Omeros Corporation (Nasdaq: OMER) today announced that it has identified compounds that interact selectively with two orphan G protein-coupled receptors (GPCRs) linked to pancreatic cancer (GPR182) and cognitive disorders (GPR12). Together with the three previously unlocked orphans linked to squamous cell carcinoma (GPR87), obesity (GPR85) and appetite control (GPR101), Omeros has now successfully unlocked five 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 expects to unlock a large percentage of these for drug development. Omeros also announced today that it has cloned approximately 90 percent of the 81 Class A orphan GPCRs into the vector of its proprietary cellular redistribution assay (CRA). The Company is advancing these receptors toward screening in its CRA.
"The progress in our GPCR program has been rapid and we remain on track to screen all of the Class A orphan GPCRs by mid-2012," stated Gregory A. Demopulos, M.D., chairman and chief executive officer of Omeros. "Out of the seven receptors screened against only a portion of our compound libraries, we have so far identified multiple small molecules for each of five orphans, demonstrating the power of our proprietary assay to open orphan GPCRs to drug development. We have nearly completed the preparatory steps for large-scale throughput, including generation of clones and constructs as well as integrating our automation capabilities, and we expect that we will soon reach our full screening rate."
Ongoing GPCR Program
Omeros has begun screening orphan GPCRs against its small-molecule chemical libraries using its proprietary, high-throughput CRA. Omeros has announced that it has identified and confirmed sets of compounds that interact selectively with five orphan receptors linked to squamous cell carcinoma (GPR87), pancreatic cancer (GPR182), obesity (GPR85), appetite control (GPR101) and cognitive disorders (GPR12). The CRA detects receptor antagonists and agonists. Antagonists comprise the majority of marketed drugs, and all of the compounds identified so far by Omeros are antagonists.