4'C-Ethynyl-thymidine acts as a chain terminator during DNA-synthesis catalyzed by HIV-1 reverse transcriptase

Summerer, Daniel; Marx, Andreas

4'C-Ethynyl-thymidine acts as a chain terminator during DNA-synthesis catalyzed by HIV-1 reverse transcriptase

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2005

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Open Access Green

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Bioorganic & Medicinal Chemistry Letters. 2005, 15(4), pp. 869-871. ISSN 0960-894X. Available under: doi: 10.1016/j.bmcl.2004.12.072

Zusammenfassung

Recently, 4'C-ethynyl nucleoside analogues have been identified as highly potent agents against HIV-1, including several multidrug-resistant strains. In contrast to most known nucleoside inhibitors 4'C-ethynyl nucleoside analogues possess a 3'-hydroxyl function. Here we show that the 5'O-triphosphate of 4'C-ethynyl thymidine gets readily incorporated into a nascent DNA strand by HIV-1 reverse transcriptase and significantly inhibits further post-incorporation chain extension by the enzyme.

Fachgebiet (DDC)

540 Chemie

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ISO 690

SUMMERER, Daniel, Andreas MARX, 2005. 4'C-Ethynyl-thymidine acts as a chain terminator during DNA-synthesis catalyzed by HIV-1 reverse transcriptase. In: Bioorganic & Medicinal Chemistry Letters. 2005, 15(4), pp. 869-871. ISSN 0960-894X. Available under: doi: 10.1016/j.bmcl.2004.12.072

BibTex

@article{Summerer2005-02-154CEth-434,
  year={2005},
  doi={10.1016/j.bmcl.2004.12.072},
  title={4'C-Ethynyl-thymidine acts as a chain terminator during DNA-synthesis catalyzed by HIV-1 reverse transcriptase},
  number={4},
  volume={15},
  issn={0960-894X},
  journal={Bioorganic & Medicinal Chemistry Letters},
  pages={869--871},
  author={Summerer, Daniel and Marx, Andreas}
}

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