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Updated: Jun 10, 2026

A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
Alternative G protein coupling and biased agonism: new insights into melanocortin-4 receptor signalling
Andreas Breit1, Thomas R H Büch, Ingrid Boekhoff
1Walther-Straub-Institut für Pharmakologie und Toxikologie, Goethestrasse 33, Ludwig-Maximilians-Universität München, 80336 München, Germany. andreas.breit@lrz.uni-muenchen.de
Abstract:
The melanocortin-4 receptor (MC4R) is a prototypical G protein-coupled receptor (GPCR) that plays a considerable role in controlling appetite and energy homeostasis. Signalling initiated by MC4R is orchestrated by multiple agonists, inverse agonism and by interactions with accessory proteins. The exact molecular events translating MC4R signalling into its physiological role, however, are not fully understood. This review is an attempt to summarize new aspects of MC4R signalling in the context of its recently discovered alternative G protein coupling, and to give a perspective on how future research could improve our knowledge about the intertwining molecular mechanisms that are responsible for the regulation of energy homeostasis by the melanocortin system.
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