公开(公告)号：US08097452B2

公开(公告)日：2012-01-17

申请号：US10272983

申请日：2002-10-17

Applicant: Ruoping Chen ,  James N. Leonard

Inventor： Ruoping Chen ,  James N. Leonard

IPC: C12N15/12 ,  C12N15/63 ,  C12N5/10

CPC classification number: C07K14/705 ,  C07K14/723

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：US20070122878A1

公开(公告)日：2007-05-31

申请号：US11417708

申请日：2006-05-04

Applicant: Ruoping Chen ,  Huong Dang ,  Chen Liaw ,  I-Lin Lin

Inventor： Ruoping Chen ,  Huong Dang ,  Chen Liaw ,  I-Lin Lin

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

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：US20070065917A1

公开(公告)日：2007-03-22

申请号：US11603386

申请日：2006-11-22

Applicant: Ruoping Chen ,  Huong Dang ,  Kevin Lowitz

Inventor： Ruoping Chen ,  Huong Dang ,  Kevin Lowitz

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

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：US06902902B2

公开(公告)日：2005-06-07

申请号：US10314048

申请日：2002-12-06

Applicant: David J. Unett ,  Ruoping Chen ,  Jeremy G. Richman ,  Daniel T. Connolly ,  Yaron Hakak ,  Dominic P. Behan ,  Derek T. Chalmers

Inventor： David J. Unett ,  Ruoping Chen ,  Jeremy G. Richman ,  Daniel T. Connolly ,  Yaron Hakak ,  Dominic P. Behan ,  Derek T. Chalmers

IPC: A61K31/4439 ,  G01N33/566 ,  G01N33/53 ,  C07H21/04 ,  C07K14/00

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.

公开(公告)号：US06482608B1

公开(公告)日：2002-11-19

申请号：US09580734

申请日：2000-05-26

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: C12N510

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 50% 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，提供了新型G蛋白偶联受体蛋白（CRF-R），其特征在于对促皮质激素释放因子（CRF）具有足够的结合亲和力，使得10nM CRF的浓度占结合物的50％ 所述受体蛋白的位点。 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：US5728545A

公开(公告)日：1998-03-17

申请号：US110286

申请日：1993-08-23

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

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

IPC: G01N33/53 ,  C07K14/72 ,  C12N15/09 ,  C12N15/12 ,  C12P21/02 ,  C12P21/08 ,  C12Q1/68 ,  C12R1/91 ,  G01N33/566 ,  C07H21/04 ,  C12N15/11

CPC classification number: C07K14/72

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 .ltoreq.10 nM of CRF occupy .gtoreq.50% 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. The invention CRF-R 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的<10nM浓度占据> =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-R可以以各种方式使用，例如在生物测定中用于制备其抗体，在含有这种蛋白质和/或抗体的治疗组合物中。

公开(公告)号：US20130165633A1

公开(公告)日：2013-06-27

申请号：US13494750

申请日：2012-06-12

Applicant: RUOPING CHEN ,  HUONG T. DANG ,  KEVIN P. LOWITZ

Inventor： RUOPING CHEN ,  HUONG T. DANG ,  KEVIN P. LOWITZ

IPC: C07K14/705

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：US08198049B2

公开(公告)日：2012-06-12

申请号：US12958954

申请日：2010-12-02

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: C12P21/06 ,  G01N33/53 ,  G01N33/567 ,  C12N1/20 ,  C12N15/00 ,  C12N5/00 ,  C12N5/02 ,  C12N15/74 ,  C07H21/02 ,  C07H21/04 ,  C07K1/00 ,  C07K14/00 ,  C07K17/00

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：US20110195431A1

公开(公告)日：2011-08-11

申请号：US12958954

申请日：2010-12-02

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: G01N33/53 ,  C12N15/12 ,  C12N15/63 ,  C12N5/07 ,  C12Q1/02 ,  C12P21/00

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：US20070079392A1

公开(公告)日：2007-04-05

申请号：US11603625

申请日：2006-11-22

Applicant: 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

Inventor： 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: A01K67/027 ,  G01N33/53 ,  C12P21/06 ,  C07D403/02 ,  C07K14/705

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。