专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

WO2008122041A2 BIASED LIGANDS FOR RECEPTORS SUCH AS THE PTH RECEPTOR 审中-公开
标题翻译：用于受体如PTH受体的偏倚配体
公开(公告)号：WO2008122041A2
公开(公告)日：2008-10-09
申请号：PCT/US2008/059143
申请日：2008-04-02
申请人： MUSC FOUNDATION FOR RESEARCH DEVELOPMENT , DUKE UNIVERSITY & DUKE UNIVERSITY HEALTH SYSTEMS , LUTTRELL, Louis, M. , LEFKOWITZ, Robert, J. , GESTY-PALMER, Diane
发明人： LUTTRELL, Louis, M. , LEFKOWITZ, Robert, J. , GESTY-PALMER, Diane
IPC分类号： A61K38/17
CPC分类号： A61K38/29 , G01N33/74 , G01N2333/635 , G01N2333/726 , G01N2500/02 , G01N2800/108
摘要： Disclosed are compositions and methods for modulating the β-arrestin pathway selectively over the G protein pathway of a G protein couple receptor, such as parathryroid hormone receptor.
摘要翻译：公开了用于在G蛋白偶联受体（例如parathryroid激素受体）的G蛋白途径上选择性调节β-抑制蛋白途径的组合物和方法。

2. 发明申请

WO2004004451A1 METHODS OF SCREENING COMPOUNDS FOR GRK6 MODULATING ACTIVITY 审中-公开
标题翻译：筛选GRK6调节活性化合物的方法
公开(公告)号：WO2004004451A1
公开(公告)日：2004-01-15
申请号：PCT/US2003/020838
申请日：2003-07-03
申请人： DUKE UNIVERSITY , CARON, Marc, G. , GAINETDINOV, Raul, R. , LEFKOWITZ, Robert, J. , PREMONT, Richard, T.
发明人： CARON, Marc, G. , GAINETDINOV, Raul, R. , LEFKOWITZ, Robert, J. , PREMONT, Richard, T.
IPC分类号： A01K67/00
CPC分类号： G01N33/5091 , A01K67/0276 , A01K2217/075 , A01K2227/105 , A01K2267/03 , C07K14/70571 , C12N9/1205 , C12N15/8509 , C12N2800/30 , G01N33/5008 , G01N33/5041 , G01N33/5088 , G01N33/74 , G01N2333/726 , G01N2500/04
摘要： The present invention relates to methods of treating disease by altering G protein coupled receptor kinase (GRK) 6. This may be done by altering the expression or activity of the protein, for example. The present invention may be used for disease diagnosis, by detecting the expression or activity of GRK6. The present invention relates to a GRK6 deficient mouse, GRK6 splice variants, and methods of use. The present invention also relates to methods of identifying compounds that alter GRK6 activity. The present invention relates to disease treatment by altering GRK6 expression or activity.
摘要翻译：本发明涉及通过改变G蛋白偶联受体激酶（GRK）6来治疗疾病的方法。这可以通过例如改变蛋白质的表达或活性来进行。通过检测GRK6的表达或活性，可以将本发明用于疾病诊断。本发明涉及GRK6缺陷小鼠，GRK6剪接变体和使用方法。本发明还涉及鉴定改变GRK6活性的化合物的方法。本发明涉及通过改变GRK6表达或活性的疾病治疗。

