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Molecules 2017, 22(7), 1188;

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

Department of Synthesis and Chemical Technology of Pharmaceutical Substances with Computer Modelling Lab, Medical University of Lublin, 4A Chodźki Str., Lublin PL20093, Poland
School of Pharmacy, University of Eastern Finland, Yliopistonranta 1, P.O. Box 1627, Kuopio FI-70211, Finland
Author to whom correspondence should be addressed.
Academic Editor: Yung Hou Wong
Received: 13 April 2017 / Revised: 4 July 2017 / Accepted: 10 July 2017 / Published: 15 July 2017
(This article belongs to the Special Issue G-protein Coupled Receptor Structure and Function)
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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. View Full-Text
Keywords: GPCRs; signaling; allostery; protein dynamics GPCRs; signaling; allostery; protein dynamics

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Bartuzi, D.; Kaczor, A.A.; Matosiuk, D. Signaling within Allosteric Machines: Signal Transmission Pathways Inside G Protein-Coupled Receptors. Molecules 2017, 22, 1188.

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