title: Engineering GPCR signaling pathways with RASSLs.
abstract: 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 (G(s), G(i) and G(q)). We review these advances here to facilitate the use of these powerful and diverse tools.
authors.affiliation: Gladstone Institute of Cardiovascular Disease, 1650 Owens Street, San Francisco, California 94158, USA. bconklin@gladstone.ucsf.edu
authors.forename: Bruce R
authors.initials: BR
authors.lastname: Conklin
authors.forename: Edward C
authors.initials: EC
authors.lastname: Hsiao
authors.forename: Sylvie
authors.initials: S
authors.lastname: Claeysen
authors.forename: Aline
authors.initials: A
authors.lastname: Dumuis
authors.forename: Supriya
authors.initials: S
authors.lastname: Srinivasan
authors.forename: John R
authors.initials: JR
authors.lastname: Forsayeth
authors.forename: Jean-Marc
authors.initials: JM
authors.lastname: Guettier
authors.forename: W C
authors.initials: WC
authors.lastname: Chang
authors.forename: Ying
authors.initials: Y
authors.lastname: Pei
authors.forename: Ken D
authors.initials: KD
authors.lastname: McCarthy
authors.forename: Robert A
authors.initials: RA
authors.lastname: Nissenson
authors.forename: Jürgen
authors.initials: J
authors.lastname: Wess
authors.forename: Joël
authors.initials: J
authors.lastname: Bockaert
authors.forename: Bryan L
authors.initials: BL
authors.lastname: Roth
mesh_terms: D000818:Animals; D019143:Evolution, Molecular; D006801:Humans; D008024:Ligands; D011485:Protein Binding; D015202:Protein Engineering / Q000379:methods*; D043562:Receptors, G-Protein-Coupled / Q000032:analysis* / Q000737:chemistry / Q000235:genetics / Q000378:metabolism*; D015398:Signal Transduction
chemical_list: D008024:Ligands; D043562:Receptors, G-Protein-Coupled