3. 发明申请

WO1998014197A1 METHOD OF INHIBITING SMOOTH MUSCLE CELL PROLIFERATION 审中-公开
标题翻译：抑制SMOOTH肌肉细胞增殖的方法
公开(公告)号：WO1998014197A1
公开(公告)日：1998-04-09
申请号：PCT/US1997017526
申请日：1997-10-03
申请人： DUKE UNIVERSITY
发明人： DUKE UNIVERSITY , KOCH, Walter, J. , LEFKOWITZ, Robert, J. , HAGEN, Per-Otto
IPC分类号： A61K31/70
CPC分类号： C12N9/1205 , A61K31/70 , A61K38/45 , A61K48/00 , C12N2799/022
摘要： The present invention relates, in general, to vascular smooth muscle proliferation and, in particular, to a method of inhibiting arterial and venous smooth muscle proliferation resulting, for example, from arterial injury or vein grafting. The invention also relates to an expression construct encoding a G beta gamma inhibitor suitable for use in such a method.
摘要翻译：本发明一般涉及血管平滑肌增生，特别涉及抑制动脉和静脉平滑肌增生的方法，其导致例如动脉损伤或静脉移植。本发明还涉及编码适用于这种方法的Gβγ抑制剂的表达构建体。

4. 发明申请

WO2017095830A1 METHODS OF TREATING FRAGILE X SYNDROME AND RELATED DISORDERS 审中-公开
标题翻译：治疗脆性X综合征和相关疾病的方法
公开(公告)号：WO2017095830A1
公开(公告)日：2017-06-08
申请号：PCT/US2016/064049
申请日：2016-11-30
申请人： MASSACHUSETTS INSTITUTE OF TECHNOLOGY , DUKE UNIVERSITY
发明人： AUERBACH, Benjamin, David , BEAR, Mark, Firman , STOPPEL, Laura, Jane , LEFKOWITZ, Robert, J.
IPC分类号： A61K38/29 , A61P19/00
CPC分类号： A61K38/465 , A61K48/00 , C12N15/113 , C12N15/1138 , C12N15/115 , C12N2310/10 , C12N2310/11 , C12N2310/12 , C12N2310/14 , C12N2310/16 , C12N2310/3231 , C12N2310/3233 , C12N2310/531
摘要： Disclosed herein are novel methodologies of treating fragile X syndrome and related disorders by inhibiting mGlu 5 -relevant signaling pathways via the reduction of β-arrestin2 protein levels or the diminution of mGlu 5 and β-arrestin2 protein interactions.
摘要翻译：本文公开了通过减少β-arrestin2蛋白水平或减少mGlu通过抑制mGlu5相关信号通路来治疗脆性X综合征和相关病症的新方法 5和β-arrestin2蛋白相互作用。

5. 发明申请

WO1992005244A1 EXPRESSION OF G PROTEIN COUPLED RECEPTORS IN YEAST 审中-公开
标题翻译：表达G蛋白偶联受体在YEAST
公开(公告)号：WO1992005244A1
公开(公告)日：1992-04-02
申请号：PCT/US1991006605
申请日：1991-09-12
申请人： DUKE UNIVERSITY
发明人： DUKE UNIVERSITY , KING, Klim , DOHLMAN, Henrik, G. , CARON, Marc, G. , LEFKOWITZ, Robert, J.
IPC分类号： C12N01/20
CPC分类号： G01N33/566 , C07K14/39 , C07K14/4722 , C07K14/70571 , C07K2319/00 , C07K2319/02 , C07K2319/32 , C07K2319/61 , C07K2319/705 , C12N15/81 , C12Q1/6897 , G01N2333/726 , G01N2500/00
摘要： Disclosed is a transformed yeast cell containing a first heterologous DNA sequence which codes for a mammalian G protein coupled receptor and a second heterologous DNA sequence which codes for a mammalian G protein alpha subunit (mammalian G alpha ). The first and second heterologous DNA sequences are capable of expression in the cell, but the cell is incapable of expressing an endogenous G protein alpha -subnit (yeast G alpha ). The cells are useful for screening compounds which affect the rate of dissociation of G alpha from G beta gamma in a cell. Also disclosed is a novel DNA expression vector useful for making cells as described above. The vector contains a first segment comprising at least a fragment of the extreme amino-terminal coding sequence of a yeast G protein coupled receptor. A second segment is positioned downstream from the first segment (and in correct reading frame therewith), with the second segment comprising a DNA sequence encoding a heterologous G protein coupled receptor.
摘要翻译：公开了含有编码哺乳动物G蛋白偶联受体的第一异源DNA序列和编码哺乳动物G蛋白α亚基（哺乳动物Gα）的第二异源DNA序列的转化酵母细胞。第一和第二异源DNA序列能够在细胞中表达，但是细胞不能表达内源性G蛋白α-亚基（酵母Gα）。细胞可用于筛选影响细胞中Gα从Gβγ解离速率的化合物。还公开了用于如上所述制备细胞的新型DNA表达载体。载体含有至少包含酵母G蛋白偶联受体的极端氨基末端编码序列的片段的第一片段。第二片段位于第一片段的下游（并且在其正确的阅读框架中），其中第二片段包含编码异源G蛋白偶联受体的DNA序列。

