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Open AccessArticle

Alpha-Bulges in G Protein-Coupled Receptors

Centre for Molecular and Biomolecular Informatics, Radboud University Medical Centre, Geert Grooteplein 26-28, 6525 GA Nijmegen, The Netherlands
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Author to whom correspondence should be addressed.
Present address: Switch Laboratory, Department of Cellular and Molecular Medicine, University of Leuven, 3000 Leuven, Belgium
Int. J. Mol. Sci. 2014, 15(5), 7841-7864; https://doi.org/10.3390/ijms15057841
Received: 20 January 2014 / Revised: 2 April 2014 / Accepted: 9 April 2014 / Published: 6 May 2014
(This article belongs to the Collection G Protein-Coupled Receptor Signaling and Regulation)
Agonist binding is related to a series of motions in G protein-coupled receptors (GPCRs) that result in the separation of transmembrane helices III and VI at their cytosolic ends and subsequent G protein binding. A large number of smaller motions also seem to be associated with activation. Most helices in GPCRs are highly irregular and often contain kinks, with extensive literature already available about the role of prolines in kink formation and the precise function of these kinks. GPCR transmembrane helices also contain many α-bulges. In this article we aim to draw attention to the role of these α-bulges in ligand and G-protein binding, as well as their role in several aspects of the mobility associated with GPCR activation. This mobility includes regularization and translation of helix III in the extracellular direction, a rotation of the entire helix VI, an inward movement of the helices near the extracellular side, and a concerted motion of the cytosolic ends of the helices that makes their orientation appear more circular and that opens up space for the G protein to bind. In several cases, α-bulges either appear or disappear as part of the activation process. View Full-Text
Keywords: GPCR; π-helix; α-bulge; GPCR activation; random forest; structure-function GPCR; π-helix; α-bulge; GPCR activation; random forest; structure-function
MDPI and ACS Style

Van der Kant, R.; Vriend, G. Alpha-Bulges in G Protein-Coupled Receptors. Int. J. Mol. Sci. 2014, 15, 7841-7864.

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