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Omeros Announces It Has Unlocked Over 20 Percent of Class A Orphan GPCRs
Date:11/30/2011

ollectively, this approach provides us the opportunity to establish broad and enforceable protection for each receptor that we unlock."

Ongoing GPCR Program

Omeros has begun screening orphan GPCRs against its small-molecule chemical libraries using its proprietary, high-throughput cellular redistribution assay (CRA).  Omeros has announced that it has identified and confirmed sets of compounds that interact selectively with 18 orphan receptors linked to metastatic melanoma (GPR19), esophageal squamous cell carcinoma and obesity-related type-2 diabetes (GPR39), squamous cell carcinoma (GPR87), pancreatic cancer (GPR182), acute lymphoblastic leukemia (P2Y8/P2RY8), sleep disorders (OPN4), cognitive disorders (GPR12), anxiety disorders (GPR31), bipolar disorder and schizophrenia (GPR78), psychotic and metabolic disorders (GPR27, GPR85, GPR173), gastrointestinal disorders (GPR20), appetite control (GPR101), rheumatoid arthritis and HIV-mediated enteropathy (GPR15), respiratory and immune disorders (GPR141), motor control (GPR139) and congenital cataracts and birth defects of the brain and spinal cord (GPR161).  The CRA detects receptor antagonists and agonists.  Antagonists comprise the majority of marketed drugs, and all of the compounds characterized so far by Omeros are antagonists.

About G Protein-Coupled Receptors

GPCRs, which mediate key physiological processes in the body, are one of the most valuable families of drug targets.  According to Insight Pharma Reports, GPCR-targeting drugs represent 30 to 40 percent of marketed pharmaceuticals.  Examples include Claritin® (allergy), Zantac® (ulcers and reflux), OxyContin® (pain), Lopressor® (high blood pressure), Imitrex® (migraine headache), Reglan® (nausea) and Abilify® (schizophrenia, bipolar disease and depression) as well as all other antihistamines, opioids, alpha and beta blockers, serotonergics and dopaminergic
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SOURCE Omeros Corporation
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