6. 发明申请

WO2019157144A1 SYSTEM AND METHOD FOR HOMOGENOUS GPCR PHOSPHORYLATION AND IDENTIFICATION OF BETA-2 ADRENERGIC RECEPTOR POSITIVE ALLOSTERIC MODULATORS 审中-公开
公开(公告)号：WO2019157144A1
公开(公告)日：2019-08-15
申请号：PCT/US2019/016999
申请日：2019-02-07
申请人： DUKE UNIVERSITY
发明人： LEFKOWITZ, Robert, J. , AHN, Seungkirl , PANI, Biswaranjan , KAHSAI, Alem, W. , WINGLER, Laura , STAUS, Dean
IPC分类号： A61K31/7088 , A61K38/17 , A61K38/43 , A61K48/00
摘要： The disclosure is directed to a G-protein coupled receptor complex. The complex includes (i) a chimeric G protein-coupled receptor (GPCR) comprising a non-native amino acid sequence located within the C-terminus of the GPCR and a synthetic phosphopeptide ligated to the non- native amino acid sequence; and (ii) a β-arrestin (βarr) protein bound to the C-terminus of the GPCR. The disclosure also provides an in vitro method for producing the aforementioned complex, as well as methods for identifying compounds or ligands which bind to and modulate the activity of the complex. Positive allosteric modulators of the β2 adrenergic receptor identified by screening a DNA-encoded library potentiate the activity of β2 agonists and have application in the treatment of obstructive airway disease, bronchospasm, or pre-term labor.

7. 发明申请

WO2009155283A2 RADIOLABLED CYCLOPAMINE ASSAY FOR THE SMOOTHENED RECEPTOR 审中-公开
标题翻译：放射性CYPOPAMINE测定用于平滑受体
公开(公告)号：WO2009155283A2
公开(公告)日：2009-12-23
申请号：PCT/US2009/047497
申请日：2009-06-16
申请人： DUKE UNIVERSITY , CHEN, Wei , BARAK, Lawrence, S. , JIANGBO, Wang , LEFKOWITZ, Robert, J. , LEYRLY, Herbert, Kim
发明人： CHEN, Wei , BARAK, Lawrence, S. , JIANGBO, Wang , LEFKOWITZ, Robert, J. , LEYRLY, Herbert, Kim
CPC分类号： G01N33/566 , G01N33/60 , G01N2500/04
摘要： The present invention discloses novel methods for screening compositions for both agonist and antagonist activity on the smoothened receptor. The assay tests ligands on the activity of the receptor using a cyclopamine binding and ultra high receptor expression.
摘要翻译：本发明公开了筛选对平滑化受体的激动剂和拮抗剂活性的组合物的新方法。该测定使用环巴胺结合和超高受体表达测试配体对受体活性。

