Drug Discovery based on Protein Crystallography

Abstract

Protein crystallograpy is now a central tool in the drug design process. Using this technique, we can determine atomic resolution structutres for many physiologically important proteins, both in their native state and in complex with a ligand. These data can assist both lead discovery and lead optimization, but at the current time most successful examples have involved the latter, Specific knowledge of the binding site obtained from these structures, enhances the lead optimization process by reducing the number of compounds to be tested. This paper describes the various technologies which are required to make a rational approach successful.