I will present work from our lab for two classes of challenging targets: protein-protein interfaces and novel allosteric sites, both to activate and inhibit protein function. We use a site-directed fragment-based discovery method, called Tethering, coupled to HTS approaches that are well-suited to probing these challenging surfaces.  These approaches have led to the discovery of potent and selective compounds and some with surprising properties that will be discussed.

Drug discovery for challenging targets

248th National Meeting (2014)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.