Molecular basis of prodrug activation by human valacyclovirase, an alpha-amino acid ester hydrolase.

Abstract excerpt

Chemical modification to improve biopharmaceutical properties, especially oral absorption and bioavailability, is a common strategy employed by pharmaceutical chemists. The approach often employs a simple structural modification and utilizes ubiquitous endogenous esterases as activation enzymes, although such enzymes are often unidentified. This report describes the crystal structure and specificity of a novel...

Topics

• Acyclovir
• Animals
• Antiviral Agents
• Binding Sites
• Carboxylic Ester Hydrolases
• Crystallography, X-Ray
• Ganciclovir
• Humans
• Hydrophobic and Hydrophilic Interactions
• Mutation
• Phylogeny