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International public-private partnership offers new paradigm for medicinal chemistry
Date:12/19/2008

The Wellcome Trust has announced a 4.1 million investment in a new initiative to generate small molecule inhibitors "chemical probes" for 25 proteins involved in epigenetic signalling, and to release these probes into the public domain with no restriction on use. Early stage information sharing on chemical probes is highly unusual and breaks with the tradition of keeping such data confidential.

The public-private partnership, to be led by the Structural Genomics Consortium (SGC), also involves GlaxoSmithKline (GSK), the National Institutes of Health Chemical Genomics Center (NCGC) in Bethesda, USA, and the Departments of Chemistry and Biochemistry at the University of Oxford. The initiative could offer a new model for future interactions between academia and industry.

The study of epigenetics tries to understand heritable changes in gene function that occur without a change in the DNA sequence. This signalling is thought to influence the timing, amount and type of proteins made by genes: In diseases these proteins can be altered, for instance, in tumour cells specific proteins are often present at much higher levels than in normal cells. Researchers believe that by identifying how these parameters are controlled, they can better understand the factors that lead to many common diseases, such as cancer, diabetes, obesity and Alzheimer's disease.

The SGC-led initiative aims to develop "chemical probes", small molecules that can stimulate or block the activity of a protein, specifically designed to affect the activity of proteins involved in epigenetic control. They will complement genetic knockouts and RNAi approaches to understand the role of these proteins in biology. The probes need to be highly selective for their target protein, and suitable for use in cellular settings. It is hoped that some probes may be a starting point for drug discovery.

The partnership is unique in that it brings the medicinal chemistry expertise
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Contact: Craig Brierley
c.brierley@wellcome.ac.uk
44-207-611-7329
Wellcome Trust
Source:Eurekalert

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