In order to increase inhibitor selectivity toward a desired target kinase, the focus has turned to developing inhibitors which bind to inactive conformations or allosteric sites
Identification and Classification of Allosteric Sites
The approach has enabled the advancement of numerous "stalled" programs by identifying new protein forms and novel binding sites including competitive and allosteric sites
on enzymes and hotspots for protein-protein interactions.
This unique offering delivers novel drug discovery tools along the path to structure determination, including the generation of purified GPCR protein (to allow biophysical ligand screening and therapeutic antibody candidate generation), the identification of novel receptor binding sites such as allosteric sites
(to confer improved potency and selectivity profiles to drug candidates), and GPCR structure determination to transform drug discovery.
may offer an improved safety profile over ATP site inhibitors as well as provide a dual mode of action.
James Wells, our founder who now heads up the Small Molecule Discovery Center at UCSF, to extend the application of Tethering into new areas of drug discovery, such as the identification of novel sites and inhibitors of allosteric sites
on promising drug targets," said Daniel N.