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Gln151 of HIV-1 reverse transcriptase acts as a steric gate towards clinically relevant acyclic phosphonate nucleotide analogues.

Antoine Frangeul Cécile Bussetta Jérôme Deval Karine Barral 1 Karine Alvarez 2 Bruno Canard 2
1 CRCM - Centre de Recherche en Cancérologie de Marseille
2 AFMB - Architecture et fonction des macromolécules biologiques
Abstract : In the treatment of HIV, the loose active site of the HIV-1 reverse transcriptase (RT) allows numerous nucleotide analogues to act as proviral DNA 'chain-terminators'. Acyclic nucleotide phosphonate analogues (ANPs) represent a particular class of nucleotide analogue that does not possess a ribose moiety. The structural basis for their substrate efficiency regarding viral DNA polymerases is poorly understood.
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Journal articles
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https://hal-amu.archives-ouvertes.fr/hal-02061712
Contributor : Karine Barral <>
Submitted on : Friday, March 8, 2019 - 12:04:19 PM
Last modification on : Wednesday, December 16, 2020 - 3:34:03 PM

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  • HAL Id : hal-02061712, version 1
  • PUBMED : 18389906

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UNIV-AMU | CNRS | INRA | CRCM | INRAE

Citation

Antoine Frangeul, Cécile Bussetta, Jérôme Deval, Karine Barral, Karine Alvarez, et al.. Gln151 of HIV-1 reverse transcriptase acts as a steric gate towards clinically relevant acyclic phosphonate nucleotide analogues.. Antiviral Therapy, International Medical Press, 2019, 13 (1), pp.115-24. ⟨hal-02061712⟩

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