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1. 发明申请

US20110177612A1 Human G Protein-Coupled Receptors and Modulators Thereof for the Treatment of Metabolic-Related Disorders 审中-公开
标题翻译：人类G蛋白偶联受体及其调节剂用于治疗代谢相关性疾病
公开(公告)号：US20110177612A1
公开(公告)日：2011-07-21
申请号：US12881014
申请日：2010-09-13
申请人： David J. Unett , Ruoping Chen , Jeremy G. Richman , Daniel Connolly , Huong T. Dang , Bryan Choi , James Leonard , Yaron Hakak , Chen Liaw , Dominic Behan , Derek Chalmers , Michael Lerner , Kevin P. Lowitz
发明人： David J. Unett , Ruoping Chen , Jeremy G. Richman , Daniel Connolly , Huong T. Dang , Bryan Choi , James Leonard , Yaron Hakak , Chen Liaw , Dominic Behan , Derek Chalmers , Michael Lerner , Kevin P. Lowitz
IPC分类号： G01N33/68
CPC分类号： C07D403/02 , A01K2217/00 , A01K2227/105 , A01K2267/03 , A61K31/4439 , C07K14/705 , G01N33/566 , G01N2333/726 , G01N2500/00
摘要： The present invention relates to methods of identifying whether a candidate compound is a modulator of a G protein-coupled receptor (GPCR). In preferred embodiments, the GPCR is human. In other preferred embodiments, the GPCR is coupled to Gi and lowers the level of intracellular cAMP. In other preferred embodiments, the GPCR is expressed endogenously by adipocytes. In further preferred embodiments, the GPCR inhibits intracellular lipolysis. In other further preferred embodiments, the GPCR is a nicotinic acid receptor. The present invention also relates to methods of using a modulator of said GPCR. Preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, stroke, insulin resistance, and type 2 diabetes.
摘要翻译：本发明涉及鉴定候选化合物是G蛋白偶联受体（GPCR）的调节剂的方法。在优选的实施方案中，GPCR是人。在其它优选实施方案中，GPCR与Gi偶联并降低细胞内cAMP的水平。在其它优选实施方案中，GPCR由脂肪细胞内源性表达。在进一步优选的实施方案中，GPCR抑制细胞内脂肪分解。在其它进一步优选的实施方案中，GPCR是烟酸受体。本发明还涉及使用所述GPCR的调节剂的方法。优选的调节剂是激动剂。本发明的激动剂可用作预防或治疗代谢相关疾病，包括血脂异常，动脉粥样硬化，冠心病，中风，胰岛素抵抗和2型糖尿病的治疗剂。

2. 发明申请

US20050154029A1 Human G protein-coupled receptors and modulators thereof for the treatment of metabolic-related disorders 有权
标题翻译：人G蛋白偶联受体及其调节剂用于治疗代谢相关疾病
公开(公告)号：US20050154029A1
公开(公告)日：2005-07-14
申请号：US10930662
申请日：2004-08-31
申请人： David Unett , Ruoping Chen , Jeremy Richman , Daniel Connolly , Huong Dang , Bryan Choi , James Leonard , Yaron Hakak , Chen Liaw , Dominic Behan , Derek Chalmers , Michael Lerner , Kevin Lowitz
发明人： David Unett , Ruoping Chen , Jeremy Richman , Daniel Connolly , Huong Dang , Bryan Choi , James Leonard , Yaron Hakak , Chen Liaw , Dominic Behan , Derek Chalmers , Michael Lerner , Kevin Lowitz
IPC分类号： A61K31/4439 , G01N33/566 , C07D43/02
CPC分类号： C07D403/02 , A01K2217/00 , A01K2227/105 , A01K2267/03 , A61K31/4439 , C07K14/705 , G01N33/566 , G01N2333/726 , G01N2500/00
摘要： The present invention relates to methods of identifying whether a candidate compound is a modulator of a G protein-coupled receptor (GPCR). In preferred embodiments, the GPCR is human. In other preferred embodiments, the GPCR is coupled to Gi and lowers the level of intracellular cAMP. In other preferred embodiments, the GPCR is expressed endogenously by adipocytes. In further preferred embodiments, the GPCR inhibits intracellular lipolysis. In other further preferred embodiments, the GPCR is a nicotinic acid receptor. The present invention also relates to methods of using a modulator of said GPCR. Preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, stroke, insulin resistance, and type 2 diabetes.
摘要翻译：本发明涉及鉴定候选化合物是G蛋白偶联受体（GPCR）的调节剂的方法。在优选的实施方案中，GPCR是人。在其它优选实施方案中，GPCR与Gi偶联并降低细胞内cAMP的水平。在其它优选实施方案中，GPCR由脂肪细胞内源性表达。在进一步优选的实施方案中，GPCR抑制细胞内脂肪分解。在其它进一步优选的实施方案中，GPCR是烟酸受体。本发明还涉及使用所述GPCR的调节剂的方法。优选的调节剂是激动剂。本发明的激动剂可用作预防或治疗代谢相关疾病，包括血脂异常，动脉粥样硬化，冠心病，中风，胰岛素抵抗和2型糖尿病的治疗剂。

