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Omeros Announces it has Unlocked 30 Percent of Class A Orphan GPCRs
Date:1/10/2012

le 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 23 orphan receptors linked to metastatic melanoma (GPR19), esophageal squamous cell carcinoma and obesity-related type-2 diabetes (GPR39), hepatocellular carcinoma (GPR80), squamous cell carcinoma (GPR87), pancreatic cancer (GPR182), acute lymphoblastic leukemia (P2Y8/P2RY8), arterial stiffness (GPR25), sleep disorders (OPN4), cognitive disorders (GPR12), anxiety disorders (GPR31), bipolar disorder and schizophrenia (GPR78), psychotic and metabolic disorders (GPR27, GPR85, GPR173), cognitive impairments (MAS1), inflammatory responses (GPR32), 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). In addition, Omeros has unlocked GPR 20 and GPR135, which have not yet been tied to any indications but are expressed preferentially in the gastrointestinal tract and brain, respectively. 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® (s
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