Protein crystallography in drug design: current bottlenecks
publication date: Sep 21, 2007
Protein crystallography is an integral component of the structure-guided drug discovery process. Rapid access to structural information about drug targets as well as bound ligands has been pivotal in accelerating lead identification and optimisation processes. While automation and robotics have been employed at every stage along the gene-to-structure path, significant challenges remain in increasing successful outcomes and in reduction of timelines. Advances in high through-put technologies to automate protein expression and crystallisation, the two weakest links in the gene-to-structure process chain, are beginning to address these issues. This article will highlight the importance of rapid structure determination of protein-ligand complexes in lead optimisation, and describe recent developments towards overcoming these bottlenecks.
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