Researchers in the Common Fund’s Molecular Libraries and Imaging program are tackling a tough biological problem—finding potential drug candidates that target G protein-coupled receptors (GPCRs). Dr. Hugh Rosen, funded in part by the Molecular Libraries and Imaging program, is a scientific founder of Receptos, Inc., a GPCR drug discovery and development company. GPCRs are proteins found on the cell membrane that transmit signals from the outside of the cell to elicit responses inside the cell. GCPRs play many important roles in the body, including hormone signaling, cellular communication in the brain, vision, and cardiac function. Because GPCRs are crucial to many biological processes, they are also implicated in a number of different diseases. One such GPCR, called sphingosine-1-phosphate receptor 1 (S1P1), plays a role in multiple sclerosis, an inflammatory and autoimmune disease which causes damage to the protective myelin sheaths of nerve cells and to the underlying nerve fibers. The current focus of Receptos, Inc. is to conduct clinical trials for a novel compound that targets S1P1, called RPC1063, in the hopes that this potential treatment will suppress circulating immune cells to blunt the underlying cause of multiple sclerosis. The discovery of this novel compound originated from the Molecular Libraries and Imaging program. The first phase 1 clinical safety study of RPC1063 was launched in January 2011, and Phase 2 Proof of Concept studies are expected in 2012. This research has the potential to improve the treatment of multiple sclerosis, and many other diseases that involve signaling by GPCRs.

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