Title: Looking for new pyrimidine acyclic nucleotide analogues designed for phosphorylation by human UMP-CMP kinase
Authors: Topalis, Dimitrios ×
Kumamoto, Hiroki
Alexandre, Julie A C
Dugué, Laurence
Pochet, Sylvie
Berteina-Raboin, Sabine
Agrofoglio, Luigi A
Deville-Bonne, Dominique #
Issue Date: 2007
Publisher: Marcel Dekker
Series Title: Nucleosides, Nucleotides & Nucleic Acids vol:26 issue:10-12 pages:1369-73
Abstract: Human UMP-CMP kinase is involved in the phosphorylation of nucleic acid precursors and also in the activation of antiviral analogues including cidofovir, an acyclic phosphonate compound that mimicks dCMP and shows a broad antiviral spectrum. The binding of ligands to the enzyme was here investigated using a fluorescent probe and a competitive titration assay. At the acceptor site, the enzyme was found to accommodate any base, purine and pyrimidine, including thymidine. A method for screening analogues based on their affinity for the UMP binding site was developed. The affinities of uracil vinylphosphonate derivatives modified in the 5 position were found similar to (d)UMP and (d)CMP and improved when compared to cidofovir.
ISSN: 1525-7770
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Non-KU Leuven Association publications
× corresponding author
# (joint) last author

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