3. 发明申请

US20070079392A1 Human G protein-coupled receptors and modulators thereof for the treatment of metabolic-related disorders 审中-公开
标题翻译：人G蛋白偶联受体及其调节剂用于治疗代谢相关疾病
公开(公告)号：US20070079392A1
公开(公告)日：2007-04-05
申请号：US11603625
申请日：2006-11-22
申请人： Chen Liaw , Dominic Behan , Derek Chalmers , Michael Lerner , Huong Dang , Bryan Choi , James Leonard , Yaron Hakak , Kevin Lowitz , David Unett , Ruoping Chen , Jeremy Richman , Daniel Connolly
发明人： Chen Liaw , Dominic Behan , Derek Chalmers , Michael Lerner , Huong Dang , Bryan Choi , James Leonard , Yaron Hakak , Kevin Lowitz , David Unett , Ruoping Chen , Jeremy Richman , Daniel Connolly
IPC分类号： A01K67/027 , G01N33/53 , C12P21/06 , C07D403/02 , C07K14/705
CPC分类号： C07D403/02 , A01K2217/00 , A01K2227/105 , A01K2267/03 , A61K31/4439 , C07K14/705 , G01N33/566 , G01N2333/726 , G01N2500/00
摘要： The present invention relates to methods of identifying whether a candidate compound is a modulator of a G protein-coupled receptor (GPCR). In preferred embodiments, the GPCR is human. In other preferred embodiments, the GPCR is coupled to Gi and lowers the level of intracellular cAMP. In other preferred embodiments, the GPCR is expressed endogenously by adipocytes. In further preferred embodiments, the GPCR inhibits intracellular lipolysis. In other further preferred embodiments, the GPCR is a nicotinic acid receptor. The present invention also relates to methods of using a modulator of said GPCR. Preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, stroke, insulin resistance, and type 2 diabetes.
摘要翻译：本发明涉及鉴定候选化合物是G蛋白偶联受体（GPCR）的调节剂的方法。在优选的实施方案中，GPCR是人。在其它优选实施方案中，GPCR与Gi偶联并降低细胞内cAMP的水平。在其它优选实施方案中，GPCR由脂肪细胞内源性表达。在进一步优选的实施方案中，GPCR抑制细胞内脂肪分解。在其它进一步优选的实施方案中，GPCR是烟酸受体。本发明还涉及使用所述GPCR的调节剂的方法。优选的调节剂是激动剂。本发明的激动剂可用作预防或治疗代谢相关疾病，包括血脂异常，动脉粥样硬化，冠心病，中风，胰岛素抵抗和2型糖尿病的治疗剂。

4. 发明申请

US20050004178A1 Human G protein-coupled receptors and modulators thereof for the treatment of metabolic-related disorders 审中-公开
公开(公告)号：US20050004178A1
公开(公告)日：2005-01-06
申请号：US10897815
申请日：2004-07-23
申请人： David Unett , Ruoping Chen , Jeremy Richman , Daniel Connolly , Chen Liaw , Dominic Behan , Derek Chalmers , Michael Lerner , Huong Dang , Bryan Choi , James Leonard , Yaron Hakak , Kevin Lowitz
发明人： David Unett , Ruoping Chen , Jeremy Richman , Daniel Connolly , Chen Liaw , Dominic Behan , Derek Chalmers , Michael Lerner , Huong Dang , Bryan Choi , James Leonard , Yaron Hakak , Kevin Lowitz
IPC分类号： A61K31/4439 , G01N33/566 , G01N33/53
CPC分类号： C07D403/02 , A01K2217/00 , A01K2227/105 , A01K2267/03 , A61K31/4439 , C07K14/705 , G01N33/566 , G01N2333/726 , G01N2500/00
摘要： The present invention relates to methods of identifying whether a candidate compound is a modulator of a G protein-coupled receptor (GPCR). In preferred embodiments, the GPCR is human. In other preferred embodiments, the GPCR is coupled to Gi and lowers the level of intracellular cAMP. In other preferred embodiments, the GPCR is expressed endogenously by adipocytes. In further preferred embodiments, the GPCR inhibits intracellular lipolysis. In other further preferred embodiments, the GPCR is a nicotinic acid receptor. The present invention also relates to methods of using a modulator of said GPCR. Preferred modulator is agonist. Agonists of the invention are useful as therapeutic agents for the prevention or treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, stroke, insulin resistance, and type 2 diabetes.

