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Receptos Scientists Publish Determination of a High Resolution Sphingosine 1-Phosphate Receptor 1 Structure in Science

SAN DIEGO, Feb. 16, 2012 /PRNewswire/ -- Receptos Inc. announced today the publication of key results relating to its expertise in S1P1 biology and structure-based drug discovery for high-value G-protein-coupled receptor (GPCR) targets in Science.

The article, entitled "Crystal Structure of a Lipid G Protein-Coupled Receptor," was co-authored by Receptos in collaboration with scientific founders Hugh Rosen, M.D., Ph.D., and Raymond Stevens, Ph.D. Drs. Rosen and Stevens are both professors at The Scripps Research Institute®, with expertise in immunology and lymphocyte trafficking and GPCR crystallography, respectively. Receptos is the exclusive licensee of the GPCR crystal structure determination technology platform, developed at The Scripps Research Institute®, which enabled the elucidation of the S1P1 receptor structure.

"Receptos and its founders have an unparalleled track record in the determination of high resolution GPCR structures to enable rational drug design," said Faheem Hasnain, President and Chief Executive Officer of Receptos. "The publication of the S1P1 structure in Science highlights the importance of this therapeutic target and Receptos's leading position in decoding receptor-ligand interactions for pharmaceutically relevant GPCR targets. Our expertise in the S1P1 field has resulted in the discovery of a best-in-class small molecule agonist, RPC1063, which is scheduled to initiate Phase 2 clinical studies in multiple sclerosis and inflammatory bowel disease later this year."

Receptos utilizes the GPCR crystal structure determination technology platform to assist in building a pipeline of high-value therapeutic candidates. In addition to RPC1063, the technology supports a small molecule glucagon-like peptide 1 (GLP1) research program, which has demonstrated proof of concept in in vivo models of type 2 diabetes. Receptos has also initiated technology collaborations to conduct novel drug screening assays and study dynamic conformational changes to receptor topography that allow rational drug design for high-value GPCR targets. These collaborators include Eli Lilly, Ono Pharmaceutical and Janssen Pharmaceuticals.

Advancements in the technology, as well as in proprietary drug discovery and development programs at Receptos, have resulted in a patent estate comprising twelve patent applications, seven of which are directed to small molecule composition of matter and four of which support the technology platform, including novel reagents to enable crystallography. The Receptos scientific management team has broad experience in the development and registration of therapeutics including rituximab, targretin, panretin, belatacept, abatacept, omalizumab, and others.

About the S1P1 Target and Utilization of the S1P1 Structure

The lyso-phospholipid sphingosine 1-phosphate modulates lymphocyte trafficking, endothelial development and integrity, heart rate, and vascular tone and maturation by activating G protein–coupled sphingosine 1-phosphate receptors. Activation of the S1P1 receptor through exogenous ligands, both physiological and pharmacological, results in significant inhibition of lymphocyte re-circulation. This physiological effect was leveraged in the development of the nonselective S1P receptor agonist prodrug fingolimod (GILENYA®), approved in 2010 for the clinical treatment of relapsing-remitting multiple sclerosis. The high resolution crystal structure of the sphingosine 1-phosphate receptor 1 has revealed the architecture of the ligand binding pocket and extracellular region providing insights into the molecular interactions associated with binding and signaling of diverse S1P ligands. In combination with mutagenesis and signaling studies, Receptos has pinpointed regions in the binding pocket responsible for driving interactions within S1P ligand classes, and prioritized drug candidates accordingly.

About GPCR Protein Crystal Structure Determination Technology

GPCR receptors are the largest single drug discovery protein family, yet many high-value targets have been intractable to traditional drug discovery techniques. Receptos offers a paradigm-shifting technology that enables, for the first time, structure-based drug design for this important target class. 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. Receptos's proprietary technology platform was exclusively licensed from The Scripps Research Institute® and has been further advanced by the company into the disciplines of drug discovery and development.

About Receptos

Receptos is a biopharmaceutical company developing autoimmune therapeutic candidates through information-driven drug discovery, including GPCR structure determination. The company's lead program is a best-in-class S1P1 small molecule agonist candidate for autoimmune indications, including multiple sclerosis and inflammatory bowel disease, which will complete a Phase 1 clinical study in the first quarter of 2012. The S1P1 program is supported by the company's proprietary high resolution protein crystal structure of the S1P1 receptor. Receptos has established partnerships for its GPCR structure determination technology platform with Eli Lilly, Ono Pharmaceutical and Janssen Pharmaceuticals, Inc. For more information visit

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