公开(公告)号：USRE42190E1

公开(公告)日：2011-03-01

申请号：US11657110

申请日：2007-01-24

Applicant: Ruoping Chen ,  James N. Leonard

Inventor： Ruoping Chen ,  James N. Leonard

IPC: G01N33/567 ,  C12N5/02 ,  C12P21/00 ,  C07H21/04

CPC classification number: C07K14/723 ,  C07K14/705

Abstract: The invention disclosed in this patent document relates to transmembrane receptors, more particularly to endogenous, human orphan G protein-coupled receptors.

Abstract translation: 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，孤儿G蛋白偶联受体。

公开(公告)号：US07893235B2

公开(公告)日：2011-02-22

申请号：US11894692

申请日：2007-08-20

Applicant: Ruoping Chen ,  Huong T. Dang ,  Chen W. Liaw ,  I-Lin Lin

Inventor： Ruoping Chen ,  Huong T. Dang ,  Chen W. Liaw ,  I-Lin Lin

IPC: C07H21/04 ,  G01N33/53 ,  G01N33/567 ,  C12P21/06 ,  C12N1/20 ,  C12N15/00 ,  C12N5/00 ,  C12N5/02 ,  C12N15/74

CPC classification number: C07K14/723 ,  C07K14/705 ,  G01N33/74 ,  G01N2333/726 ,  G01N2500/02

Abstract: The invention disclosed in this patent document relates to transmembrane receptors, more particularly to endogenous, human orphan G protein-coupled receptors.

Abstract translation: 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，孤儿G蛋白偶联受体。

公开(公告)号：US20070134764A1

公开(公告)日：2007-06-14

申请号：US11601928

申请日：2006-11-20

Applicant: Ruoping Chen ,  Zhi Chu ,  Huong Dang ,  Kevin Lowitz ,  Cameron Pride

Inventor： Ruoping Chen ,  Zhi Chu ,  Huong Dang ,  Kevin Lowitz ,  Cameron Pride

IPC: C07K14/705 ,  C07H21/04 ,  C12P21/06

CPC classification number: C07K14/723 ,  A61K38/00 ,  C07D231/12 ,  C07D231/16 ,  C07D409/12 ,  C07K14/705 ,  C07K14/70571 ,  G01N33/566 ,  G01N2333/70571 ,  G01N2333/726

Abstract: 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, and to mutated (non-endogenous) versions of the human GPCRs for evidence of constitutive activity.

Abstract translation: 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，以及用于组成型活性证据的人GPCR的突变（非内源）版本。

公开(公告)号：US20050227295A9

公开(公告)日：2005-10-13

申请号：US10723955

申请日：2003-11-26

Applicant: Ruoping Chen ,  Chen Liaw ,  Kevin Lowitz ,  Derek Chalmers ,  Dominic Behan

Inventor： Ruoping Chen ,  Chen Liaw ,  Kevin Lowitz ,  Derek Chalmers ,  Dominic Behan

IPC: A61K38/00 ,  C07K14/705 ,  C07K14/72 ,  G01N33/566 ,  C12Q1/68 ,  G01N33/53 ,  G01N33/567

CPC classification number: C07K14/705 ,  A61K38/00 ,  C07K14/723 ,  G01N33/566

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20050154029A1

公开(公告)日：2005-07-14

申请号：US10930662

申请日：2004-08-31

Applicant: 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

Inventor： 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: A61K31/4439 ,  G01N33/566 ,  C07D43/02

CPC classification number: C07D403/02 ,  A01K2217/00 ,  A01K2227/105 ,  A01K2267/03 ,  A61K31/4439 ,  C07K14/705 ,  G01N33/566 ,  G01N2333/726 ,  G01N2500/00

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US06653086B1

公开(公告)日：2003-11-25

申请号：US09364425

申请日：1999-07-30

Applicant: Dominic P. Behan ,  Derek T. Chalmers ,  Chen W. Liaw ,  I Lin-Lin ,  Kevin P. Lowitz ,  Ruoping Chen

Inventor： Dominic P. Behan ,  Derek T. Chalmers ,  Chen W. Liaw ,  I Lin-Lin ,  Kevin P. Lowitz ,  Ruoping Chen

IPC: C12N1500

CPC classification number: C07D231/12 ,  C07D231/16 ,  C07D233/42 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D513/04 ,  C07K14/70571 ,  G01N33/68 ,  G01N2500/00

Abstract: Disclosed herein are techniques for directly identifying candidate compounds as agonists, partial agonists and/or, most preferably, inverse agonists, to endogenous, constitutively activated orphan G protein-coupled receptors. Such directly identified compounds can be utilized, most preferably, in pharmaceutical compositions

