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Omeros Unlocks Orphan GPCRs Linked to Leukemia and Sleep Disorders

Mon, 06/27/2011 - 3:33am
Bio-Medicine.Org

SEATTLE, June 27, 2011 /PRNewswire/ -- Omeros Corporation (NASDAQ: OMER) today reported that it has identified compounds that interact with orphan G protein-coupled receptors (GPCRs) P2Y8 and OPN4. P2Y8 (also known as P2RY8) is associated with acute lymphoblastic leukemia (ALL), an aggressive cancer of the white blood cells. ALL is the most common type of malignancy diagnosed in children. The OPN4 receptor is involved with regulation of circadian rhythms, and could provide a target for drugs to improve alertness and to treat a wide range of sleep disorders ranging from narcolepsy and jet lag to insomnia.

Omeros has now announced that it has unlocked 10 of the 81 Class A orphan GPCRs. GPCRs represent the premier family of drug targets, with more than 30 percent of currently marketed drugs targeting only 46 GPCRs. There are approximately 120 orphan GPCRs, and Omeros, which expects to unlock a large percentage of these for drug development, is initially targeting Class A orphan GPCRs.

"The P2Y8 and OPN4 receptors are linked to important therapeutic areas that receive significant industry attention," said Gregory A. Demopulos, M.D., chairman and chief executive officer of Omeros. "By identifying compounds that interact with these two orphan receptors, our proprietary screening technology has opened previously closed drug-development pathways for ALL and sleep disorders."

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 10 orphan receptors linked to squamous cell carcinoma (GPR87), pancreatic cancer (GPR182),acute lymphoblastic leukemia (P2Y8/P2RY8), metabolic and psychotic disorders(GPR27, GPR85, GPR173), appetite c

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