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1. 发明申请

WO2008021552A9 BIASED LIGANDS AND METHODS OF IDENTIFYING SAME 审中-公开
标题翻译：偏心配偶和识别方法
公开(公告)号：WO2008021552A9
公开(公告)日：2008-05-29
申请号：PCT/US2007018394
申请日：2007-08-20
申请人： UNIV DUKE , LEFKOWITZ ROBERT J , RAJAGOPAL KESHAVA , WHALEN ERIN J , DRAKE MATTHEW T , VIOLIN JONATHAN D , ROCKMAN HOWARD A , DEWIRE SCOTT M
发明人： LEFKOWITZ ROBERT J , RAJAGOPAL KESHAVA , WHALEN ERIN J , DRAKE MATTHEW T , VIOLIN JONATHAN D , ROCKMAN HOWARD A , DEWIRE SCOTT M
IPC分类号： G01N33/53
CPC分类号： G01N33/74 , G01N2333/726
摘要： The present invention relates to G protein-coupled receptor ligands having a relative efficacy for stimulating ß-arrestin/G protein-coupled receptor kinase (GRK) function (e.g., signaling) that is greater than their relative efficacy for stimulating G-protein signaling function. These "ß-arrestin/GRK biased ligands" can act as agonists or antagonists of G protein-mediated signaling and agonists of ß-arrestin/GRK-mediated signal transduction. The invention further relates to methods of identifying such ligands and to methods of using same in a variety of therapeutic settings.
摘要翻译：本发明涉及具有刺激ß-抑制蛋白/ G蛋白偶联受体激酶（GRK）功能（例如，信号传导）的相对功效的G蛋白偶联受体配体，其大于其刺激G蛋白信号功能的相对功效。这些“ß-arrestin / GRK偏倚配体”可以作为G蛋白介导的信号传导的激动剂或拮抗剂，以及β-arrestin / GRK介导的信号转导的激动剂。本发明还涉及鉴定这些配体的方法以及在多种治疗方法中使用它们的方法。

2. 发明申请

WO2008021552A3 BIASED LIGANDS AND METHODS OF IDENTIFYING SAME 审中-公开
标题翻译：偏差配体和鉴定方法
公开(公告)号：WO2008021552A3
公开(公告)日：2008-11-06
申请号：PCT/US2007018394
申请日：2007-08-20
申请人： UNIV DUKE , LEFKOWITZ ROBERT J , RAJAGOPAL KESHAVA , WHALEN ERIN J , DRAKE MATTHEW T , VIOLIN JONATHAN D , ROCKMAN HOWARD A , DEWIRE SCOTT M
发明人： LEFKOWITZ ROBERT J , RAJAGOPAL KESHAVA , WHALEN ERIN J , DRAKE MATTHEW T , VIOLIN JONATHAN D , ROCKMAN HOWARD A , DEWIRE SCOTT M
IPC分类号： G01N33/53 , A01N37/18 , A61K38/00 , G01N33/567
CPC分类号： G01N33/74 , G01N2333/726
摘要： The present invention relates to G protein-coupled receptor ligands having a relative efficacy for stimulating ß-arrestin/G protein-coupled receptor kinase (GRK) function (e.g., signaling) that is greater than their relative efficacy for stimulating G-protein signaling function. These "ß-arrestin/GRK biased ligands" can act as agonists or antagonists of G protein-mediated signaling and agonists of ß-arrestin/GRK-mediated signal transduction. The invention further relates to methods of identifying such ligands and to methods of using same in a variety of therapeutic settings.
摘要翻译：本发明涉及具有刺激β-arrestin / G蛋白偶联受体激酶（GRK）功能（例如，信号传导）的相对功效的G蛋白偶联受体配体，其大于其刺激G蛋白信号传导功能的相对功效。这些“β-arrestin / GRK偏爱配体”可以作为G蛋白介导的信号传导的激动剂或拮抗剂，以及β-arrestin / GRK介导的信号转导的激动剂。本发明进一步涉及鉴定此类配体的方法以及在各种治疗环境中使用它们的方法。

3. 发明申请

WO2009151542A3 NICOTINIC ACID RECEPTOR LIGANDS 审中-公开
公开(公告)号：WO2009151542A3
公开(公告)日：2010-02-25
申请号：PCT/US2009003218
申请日：2009-05-27
申请人： UNIV DUKE , 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 ß-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。

4. 发明申请

WO2006076225A2 METHODS AND SYSTEMS FOR IDENTIFYING AND MONITORING S-NITROSOTHIOLS IN BIOLOGICAL SAMPLES 审中-公开
标题翻译：用于鉴定和监测生物样品中的S-硝基酚的方法和系统
公开(公告)号：WO2006076225A2
公开(公告)日：2006-07-20
申请号：PCT/US2006000457
申请日：2006-01-06
申请人： WHALEN ERIN J
发明人： WHALEN ERIN J
IPC分类号： G01N33/50
CPC分类号： G01N33/5038 , Y10T436/182
摘要： The present invention describes methods and kits for determining the level of S- nitrosothiols in biological fluid samples. The method includes separating tissue or cellular matter from the biological fluid sample and then contacting the biological fluid sample with paraformaldehyde in an amount sufficient to fix free thiols thereby essentially eliminating diaphorase activity of the free thiols. The biological fluid sample is then contacted with NADPH and nitro blue tetrazolium (NBT) wherein S-nitrosothiols in the biological fluid sample facilitate the reduction of NBT to NBT formazan or diformazan in the presence of paraformaldehyde. The amount of reduced NBT is measured and the determined levels correlate to the amount of S-nitrosothiols in the biological fluid sample.
摘要翻译：本发明描述了用于确定生物流体样品中S-亚硝基硫醇水平的方法和试剂盒。该方法包括从生物流体样品中分离组织或细胞物质，然后使生物液体样品与多聚甲醛接触，其量足以固定游离硫醇，从而基本上消除游离硫醇的心肌黄酶活性。然后生物流体样品与NADPH和硝基蓝四唑（NBT）接触，其中生物液体样品中的S-亚硝基硫醇有助于在多聚甲醛存在下将NBT还原为NBT甲an或二唑。测量降低的NBT的量并且测定的水平与生物液体样品中的S-亚硝基硫醇的量相关。

5. 发明申请

WO2004039313A3 PREVENTING DESENSITIZATION OF RECEPTORS 审中-公开
标题翻译：预防受体的降解
公开(公告)号：WO2004039313A3
公开(公告)日：2004-07-22
申请号：PCT/US0329134
申请日：2003-10-20
申请人： UNIV DUKE
发明人： STAMLER JONATHAN S , LEFKOWITZ ROBERT J , WHALEN ERIN J , KOCH WALTER J , PIANTADOSI CLAUDE A
IPC分类号： A61K45/00 , A61K20060101 , A61K31/19 , A61K31/195 , A61K31/198 , A61K31/21 , A61K31/223 , A61K31/5377 , A61K38/00 , A61K38/05 , A61K38/06 , A61P1/00 , A61P7/00 , A61P7/02 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P9/14 , A61P11/00 , A61P11/06 , A61P19/02 , A61P21/00 , A61P25/00 , A61P25/22 , A61P25/24
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。这具有适用性，例如对于患有心力衰竭的患者或手术后的左心室心脏装置或心脏泵，或即将进行手术并且在心脏事件或鸦片剂或鸦片剂或成瘾患有高胆固醇或囊性纤维化的患者中类风湿关节炎。

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