Abstract

Chemical Probes to Explore 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) and Toronto. The consortium has established a large public-private partnership involving currently nine 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 proteins targeting histone lysine demethylases and bromodomains. 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 27 probes against epigenetic targets. Recently developed probe molecules and their impact on target validation will be presented.