5. 发明申请

US20050227295A9 Constitutively activated human G protein coupled receptors 失效
标题翻译：组成性激活人类G蛋白偶联受体
公开(公告)号：US20050227295A9
公开(公告)日：2005-10-13
申请号：US10723955
申请日：2003-11-26
申请人： Ruoping Chen , Chen Liaw , Kevin Lowitz , Derek Chalmers , Dominic Behan
发明人： Ruoping Chen , Chen Liaw , Kevin Lowitz , Derek Chalmers , Dominic Behan
IPC分类号： A61K38/00 , C07K14/705 , C07K14/72 , G01N33/566 , C12Q1/68 , G01N33/53 , G01N33/567
CPC分类号： C07K14/705 , A61K38/00 , C07K14/723 , G01N33/566
摘要： The invention disclosed in this patent document relates to transmembrane receptors, more particularly to a human G protein-coupled receptor for which the endogenous ligand is unknown (“orphan GPCR receptors”), and most particularly to mutated (non-endogenous) versions of the human GPCRs for evidence of constitutive activity.
摘要翻译：本专利文献中公开的发明涉及跨膜受体，更具体地涉及内源性配体未知的人G蛋白偶联受体（“孤儿GPCR受体”），最特别地涉及突变（非内源）版本的人类GPCRs作为组成型活动的证据。

6. 发明申请

US20070072248A1 Constitutively activated human G protein coupled receptors 审中-公开
标题翻译：组成性激活人类G蛋白偶联受体
公开(公告)号：US20070072248A1
公开(公告)日：2007-03-29
申请号：US11603356
申请日：2006-11-21
申请人： Ruoping Chen , Chen Liaw , Kevin Lowitz , Derek Chalmers , Dominic Behan
发明人： Ruoping Chen , Chen Liaw , Kevin Lowitz , Derek Chalmers , Dominic Behan
IPC分类号： G01N33/567 , A61K38/55
CPC分类号： G01N33/74 , G01N2333/726 , G01N2500/00 , G01N2800/24
摘要： The invention disclosed in this patent document relates to transmembrane receptors, more particularly to a human G protein-coupled receptor for which the endogenous ligand is unknown (“orphan GPCR receptors”), and most particularly to mutated (non-endogenous) versions of the human GPCRs for evidence of constitutive activity.
摘要翻译：本专利文献中公开的发明涉及跨膜受体，更具体地涉及内源性配体未知的人G蛋白偶联受体（“孤儿GPCR受体”），最特别地涉及突变（非内源）版本的人类GPCRs作为组成型活动的证据。

7. 发明申请

US20060240523A1 Endogenous and non-endogenous versions of human G protein-coupled receptors 审中-公开
公开(公告)号：US20060240523A1
公开(公告)日：2006-10-26
申请号：US11479174
申请日：2006-06-30
申请人： Chen Liaw , Derek Chalmers , Dominic Behan , Dominique Maciejewski-Lenior , James Leonard , I-Lin Lin , Daniel Ortuno
发明人： Chen Liaw , Derek Chalmers , Dominic Behan , Dominique Maciejewski-Lenior , James Leonard , I-Lin Lin , Daniel Ortuno
IPC分类号： C07K14/705 , C07H21/04 , C12P21/06
CPC分类号： C07K14/70571 , C07K14/723 , G01N33/566 , G01N2333/70571 , G01N2333/726
摘要： The invention disclosed in this patent document relates to transmembrane receptors, more particularly to a human G protein-coupled receptor and to mutated (non-endogenous) versions of the human GPCRs for evidence of constitutive activity.

