By a News Reporter-Staff News Editor at Diabetes Week -- Omeros Corporation (NASDAQ: OMER) announced that it has identified compounds that functionally interact with each of six additional orphan G protein-coupled receptors (GPCRs) that have been linked to a wide range of diseases in the areas of neurologic disorders, cardiovascular disease and oncology. Identification of compounds that functionally interact with orphan GPCRs facilitates the development of drugs that target those receptors. Omeros has now unlocked 52 Class A orphan GPCRs, representing approximately 65 percent of these targets (see also technology-Companies.html">Biotechnology Companies).
The six additional orphan GPCRs unlocked by Omeros are GPR37, GPR37L1, GPR132, GPR174, GPR176 and LGR5. GPR37 has been linked to Parkinson's disease. GPR37L1, GPR132 and GPR176 are associated with cardiovascular indications, specifically hypertension and cardiac hypertrophy (GPR37L1 and GPR132) and atherosclerosis (GPR176). GPR174 has been linked to melanoma and Grave's disease, while LGR5 is expressed in cancer stem cells and has been associated with esophageal adenocarcinoma.
In addition, using its proprietary Cellular Redistribution Assay (CRA) technology, which has already successfully "unlocked" 52 Class A orphan GPCRs, Omeros has identified small molecules that interact with two non-orphan Class B GPCRs; the glucagon-like peptide 1 receptor (GLP-1R) and the parathyroid hormone 1 receptor (PTH-1R). Both of these receptors are established drug targets--GLP-1R for diabetes and PTH-1R for osteoporosis. The marketed drugs currently available that target these receptors are all injectable, with 2012 annual sales of GLP-1R agents and PTH-1R agents exceeding $2.0 billion and $1.1 billion, respectively. Omeros' identification of small molecules targeting GLP-1R and PTH-1R could lead to the development of oral medications for these diseases that provide dosing advantages over the injectable agents on the market. Omeros is in the process of filing broad patent applications around its discoveries, and compound optimization efforts are in progress.
"Using our proprietary technology, we continue to add to the number of druggable Class A orphan GPCRs - now 52 and spanning a broad range of important disorders - that we believe Omeros exclusively controls," said Gregory A. Demopulos, M.D., chairman and chief executive officer of Omeros. "Our team has now also turned to Class B GPCRs, starting with two receptors that are commercially validated but whose corresponding marketed drugs are only peptides or proteins, requiring daily or weekly injections. By identifying small molecules that functionally interact with these receptors, Omeros is opening the door to new oral treatments for diabetes and bone loss."
Keywords for this news article include: Omeros Corporation, Biotechnology Companies.
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