of telomere repeats. To clarify the susceptibility of telomerase to HIV-1 reverse transcriptase inhibitors (RT), we investigated the inhibitory effects of 3'-azido-3'-deoxythymidine 5'-triphosphate (AZTTP), which is known to be a potent HIV-1 RT inhibitor, and acyclovir triphosphate (ACVTP). Lineweaver-Burk plot analyses showed that the inhibition mode of these compounds was competitive with the substrate dNTP counterpart. However, inhibition by AZTTP was weak (Ki = 15 microM, Km of dTTP = 7.1 microM). Interestingly, ACVTP showed considerable inhibition. The Ki value of ACVTP was 5.0 microM, being smaller than the Km of dGTP (12 microM). FAU - Yamaguchi, T AU - Yamaguchi T AD - Department of Biological Sciences, Biotechnology Research Center, Teikyo University of Science and Technology, Uenohara, Yamanashi 409-0193, Japan. FAU - Takayama, Y AU - Takayama Y FAU - Saito, M AU - Saito M FAU - Ishikawa, F AU - Ishikawa F FAU - Saneyoshi, M AU - Saneyoshi M LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PL - England TA - Nucleic Acids Res Suppl JT - Nucleic acids research. Supplement (2001) JID - 101169367 RN - 0 (Dideoxynucleotides) RN - 0 (Nucleosides) RN - 0 (Reverse Transcriptase Inhibitors) RN - 0 (Thymine Nucleotides) RN - 4B9XT59T7S (Zidovudine) RN - 66341-18-2 (acyclovir triphosphate) RN - 6RGF96R053 (zidovudine triphosphate) RN - EC 2.7.7.49 (Telomerase) RN - X4HES1O11F (Acyclovir) SB - IM MH - Acyclovir/*analogs & derivatives/chemistry/*pharmacology MH - Dideoxynucleotides MH - HeLa Cells MH - Humans MH - Nucleosides/chemistry MH - Reverse Transcriptase Inhibitors/chemistry/*pharmacology MH - Telomerase/*metabolism MH - Thymine Nucleotides/chemistry/*pharmacology MH - Zidovudine/*analogs & derivatives/chemistry/*pharmacology EDAT- 2003/07/03 05:00 MHDA- 2003/08/16 05:00 CRDT- 2003/07/03 05:00 PHST- 2003/07/03 05:00 [pubmed] PHST- 2003/08/16 05:00 [medline] PHST- 2003/07/03 05:00 [entrez] AID - 10.1093/nass/1.1.211 [doi] PST - ppublish SO - Nucleic Acids Res Suppl. 2001;(1):211-2. doi: 10.1093/nass/1.1.211.