8. 发明申请

US20050119182A1 Non-endogenous, constitutively activated human serotonin receptors and small molecule modulators thereof 有权
标题翻译：非内源性，组成型激活的人血清素受体及其小分子调节剂
公开(公告)号：US20050119182A1
公开(公告)日：2005-06-02
申请号：US10980560
申请日：2004-11-02
申请人： Dominic Behan , Derek Chalmers , Chen Liaw , Joseph Russo , William Thomsen
发明人： Dominic Behan , Derek Chalmers , Chen Liaw , Joseph Russo , William Thomsen
IPC分类号： C07D231/12 , C07D231/16 , C07D409/12 , C07K14/705 , C07K14/72 , G01N33/566 , A61K38/17 , C07H21/04
CPC分类号： C07D231/12 , C07D231/16 , C07D409/12 , C07K14/70571 , C07K14/723 , G01N33/566 , G01N2333/70571 , G01N2333/726
摘要： Disclosed herein are non-endogenous, constitutively activated forms of the human 5-HT2A and human 5-HT2C receptors and uses of such receptors to screen candidate compounds. Further disclosed herein are candidate compounds identified by the screening method which act at the 5HT2A receptors. Yet further disclosed is a new class of compounds which act at the 5HT2A receptors.
摘要翻译：本文公开了非内源性，组成型活化形式的人5-HT2A和人5-HT 2C受体以及这些受体用于筛选候选化合物的用途。本文进一步公开的是通过在5HT2A受体上起作用的筛选方法鉴定的候选化合物。还进一步公开了作为5HT2A受体的新类化合物。

9. 发明授权

US07741064B2 Materials and methods relating to G-protein coupled receptor oligomers 有权
标题翻译：与G蛋白偶联受体低聚物有关的材料和方法
公开(公告)号：US07741064B2
公开(公告)日：2010-06-22
申请号：US12119401
申请日：2008-05-12
申请人： Graeme Milligan , Dominic Behan
发明人： Graeme Milligan , Dominic Behan
IPC分类号： C07K14/705 , C07K19/00 , C12N15/62 , G01N33/566
CPC分类号： C07K14/705 , A61K38/00 , C07K14/4722 , C07K14/70571 , C07K14/723 , C07K2319/00 , G01N33/566 , G01N2333/726
摘要： The invention provides materials and methods relating to G-protein coupled receptor (GPCR) oligomers. Complexes of two or more GPCRs associated with G-proteins are provided. Also provided are fusion proteins comprising a GPCR and a G-protein, nucleic acids, expression vectors and host cells. Methods of producing the complexes and fusion proteins of the invention are also provided.
摘要翻译：本发明提供了与G蛋白偶联受体（GPCR）寡聚体有关的材料和方法。提供了与G蛋白相关的两个或多个GPCR的复合物。还提供了包含GPCR和G蛋白，核酸，表达载体和宿主细胞的融合蛋白。还提供了制备本发明的复合物和融合蛋白的方法。

10. 发明申请

US20080009551A1 Methods and Compositions for Identifying Modulators of G Protein-Coupled Receptors 审中-公开
标题翻译：鉴定G蛋白偶联受体的调节剂的方法和组合
公开(公告)号：US20080009551A1
公开(公告)日：2008-01-10
申请号：US10554521
申请日：2004-04-29
申请人： Fu-Yue Zeng , Dominic Behan
发明人： Fu-Yue Zeng , Dominic Behan
IPC分类号： A61K35/00 , A61P43/00 , C07H21/00 , C07K14/00 , C12Q1/02 , C12Q1/68
CPC分类号： C07K14/705
摘要： The subject invention provides methods for making ligand upregulatable G-protein coupled receptors (GPCRs). Ligand upregulatable GPCRs contain a modified TM5-IC3-TM6 segment, which provides for increased levels of the ligand upregulatable GPCR in a host cell in the presence of a ligand as compared to the absence of the ligand. The subject invention also provides assays for screening test compounds for a ligand of a GPCR using a ligand upregulatable GPCR. In these assays, a ligand upregulatable GPCR is contacted with a test compound, and an increase in the detectable amount of the ligand upregulatable GPCR in the host cell indicates that the test compound is a ligand of the GPCR. Said indicated ligands encompass modulators of the GPCR. Said modulators of the GPCR are particularly useful in treating GPCR-related conditions.
摘要翻译：本发明提供了制备配体可上调的G-蛋白偶联受体（GPCR）的方法。配体可升高的GPCR含有修饰的TM5-IC3-TM6区段，其与配体不存在相比，在配体存在下提供宿主细胞中配体上调GPCR的水平。本发明还提供了使用配体上调GPCR筛选GPCR配体的测试化合物的测定法。在这些测定中，配体可升高的GPCR与受试化合物接触，并且宿主细胞中配体上调GPCR的可检测量的增加表明测试化合物是GPCR的配体。所述指示的配体包括GPCR的调节剂。 GPCR的所述调节剂在治疗GPCR相关病症中特别有用。

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