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Looking for new pyrimidine acyclic nucleotide analogues designed for phosphorylation by human ump-cmp kinase.

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.
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https://hal-pasteur.archives-ouvertes.fr/pasteur-00202298
Contributor : Sylvie Pochet <>
Submitted on : Friday, January 4, 2008 - 6:28:36 PM
Last modification on : Wednesday, May 27, 2020 - 5:34:02 PM

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Dimitri Topalis, Hiroki Kumamoto, Julie a C Alexandre, Laurence Dugué, Sylvie Pochet, et al.. Looking for new pyrimidine acyclic nucleotide analogues designed for phosphorylation by human ump-cmp kinase.. Nucleosides, Nucleotides and Nucleic Acids, Taylor & Francis, 2007, 26 (10), pp.1369-73. ⟨10.1080/15257770701533982⟩. ⟨pasteur-00202298⟩

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