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G Protein-Coupled Receptors (GPCRs)
GPCRs, which are cell surface membrane proteins involved in mediating both sensory and nonsensory functions, comprise one of the largest families of proteins in the genomes of multicellular organisms. Sensory GPCRs are involved in the perception of light, odors, taste and sexual attractants. Non-sensory GPCRs are involved in metabolism, behavior, reproduction, development, hormonal homeostasis and regulation of the central nervous system. The vast majority of GPCR drug targets are non-sensory. Although GPCRs form a super-family of receptors, individual GPCRs display a high degree of specificity and affinity for the functionally active molecules, or ligands, that bind to a given receptor. Ligands can either activate the receptor (agonists) or inhibit it (antagonists and inverse agonists). When activated by its ligand, the GPCR interacts with intracellular G proteins, resulting in a cascade of signaling events inside the cell that ultimately leads to the particular function linked to the receptor. Without a known ligand, there is no template from which medicinal chemistry efforts can be readily initiated nor a means to identify the GPCR’s signaling pathway and, therefore, drugs are very difficult to develop against orphan GPCRs. “Unlocking” these orphan GPCRs by identifying one or more of their respective ligands could lead to the development of drugs that act at these new targets.

To our knowledge, despite efforts by others in the biopharmaceutical industry and academic community, Omeros’ technology is the first commercially viable technology capable of identifying ligands of orphan GPCRs in high throughput. We have developed a proprietary cellular redistribution assay, or CRA, which we use in a high-throughput manner to identify synthetic ligands, including antagonists, agonists and inverse agonists, that bind to and affect the function of orphan GPCRs.

Omeros has announced that it has identified and confirmed sets of compounds that interact selectively with the following orphan receptors:

GPCR Metabolic & Cardiovascular Indications GPCROncology Indications
GPR12Obesity, Cognitive Impairments GPR19 Melanoma, Lung Cancer
GPR21 Obesity, Diabetes GPR20 Gastro-Intestinal Stromal Tumors, Acute Myeloid Leukemia
GPR22 Cardiovascular Diseases, Anxiety GPR65 Renal Cell Carcinoma, Ovarian Cancer, Inflammation
GPR25 Arterial Stiffness GPR68 Ovarian Cancer, Prostate Cancer, Osteoporosis
GPR37L1 Hypertension GPR80 Hepatocellular Carcinoma
GPR39 Diabetes GPR87 Squamous Cell Carcinoma
GPR45 Obesity GPR150 Ovarian Cancer
GPR50 Metabolic Disorders GPR161 Triple-Negative Breast Cancer, Sarcomas
GPR61 Eating Disorders GPR174 Regulatory T-Cell Modulation
GPR82 Appetite, Body Weight LGR4 Cancer Stem Cells, Bone Diseases
GPR101 Appetite and Eating Disorders LGR5 Cancer Stem Cells, Esophageal Adenocarcinoma
GPR132 Atherosclerosis P2Y8 Leukemias, Lymphomas
GPR146 Dyslipidemia, Diabetes  
GPR171 Eating Disorders
GPR176 Atherosclerosis
SREB1/GPR27 Diabetes, Schizophrenia
GPCRCNS Indications GPCR Miscellaneous Indications
GPR17 Myelin Disorders, Multiple Sclerosis GPR15HIV Enteropathy, Rheumatoid Arthritis
GPR31Anxiety Disorders GPR32 Acute Inflammatory Responses
GPR37 Parkinson’s Disease GPR83 Autoimmune Diseases, PTSD
GPR52Schizophrenia GPR183Osteoporosis and EBV
GPR63Autism CCRL2Rheumatoid Arthritis
GPR78Bipolar Disorder, Schizophrenia LGR6Hair Follicle Stem Cells, Wound Repair
GPR139 Motor Disorders GPCRs with Unknown Indications
GPR141 Autism
GPR135 GPR182
GPR151 Schizophrenia, Cognition
GPR153 Schizophrenia
MAS1 Cognitive Impairments
OPN4 SAD, Depression, Jet Lag, Sleep Disorders
SREB2/GPR85 Schizophrenia, Obesity
SREB3/GPR173 Schizophrenia, Obesity

In parallel, Omeros is executing on its intellectual property strategy to protect each unlocked target through a multipronged approach directed to compound structures, uniquely identified signaling pathways and associated therapeutic indications. Collectively, this approach provides Omeros the opportunity to establish broad and enforceable protection for each unlocked receptor.

We are conducting in vitro and in vivo preclinical efficacy studies and optimizing compounds for a number of targets including: GPR151, linked to schizophrenia and cognition; GPR161, which is associated with triple negative breast cancer and various sarcomas; GPR183, linked to osteoporosis and to Epstein-Barr virus infections and related diseases; GPR174, which appears to be involved in the modulation of the immune system and, in particular, increases cytokine production and inhibits production of regulatory T cells, or "T-regs," and checkpoint molecules, all of which are known to be important in autoimmune disease, such as multiple sclerosis, in cancer and in organ transplantation; and OPN4, linked to seasonal affective disorder, mood disorders, sleep disorders and photophobia.

Patent Position
As of February 16, 2018, we owned six issued patents and 14 pending patent applications in the U.S., and 54 issued patents and two pending patent applications in foreign markets, which are directed to previously unknown links between specific molecular targets in the brain and a series of CNS disorders, our cellular redistribution assay and other research tools that are used in our GPCR program and to orphan GPCRs and other GPCRs for which we have identified functionally interacting compounds using our CRA.