Abstract translation: 本文公开了用于直接鉴定候选化合物作为内源性，组成型激活的孤儿G蛋白偶联受体的激动剂，部分激动剂和/或最优选的反向激动剂的技术。 这种直接鉴定的化合物可以最优选地用于药物组合物中

公开(公告)号：US07829298B2

公开(公告)日：2010-11-09

申请号：US10930662

申请日：2004-08-31

Applicant: David J. Unett ,  Ruoping Chen ,  Jeremy G. Richman ,  Daniel T. Connolly ,  Huong T. Dang ,  Bryan J. Choi ,  James N. Leonard ,  Yaron Hakak ,  Chen W. Liaw ,  Dominic P. Behan ,  Derek T. Chalmers ,  Michael R. Lerner ,  Kevin P. Lowitz

Inventor： David J. Unett ,  Ruoping Chen ,  Jeremy G. Richman ,  Daniel T. Connolly ,  Huong T. Dang ,  Bryan J. Choi ,  James N. Leonard ,  Yaron Hakak ,  Chen W. Liaw ,  Dominic P. Behan ,  Derek T. Chalmers ,  Michael R. Lerner ,  Kevin P. Lowitz

IPC: G01N33/53

CPC classification number: C07D403/02 ,  A01K2217/00 ,  A01K2227/105 ,  A01K2267/03 ,  A61K31/4439 ,  C07K14/705 ,  G01N33/566 ,  G01N2333/726 ,  G01N2500/00

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US07816492B2

公开(公告)日：2010-10-19

申请号：US11417708

申请日：2006-05-04

Applicant: Ruoping Chen ,  James N. Leonard

Inventor： Ruoping Chen ,  James N. Leonard

IPC: C07K14/00 ,  C07H21/04

CPC classification number: C07K14/723 ,  C07K14/705 ,  G01N33/74 ,  G01N2333/726 ,  G01N2500/02

Abstract: The invention disclosed in this patent document relates to transmembrane receptors, more particularly to endogenous, human orphan G protein-coupled receptors.

Abstract translation: 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，孤儿G蛋白偶联受体。

公开(公告)号：US07358225B2

公开(公告)日：2008-04-15

申请号：US10649193

申请日：2003-08-26

Applicant: Marilyn H. Perrin ,  Ruoping Chen ,  Kathy A. Lewis ,  Wylie W. Vale, Jr. ,  Cynthia J. Donaldson ,  Paul Sawchenko

Inventor： Marilyn H. Perrin ,  Ruoping Chen ,  Kathy A. Lewis ,  Wylie W. Vale, Jr. ,  Cynthia J. Donaldson ,  Paul Sawchenko

IPC: C07K14/435 ,  C07K14/72 ,  C07K14/705 ,  A61K38/00 ,  A61K38/17

CPC classification number: C07K14/72 ,  A61K38/00 ,  C07K14/723

Abstract: In accordance with the present invention, there are provided novel G-protein-coupled receptor proteins (CRF-R) characterized by having sufficient binding affinity for corticotropin releasing factor (CRF) such that concentrations of £ 10 nM of CRF occupy 350% of the binding sites of said receptor protein. Nucleic acid sequences encoding such receptors, assays employing same, as well as antibodies derived therefrom, are also disclosed. Invention CRF-Rs can be employed in a variety of ways, such as, for example, in bioassays, for production of antibodies thereto, in therapeutic compositions containing such proteins and/or antibodies.

Abstract translation: 根据本发明，提供了新颖的G蛋白偶联受体蛋白（CRF-R），其特征在于对促肾上腺皮质激素释放因子（CRF）具有足够的结合亲和力，使得CRF 10nM的浓度占据了3 所述受体蛋白的结合位点的50％。 还公开了编码这种受体的核酸序列，使用其的测定法，以及由其衍生的抗体。 本发明CRF-Rs可以以各种方式使用，例如在生物测定中用于生产抗体，在含有这种蛋白质和/或抗体的治疗组合物中。

公开(公告)号：US08440391B2

公开(公告)日：2013-05-14

申请号：US10723955

申请日：2003-11-26

Applicant: Ruoping Chen ,  Chen W. Liaw ,  Kevin P. Lowitz ,  Derek T. Chalmers ,  Dominic P. Behan

Inventor： Ruoping Chen ,  Chen W. Liaw ,  Kevin P. Lowitz ,  Derek T. Chalmers ,  Dominic P. Behan

IPC: C12Q1/00 ,  C12Q1/68 ,  C07K14/435

CPC classification number: C07K14/705 ,  A61K38/00 ,  C07K14/723 ,  G01N33/566

Abstract: 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.