SAN DIEGO, Oct. 1, 2012 /PRNewswire/ -- Receptos Inc. today announced that the company is scheduled to present the Featured Presentation at the 10th Annual Discovery on Target Conference at 8:40 a.m. EDT today at the Copley Marriott Hotel in Boston. Mike Hanson, director of structural biology, will speak about the technological advancements in the field that have enabled GPCR structural biology, with an emphasis on the sphingosine 1-phosphate 1 receptor (S1P1) and adenosine a2a receptor targets.
On July 12, 2012, Receptos co-published the highest resolution GPCR structure to date (1.8 angstrom) of the adenosine a2a receptor in Science, which revealed new detail, including a previously unknown allosteric binding site. Receptos also published the determination of a high resolution S1P1 receptor in Science on February 16, 2012, which revealed an enclosed binding pocket and a potential ligand entry route through the lipid bilayer. Receptos is the exclusive licensee of the GPCR crystal structure determination technology platform from The Scripps Research Institute and, together with scientific founder Raymond Stevens, Ph.D., has an unparalleled publication record that includes the identification of 15 distinct structures of eight unique receptors over the last five years.
About the Role of S1P1 in Immune Cell Trafficking
S1P1 is a G protein-coupled receptor (GPCR) that binds the lipid signaling molecule sphingosine 1-phosphate (S1P). S1P is a circulating lipid that binds to five GPCRs termed S1P1-5. S1P1 selectively regulates physiological functions in the immune and cardiovascular systems, including immune cell trafficking and the maintenance of endothelial integrity. In autoimmune disorders, S1P1 agonism works by selectively sequestering circulating lymphocytes, blunting the underlying cause of disease. The therapeutic utility of S1P agonism has been demonstrated by the recent marketing authorization for fingolimod, indicated for the treatment of relapsing multiple sclerosis (MS). Receptos is developing RPC1063, a novel, differentiated, selective S1P1 agonist exhibiting picomolar potency that is effective in rodent models of both MS and inflammatory bowel disease (IBD), and possesses an excellent safety profile in non-clinical toxicology studies. Receptos has completed a Phase 1 clinical safety study with RPC1063 under a US IND that supports the desired differentiation profile and establishes justification for initiation of MS and IBD clinical efficacy trials in 2012.
Receptos is a biopharmaceutical company developing autoimmune therapeutic candidates through information - driven drug discovery, including GPCR structure determination. The company's lead program, RPC1063, is a best-in-class S1P1 small molecule agonist candidate for autoimmune indications. Receptos' expertise in S1P1 biology has been informed by the company's high resolution protein crystal structure of the S1P1 receptor, published in Science earlier this year. Receptos has established partnerships for its GPCR structure determination technology platform with Eli Lilly, Ono Pharmaceutical and Janssen Pharmaceuticals, Inc. For more information visit www.receptos.com.