| author(s) |
Dimitri Topalis1, Hiroki Kumamoto2, Julie A C Alexandre1, Laurence Dugué3, Sylvie Pochet3, Sabine Berteina-Raboin2, Luigi A Agrofoglio2, Dominique Deville-Bonne1 |
| laboratory |
|
| Collection(s) : |
|
| PMID |
18066785 |
| title |
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. |
| subject |
Life Sciences/Microbiology and Parasitology
|
| fulltext language |
English |
| ISSN |
1525-7770 |
|
|
| DOI |
10.1080/15257770701533982 |
| journal |
Nucleosides Nucleotides & Nucleic Acids |
| Audience |
international |
| publication date |
2007 |
| volume |
26 |
| issue |
10 |
| page, identifiant, ... |
1369-73 |
|
