Engineering GPCR signaling pathways with RASSLs

被引：0

作者：

Bruce R Conklin

Edward C Hsiao

Sylvie Claeysen

Aline Dumuis

Supriya Srinivasan

John R Forsayeth

Jean-Marc Guettier

W C Chang

Ying Pei

Ken D McCarthy

Robert A Nissenson

Jürgen Wess

Joël Bockaert

Bryan L Roth

机构：

[1] Gladstone Institute of Cardiovascular Disease,Departments of Medicine and Cellular and Molecular Pharmacology

[2] University of California,and Departments of Medicine and Physiology

[3] San Francisco,Department of Physiology

[4] Endocrine Research Unit,Department of Neurosurgery

[5] Veterans Affairs Medical Center,Department of Pharmacology

[6] University of California,undefined

[7] San Francisco,undefined

[8] Centre National de la Recherche Scientifique,undefined

[9] UMR 5203,undefined

[10] Institut de Génomique Fonctionnelle,undefined

[11] 141 rue de la Cardonille and Institut National de la Santé et de la Recherche Médicale,undefined

[12] U661,undefined

[13] and Université Montpellier,undefined

[14] 600 16th St. University of California,undefined

[15] San Francisco,undefined

[16] University of California,undefined

[17] San Francisco,undefined

[18] MCB 226,undefined

[19] Laboratory of Bioorganic Chemistry,undefined

[20] National Institute of Diabetes and Digestive and Kidney Diseases,undefined

[21] National Institutes of Health,undefined

[22] 9000 Rockville Pike,undefined

[23] Graduate Program in Pharmaceutical Sciences and Pharmacogenomics,undefined

[24] University of California,undefined

[25] San Francisco,undefined

[26] 1700 Fourth Street,undefined

[27] Byers Hall,undefined

[28] Suite BH-216,undefined

[29] University of North Carolina,undefined

[30] Chapel Hill,undefined

[31] 1106 Mary Ellen Jones Building,undefined

[32] CB 7365,undefined

来源：

Nature Methods | 2008年 / 5卷

关键词：

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学科分类号：

摘要：

We are creating families of designer G protein–coupled receptors (GPCRs) to allow for precise spatiotemporal control of GPCR signaling in vivo. These engineered GPCRs, called receptors activated solely by synthetic ligands (RASSLs), are unresponsive to endogenous ligands but can be activated by nanomolar concentrations of pharmacologically inert, drug-like small molecules. Currently, RASSLs exist for the three major GPCR signaling pathways (Gs, Gi and Gq). We review these advances here to facilitate the use of these powerful and diverse tools.

引用

页码：673 / 678

页数：5

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