Structural Genomics: The Ultimate Approach for Rational Drug Design

Abstract

Structural genomics can be defined as structural biology on a large number of target proteins in parallel. This approach plays an important role in modern structure-based drug design. Although a number of structural genomics initiatives have been initiated, relatively few are associated with integral membrane proteins. This indicates the difficulties in expression, purification, and crystallization of membrane proteins, which has also been confirmed by the existence of some 100 high-resolution structures of membrane proteins among the more than 30,000 entries in public databases. Paradoxically, membrane proteins represent 60-70% of current drug targets and structural knowledge could both improve and speed up the drug discovery process. In order to improve the success rate for structure resolution of membrane proteins structural genomics networks have been established.