8. 发明申请

WO2004039313A2 PREVENTING DESENSITIZATION OF RECEPTORS 审中-公开
标题翻译：预防受体的缺失
公开(公告)号：WO2004039313A2
公开(公告)日：2004-05-13
申请号：PCT/US2003/029134
申请日：2003-10-20
申请人： DUKE UNIVERSITY
发明人： STAMLER, Jonathan, S. , LEFKOWITZ, Robert, J. , WHALEN, Erin, j. , KOCH, Walter, J. , PIANTADOSI, Claude, A.
IPC分类号： A61K
CPC分类号： A61K31/21 , A61K31/19 , A61K31/223 , A61K31/5377 , A61K38/063
摘要： Desensitization of receptors that control disease is prevented by inhibiting G-protein receptor kinases. This has applicability, e.g., for patients with heart failure or on a left ventricular heart device or a heart pump after surgery or about to undergo surgery and at high risk for a cardiac event or on an opiate or addicted to opiate or with cystic fibrosis or rheumatoid arthritis.
摘要翻译：通过抑制G蛋白受体激酶来防止控制疾病的受体的脱敏。这适用于例如心脏衰竭患者或左心室心脏装置或手术后心脏泵或即将接受手术并且处于心脏事件高风险或鸦片制剂上或患有阿片制剂或囊性纤维化或类风湿关节炎。

9. 发明申请

WO2009151542A2 NICOTINIC ACID RECEPTOR LIGANDS 审中-公开
公开(公告)号：WO2009151542A2
公开(公告)日：2009-12-17
申请号：PCT/US2009/003218
申请日：2009-05-27
申请人： DUKE UNIVERSITY , LEFKOWITZ, Robert, J. , DEWIRE, Scott, M. , WHALEN, Erin, J. , VIOLIN, Jonathan, D. , WALTERS, Robert, W.
发明人： LEFKOWITZ, Robert, J. , DEWIRE, Scott, M. , WHALEN, Erin, J. , VIOLIN, Jonathan, D. , WALTERS, Robert, W.
IPC分类号： G01N33/68 , C07K14/705
CPC分类号： G01N33/566 , C07K14/705 , G01N2333/726 , G01N2800/044
摘要： The present invention relates, in general, to nicotinic acid receptor ligands and, in particular, to ligands that have a relative efficacy for activating a G- protein-coupled receptor function (e.g., signaling) that is greater than their relative efficacy for stimulating β-arrestin function (e.g., recruitment and/or signaling). The invention further relates to the use of such "biased ligands" to decrease triglycerides levels and to potentially increase high density lipoprotein (HDL) levels in patients and potentially lower low density lipoprotein (LDL) and/or very low density lipoprotein (VLDL) levels. In addition, the invention relates to methods of identifying such "biased ligands".
摘要翻译：本发明一般涉及烟酸受体配体，尤其涉及具有激活G-蛋白偶联受体功能（例如，信号传导）的相对功效的配体，其大于其刺激ß的相对功效 -arrestin功能（例如招聘和/或信令）。本发明还涉及这种“有偏配体”降低甘油三酯水平并潜在地增加患者中高密度脂蛋白（HDL）水平以及潜在地降低低密度脂蛋白（LDL）和/或极低密度脂蛋白（VLDL）水平的用途。此外，本发明涉及鉴定这种“有偏配体”的方法。

10. 发明申请

WO2008103393A1 PROTEIN TRAFFICKING 审中-公开
标题翻译：蛋白质运输
公开(公告)号：WO2008103393A1
公开(公告)日：2008-08-28
申请号：PCT/US2008/002257
申请日：2008-02-21
申请人： DUKE UNIVERSITY , LEFKOWITZ, Robert, J. , VIOLIN, Jonathan, D.
发明人： LEFKOWITZ, Robert, J. , VIOLIN, Jonathan, D.
IPC分类号： G01N33/53 , G01N33/567 , C12N5/00 , C12N5/02
CPC分类号： G01N33/6803 , G01N2333/726
摘要： The present invention relates, in general, to protein trafficking, and, in particular, to a method of measuring protein trafficking to and from a plasma membrane.
摘要翻译：本发明一般涉及蛋白质的运输，尤其涉及一种测定向质膜和从质膜传送蛋白质的方法。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式