Structural effects on the phosphorylation of 3-substituted 1-beta-D-ribofuranosyl-1,2,4-triazoles by human adenosine kinase.

The conversion of ribavirin to the monophosphate by adenosine kinase is the rate-limiting step in activation of this broad spectrum antiviral drug. Variation of the 3-substituents in a series of bioisosteric and homologated 1-beta-D-ribofuranosyl-1,2,4-triazoles has marked effects on activity with the human adenosine kinase, and analysis of computational descriptors and binding models offers insight for the design of novel substrates.

Citation

Sidath C Kumarapperuma, Yanjie Sun, Marjan Jeselnik, Kiwon Chung, William B Parker, Colleen B Jonsson, Jeffrey B Arterburn. Structural effects on the phosphorylation of 3-substituted 1-beta-D-ribofuranosyl-1,2,4-triazoles by human adenosine kinase. Bioorganic & medicinal chemistry letters. 2007 Jun 01;17(11):3203-7

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PMID: 17379518

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