Signaling within Allosteric Machines: Signal Transmission Pathways Inside G Protein-Coupled Receptors

In recent years, our understanding of function of G protein-coupled receptors (GPCRs) has changed from a picture of simple signal relays, transmitting only a particular signal to a particular G protein heterotrimer, to versatile machines, capable of various responses to different stimuli and being m...

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Bibliographic Details
Main Authors: Damian Bartuzi, Agnieszka A. Kaczor, Dariusz Matosiuk
Format: Article
Language:English
Published: MDPI AG 2017-07-01
Series:Molecules
Subjects:
Online Access:https://www.mdpi.com/1420-3049/22/7/1188
Description
Summary:In recent years, our understanding of function of G protein-coupled receptors (GPCRs) has changed from a picture of simple signal relays, transmitting only a particular signal to a particular G protein heterotrimer, to versatile machines, capable of various responses to different stimuli and being modulated by various factors. Some recent reports provide not only the data on ligands/modulators and resultant signals induced by them, but also deeper insights into exact pathways of signal migration and mechanisms of signal transmission through receptor structure. Combination of these computational and experimental data sheds more light on underlying mechanisms of signal transmission and signaling bias in GPCRs. In this review we focus on available clues on allosteric pathways responsible for complex signal processing within GPCRs structures, with particular emphasis on linking compatible in silico- and in vitro-derived data on the most probable allosteric connections.
ISSN:1420-3049