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Oligomerization and cooperativity in GPCRs from the perspective of the angiotensin AT1 and dopamine D2 receptors

Research output: Contribution to journalArticle

Isik Kantarcioglu, Ramin Ekhteiari Salmas, Ismail Erol, Serdar Durdagi, Busecan Aksoydan

Original languageEnglish
JournalNeuroscience Letters
Early online date20 Apr 2018
DOIs
Accepted/In press16 Apr 2018
E-pub ahead of print20 Apr 2018

King's Authors

Abstract

G Protein-Coupled Receptors (GPCRs) can form homo- and heterodimers or constitute higher oligomeric clusters with other heptahelical GPCRs. In this article, multiscale molecular modeling approaches as well as experimental techniques which are used to study oligomerization of GPCRs are reviewed. In particular, the effect of dimerization/oligomerization to the ligand binding affinity of individual protomers and also on the efficacy of the oligomer are discussed by including diverse examples from the literature. In addition, possible allosteric effects that may emerge upon interaction of GPCRs with membrane components, like cholesterol, is also discussed. Investigation of these above-mentioned interactions may greatly contribute to the candidate molecule screening studies and development of novel therapeutics with fewer adverse effects.

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