Faculty Opinions recommendation of Structural insights into emergent signaling modes of G protein-coupled receptors.

Author(s):  
John Lowe
2011 ◽  
Vol 32 (10) ◽  
pp. 591-600 ◽  
Author(s):  
Julia K. Archbold ◽  
Jack U. Flanagan ◽  
Harriet A. Watkins ◽  
Joseph J. Gingell ◽  
Debbie L. Hay

2013 ◽  
Vol 41 (1) ◽  
pp. 135-136 ◽  
Author(s):  
Bice Chini ◽  
Marco Parenti ◽  
David R. Poyner ◽  
Mark Wheatley

The papers resulting from the recent Biochemical Society Focused Meeting ‘G-Protein-Coupled Receptors: from Structural Insights to Functional Mechanisms’ held in Prato in September 2012 are introduced in the present overview. A number of future goals for GPCR (G-protein-coupled receptor) research are considered, including the need to develop biophysical and computational methods to explore the full range of GPCR conformations and their dynamics, the need to develop methods to take this into account for drug discovery and the importance of relating observations on isolated receptors or receptors expressed in model systems to receptor function in vivo.


2020 ◽  
Vol 295 (33) ◽  
pp. 11626-11642 ◽  
Author(s):  
Ieva Sutkeviciute ◽  
Jean-Pierre Vilardaga

G protein–coupled receptors (GPCRs) represent the largest family of cell membrane proteins, with >800 GPCRs in humans alone, and recognize highly diverse ligands, ranging from photons to large protein molecules. Very important to human medicine, GPCRs are targeted by about 35% of prescription drugs. GPCRs are characterized by a seven-transmembrane α-helical structure, transmitting extracellular signals into cells to regulate major physiological processes via heterotrimeric G proteins and β-arrestins. Initially viewed as receptors whose signaling via G proteins is delimited to the plasma membrane, it is now recognized that GPCRs signal also at various intracellular locations, and the mechanisms and (patho)physiological relevance of such signaling modes are actively investigated. The propensity of GPCRs to adopt different signaling modes is largely encoded in the structural plasticity of the receptors themselves and of their signaling complexes. Here, we review emerging modes of GPCR signaling via endosomal membranes and the physiological implications of such signaling modes. We further summarize recent structural insights into mechanisms of GPCR activation and signaling. We particularly emphasize the structural mechanisms governing the continued GPCR signaling from endosomes and the structural aspects of the GPCR resensitization mechanism and discuss the recently uncovered and important roles of lipids in these processes.


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