Title: Influence of the linkage between leaving group and nucleoside on substrate efficiency for incorporation in DNA catalyzed by reverse transcriptase
Authors: Giraut, Anne
Herdewijn, Piet # ×
Issue Date: Jul-2010
Publisher: Wiley-VCH
Series Title: Chembiochem vol:11 issue:10 pages:1399-403
Abstract: An amino acid deoxyadenosine phosphoramidate and the corresponding phosphodiester congener have been synthesized and tested for primer extension by HIV-1 reverse transcriptase. Replacement of the phosphoramidate linkage of L-histidine-dAMP by a phosphodiester linkage was found to have a beneficial influence on the affinity of this substrate towards HIV-1 reverse transcriptase and on the velocity of the nucleotide incorporation reaction. Modifications of the nature of the P--X bond can be useful to fine-tune the substrate properties of nucleoside triphosphate analogues. Our results also demonstrate that polymerization pausing observed during the incorporation of leaving group modified dNTPs is not caused by the nature of the linkage.
ISSN: 1439-4227
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Medicinal Chemistry (Rega Institute)
Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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