Senior Vice President RAPT Therapeutics South San Francisco , California
The deubiquitinase USP7 is a key regulator of oncogenic driver proteins. We discovered a series of structurally novel USP7 inhibitors that exhibited good selectivity across a panel of other DUBs . Insights gained from x-ray crystal structures, enhanced with advanced computational chemistry facilitated the discovery of highly potent USP7 inhibitors. These studies suggested changes that could be made to the structure which both maintained potency and had improved oral exposure. This has led to compounds that show promising activity in anti-tumor models.
ways in wUpon completion, participant will be able to understand the role that USP7 plays in controlling ongenic drivers.
Upon completion, participant will be able to understand the potential of USP7 inhibitors in difficult to treat cancers.
Upo completion, particiapnts will be mad aware of computational methods that can be used toeffectively leverage X-Ray structures to design compounds with good inhibitory potency and good PK properties.