![]() The CRA detects receptor antagonists, agonists, inverse agonists and allosteric modulators for a given GPCR without requiring the receptor's ligand or any knowledge of the receptor's signaling pathway(s). Omeros is screening orphan and difficult-to-drug Class A and Class B GPCRs against its small-molecule chemical libraries using its proprietary, high-throughput cellular redistribution assay (CRA). The GPR17 antagonists that we are developing could lead to the first drug able to promote remyelination and restore neural function in patients with MS." There are no approved remyelinating therapeutics - all approved agents for the treatment of MS are anti-inflammatories. ![]() "GPR17 is one of those receptors, and the EAE data further underscore the potential for the compounds that we have identified with our CRA. Demopulos, M.D., chairman and chief executive officer of Omeros. "Our GPCR platform - built around our proprietary CRA - continues to unlock wholly new drug targets, and we expect that our sole knowledge of the identities of their interacting compounds together with our patent positions will give Omeros exclusive control of those receptors," stated Gregory A. In this EAE model, animals treated with GPR17-targeting compounds, compared to untreated animals, significantly improved mean clinical scores, which quantify disease progression by measuring motor dysfunction and are used as a surrogate indicator of demyelination. Myelin is a key component of the proper functioning of the central nervous system, and myelin deficiency is a hallmark of a large number of neurodegenerative autoimmune diseases, including MS. Having discovered compounds that functionally interact with GPR17, Omeros previously showed that GPR17 antagonists promote generation of mature oligodendrocytes, the cells that produce myelin. Using its proprietary high-throughput Cellular Redistribution Assay (CRA), Omeros believes that it alone has identified compounds that functionally interact with GPR17 and has patents pending that are broadly directed to any such compounds active at the receptor. Compounds previously discovered by Omeros that inhibit GPR17, an orphan G protein-coupled receptor (GPCR) unlocked by Omeros, significantly improved function from experimental autoimmune encephalomyelitis (EAE) in mice. SEATTLE, Ap/PRNewswire/ - Omeros Corporation (NASDAQ: OMER) today announced positive data in the most commonly used model for studying the clinical and pathological features of multiple sclerosis (MS), further advancing its development program of GPR17-targeting compounds for the treatment of MS.
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