Stc.unm

University of Michigan

Daniel F Cimino

Larry A Sklar

Eric R Prossnitz

Bruce S Edwards

Tudor Oprea

Peter C Simons

Jeffrey Arterburn

Susan M Young

Cristian-George Bologa

Chetana M Revankar

Sergey E Tkatchenko

Alexander Kiselyov

Tione Buranda

Anna Waller

Alexandor Kiselyov

Sean Biggs

Alex T Key

Mei Shi

The current invention is in the field of molecular biology/pharmacology and provides compounds which modulate the effects of GPR30 as well as the classical estrogen receptors alpha and beta (ER&#x3b1; and ER&#x3b2;). These compounds may function as agonists and/or antagonists of one or more of the disclosed estrogen receptors. Diseases which are mediated through one or more of these receptors include cancer (particularly breast, reproductive and other hormone-dependent cancers, leukemia, colon cancer, prostate cancer), reproductive (genito-urological) including endometreitis, prostatitis, polycystic ovarian syndrome, bladder control, hormone-related disorders, hearing disorders, cardiovascular conditions including hot flashes and profuse sweating, hypertension, stroke, obesity, osteoporosis, hematologic diseases, vascular diseases or conditions such as venous thrombosis, atherosclerosis, among numerous others and disorders of the central and peripheral nervous system, including depression, insomnia, anxiety, multiple sclerosis, neuropathy, neurodegenerative disoders such as Parkinson's disease and Alzheimer's disease, as well as inflammatory bowel disease, Crohn's disease, coeliac (celiac) disease and related disorders of the intestine. A contraceptive indication to prevent or reduce the likelihood of pregnancy after intercourse is a further aspect of the present invention.

Compounds for binding to ER alpha/beta and GPR30, methods of treating disease states and conditions mediated through these receptors and identification thereof

The current invention is in the field of molecular biology/pharmacology and provides compounds which modulate the effects of GPR30 as well as the classical estrogen receptors alpha and beta (ER&#x3b1; and ER&#x3b2;). These compounds may function as agonists and/or antagonists of one or more of the disclosed estrogen receptors. Diseases which are mediated through one or more of these receptors include cancer (particularly breast, reproductive and other hormone-dependent cancers, leukemia, colon cancer, prostate cancer), reproductive (genito-urological) including endometritis, prostatitis, polycystic ovarian syndrome, bladder control, hormone-related disorders, hearing disorders, cardiovascular conditions including hot flashes and profuse sweating, hypertension, stroke, obesity, osteoporosis, hematologic diseases, vascular diseases or conditions such as venous thrombosis, atherosclerosis, among numerous others and disorders of the central and peripheral nervous system, including depression, insomnia, anxiety, multiple sclerosis, neuropathy, neurodegenerative disorders such as Parkinson's disease and Alzheimer's disease, as well as inflammatory bowel disease, Crohn's disease, coeliac (celiac) disease and related disorders of the intestine. A contraceptive indication to prevent or reduce the likelihood of pregnancy after intercourse is a further aspect of the present invention.

Compounds for binding to ER&#x3b1;/&#x3b2; and GPR30, methods of treating disease states and conditions mediated through these receptors and identification thereof

The present invention relates generally to molecular assemblies, more particularly to an assay for the detection of G-protein coupled receptor (GPCR) molecular assemblies and bead-based detection of ligand-GPCR complexes and to methods for identifying compounds as agonists, partial agonists or antagonists of the binding of G-protein coupled receptors to G-protein and for use of these compounds in the treatment of conditions or disease states in a mammalian subject or patient, including humans, where G-protein coupled receptor binding to G-protein is implicated.

Multiplex analysis for high throughput discrimination of GPCR agonists and antagonists

The present invention provides a general approach for G protein coupled receptors that may be used to define agonists and antagonists, and the specificity of receptor coupling to G protein subunits. Methods of the present invention use small volumes (microliters) and are compatible with high throughput flow cytometry. When assays of the present invention are multiplexed, the specificity of the interactions of a receptor with many G proteins may be determined simultaneously.

Bead-based detection of ligand-GPCR-G protein complexes

Growing community of inventors

Tijeras, NM, United States of America

Daniel F Cimino