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Welcome Chemical Genetics and Genomics: What are they and are they helping drug discovery? 10 th March 2005 Organisers: Dr Robert Williams, Head of Preclinical Development, Cancer Research UK and Dr Katherine Brown, Imperial College London The stated goal of chemical genetics as articulated by its pioneer Stuart Schreiber is ‘to find a small-molecule modulator for each individual function of all proteins.' Such tools could be used to probe gene function in a manner somewhat analogous to the classical genetics strategy of mutagenesis. To those in the drug discovery community, the aforementioned statement is in itself enough to provoke vigorous debate. The field of chemical genetics has however broadened significantly and the terms ‘chemical genomics' and ‘chemical proteomics' have emerged. These terms are often used interchangeably and have become a ‘catch-all' category for approaches that aim to unravel biology by interrogating proteins, genes, cells or organisms with small organic molecules. At the core of this lie two, clearly distinguishable approaches, namely forward and reverse. Put simply, in the forward approach compounds are identified on the basis of activity in cell-based systems or organisms followed by molecular target identification. Popular readouts include changes in gene expression profiles, which may be linked to molecular pathology. The reverse approach, which has been more prevalent in recent years, involves screening compound libraries against isolated, structurally characterised proteins, using increasingly sophisticated ‘smart' libraries. The SMR symposium to be held on 10 th March 2005 brings together proponents of forward and reverse approaches and highlights technological developments in a field the Boston Consulting Group have reported may save $200 million in development costs per drug. A thought provoking day of scientific debate is assured.
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