SEATTLE, June 27, 2011 /PRNewswire/ — Omeros Corporation
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
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