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    Compounds for binding to ERα/β and GPR30, methods of treating disease states and conditions mediated through these receptors and identification thereof
    1.
    发明授权
    Compounds for binding to ERα/β and GPR30, methods of treating disease states and conditions mediated through these receptors and identification thereof 有权
    用于结合ERα/ bgr的化合物 和GPR30，治疗通过这些受体介导的疾病状态和病症的方法及其鉴定

    公开(公告)号：US07875721B2

    公开(公告)日：2011-01-25

    申请号：US11497751

    申请日：2006-08-02

    申请人： Eric R. Prossnitz ,  Sergey E. Tkatchenko ,  Chetana M. Revankar ,  Larry A. Sklar ,  Jeffrey B. Arterburn ,  Daniel F. Cimino ,  Tudor I. Oprea ,  Cristian-George Bologa ,  Bruce S. Edwards ,  Alexander Kiselyov ,  Susan M. Young

    发明人： Eric R. Prossnitz ,  Sergey E. Tkatchenko ,  Chetana M. Revankar ,  Larry A. Sklar ,  Jeffrey B. Arterburn ,  Daniel F. Cimino ,  Tudor I. Oprea ,  Cristian-George Bologa ,  Bruce S. Edwards ,  Alexander Kiselyov ,  Susan M. Young

    IPC分类号： A61K31/435 ,  C07D221/06

    CPC分类号： C07D221/16 ,  C07D405/04 ,  C07D405/14

    摘要： 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 (ERα and ERβ). 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.

    摘要翻译： 本发明在分子生物学/药理学领域，并提供调节GPR30以及经典雌激素受体α和β（ERα和ER和bgr）的作用的化合物。 这些化合物可以作为一种或多种所公开的雌激素受体的激动剂和/或拮抗剂。 通过这些受体中的一种或多种介导的疾病包括癌症（特别是乳腺，生殖和其他激素依赖性癌症，白血病，结肠癌，前列腺癌），生殖（泌尿系）包括子宫内膜炎，前列腺炎，多囊卵巢综合征，膀胱 控制，激素相关疾病，听觉障碍，心血管疾病，包括潮热和大量出汗，高血压，中风，肥胖，骨质疏松症，血液病，血管疾病或诸如静脉血栓形成，动脉粥样硬化等疾病，以及许多其他疾病和中枢和 周围神经系统，包括抑郁症，失眠，焦虑，多发性硬化，神经病变，神经变性疾病如帕金森病和阿尔茨海默病，以及炎性肠病，克罗恩病，腹腔（腹腔）疾病和肠道相关疾病。 用于预防或减少性交后怀孕的可能性的避孕指示是本发明的另一方面。

    Glutathione beads and GST fusion proteins
    4.
    发明授权
    Glutathione beads and GST fusion proteins 有权
    谷胱甘肽和GST融合蛋白

    公开(公告)号：US07785900B1

    公开(公告)日：2010-08-31

    申请号：US11652432

    申请日：2007-01-11

    申请人： Peter C. Simons ,  Larry A. Sklar ,  Eric R. Prossnitz ,  Angela Wandinger-Ness ,  Mathewos Z. Tessema ,  John C. Reed ,  Dayong Zhai

    发明人： Peter C. Simons ,  Larry A. Sklar ,  Eric R. Prossnitz ,  Angela Wandinger-Ness ,  Mathewos Z. Tessema ,  John C. Reed ,  Dayong Zhai

    IPC分类号： G01N33/543 ,  G01N33/53

    CPC分类号： G01N33/54393 ,  G01N33/543

    摘要： The present invention relates generally to glutathione derivatized beads which are adapted for use in conjunction with glutathione-S-transferase fusion proteins (generally, GST fusion proteins, which contain a fluorescent label such as fluorescent green protein) for use in flow cytometry. The present invention also relates to methods for detecting and/or quantifying interactions between a GST fusion protein and their binding partners, in particular, labeled binding partners such as fluorescently labeled binding partners. By creating glutathione beads with an appropriate high or increased site density, disadvantages often associated with low affinity systems and quick off-rates in solution may be resolved to provide a workable system and method. Methods of identifying potential agonists, antagonists and regulator compounds of proteins fused to GST from libraries of compounds represents another aspect of the present invention.

    摘要翻译： 本发明一般涉及适用于与流式细胞术中使用的谷胱甘肽-S-转移酶融合蛋白（通常为含有荧光标记如荧光绿蛋白的GST融合蛋白）结合使用的谷胱甘肽衍生化珠粒。 本发明还涉及用于检测和/或定量GST融合蛋白与其结合配偶体，特别是标记的结合配偶体如荧光标记的结合配偶体之间的相互作用的方法。 通过产生具有适当的高或增加的位点密度的谷胱甘肽珠，可以解决通常与低亲和力系统相关的缺点和解决方案中的快速关闭速率，以提供可行的系统和方法。 从化合物文库鉴定与GST融合的蛋白质的潜在激动剂，拮抗剂和调节剂化合物的方法代表本发明的另一方面。