Abstract

Chemical Probes for Epigenetic Targets

Susanne Muller Knapp, Group Head Structural Genomics Consortium (SGC), University Of Oxford

The SGC (Structural Genomics Consortium) is an academic charity with laboratories in Oxford (UK), Toronto (Canada) and Campinas (Brazil). The consortium encompasses a large public-private partnership involving currently ten pharmaceutical companies. We have established a chemical biology platform for the development of cell active, highly specific and potent chemical tool compounds ‘chemical probes’ for epigenetic targets. Our probe molecules have enabled new biology and have led to new therapeutic indications as the first inhibitors are entering clinical trials. In keeping with SGC policy, structure, biochemical and cellular data associated with each probe are promptly made available and the characterized probe molecules are distributed to academic and industrial laboratories without constrains. Currently the consortium has developed more than 30 probes against epigenetic targets. Data obtained by these probes complement findings obtained by more traditional methods and provide a better route for target validation. Recently developed probe molecules and their potential applications in drug discovery as well as lessons learned will be presented.