Novasite Pharmaceuticals Inc has received three Phase I Small Business Innovative Research (SBIR) awards from the National Institutes of Health (NIH) totaling $582,500. The awards consist of a grant from the National Institute for Mental Health (NIMH), a grant from the National Institute for Drug Abuse (NIDA) and a contract from the National Cancer Institute (NCI). The awards are for the crystallization of three important families of G-protein coupled receptors (GPCRs): Serotonin, Cannabinoid and EDG, respectively.
"Novasite is focused on solving the bottleneck in GPCR crystallization, which is the generation of high-quality purified receptor samples," stated Dr. Krysztof Palczewski, who led the first and only successful effort thus far to elucidate the crystal structure of a GPCR and who heads Novasite's crystallography program. Juan Ballesteros, Chief Scientific Officer of Novasite observed that, "The successful structural elucidation of these receptors may significantly increase our ability to engineer better pharmacological properties for GPCR-targeted drugs."
GPCRs are therapeutically important receptors, representing the targets of more than 40% of worldwide drug sales. The Serotonin, Cannabinoid and EDG receptors are currently prime targets for drug discovery, implicated in a wide range of indications such as oncology, autoimmune disease, psychiatric disease, pain and obesity. Until now the lack of three-dimensional crystal structures of these membrane-bound receptors has hindered discovery of drugs which are selective for specific GPCRs.