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Phosphorylation of Anti-HIV Nucleoside Analogs by Nucleoside Diphosphate Kinase |
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| Authors: | Benoit Schneider Yingwu Xu Olivier Sellam Robert Sarfati Joel Janin Michel Véron |
| Affiliation: | 1. Unité de Régulation Enzymatique des Activités Cellulaires, CNRS URA 1773 , Institut Pasteur , Paris, France;2. Laboratoire d'Enzymologie et de Biochimie Structurales , CNRS UPR 9063, 91198, Gif-sur-Yvette, France;3. Unité de Chimie Organique , Institut Pasteur , Paris, France |
| Abstract: | Abstract The reaction of NDP kinase with antiviral nucleoside triphosphates used in antiviral therapies was studied at the presteady state by fluorescence stopped-flow and compared with the steady-state parameters. The affinity of the analogs was determined by fluorescence titration of a mutated enzyme with an inserted Trp in the binding site. The lack of the 3′ hydroxyl in analogs is shown to decrease the kcat more than the KD. |
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