Stc.unm

Bio-tech Imaging, Inc.

Susan M Young

Larry A Sklar

Bruce S Edwards

Eric R Prossnitz

Tudor Oprea

Jeffrey Arterburn

Daniel F Cimino

Cristian-George Bologa

Chetana M Revankar

Sergey E Tkatchenko

Alexander Kiselyov

Robert A Hallowitz

Chester F King

Alexandor Kiselyov

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 to cells which have improved receptivity to viruses which are capable of infecting them. Receptivity to such viruses is improved by selecting cells from a population which express the receptor(s) that enable a virus to attach to the cell and gain entry into it. Any combination of viruses and host cell lines can be used. In a preferred embodiment, the present invention relates to improving receptivity or infectivity of a cell line which can be infected with an immunodeficiency virus, such as HIV-1. Especially preferred embodiments of the invention relate to methods of improving (or assaying for) the infectivity for HIV-1 in a HIV-1 receptive cell line, preferably a continuous cell line transformed with DNAs coding for expressible CD4 and expressible HIV-1 coreceptor, comprising, in any effective order, a) isolating the cells expressing CD4 and an HIV-1 coreceptor on their cell surface; b) contacting the isolated cells with HIV-1 under conditions effective for the HIV-1 to infect the cells; and c) detecting the number of cells infected with HIV-1, thereby assaying for infectivity of HIV-1. This method facilitates the measurement of true infectivity and infectivity reduction values by quantifying the percentage of infected cells in the population of specific cells capable of being infected by virus, rather than in a population of mixed cells, only some which are capable of being infected.

Methods of improving infectivity of cells for viruses

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Albuquerque, NM, United States of America

Susan M Young