Alternative G protein coupling and biased agonism: New insights into melanocortin-4 receptor signalling

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• 作者：Andreas Breit ; ^a ; ^{andreas.breit@lrz.uni-muenchen.de} ; Thomas R.H. B&#xfc ; ch^a ; Ingrid Boekhoff^a ; Hans J&#xfc ; rgen Solinski^a ; Ellen Damm^a ; Thomas Gudermann^a
• 关键词：Melanocortins ; MC4R ; AGRP ; Obesity ; Alternative G protein coupling ; Biased agonism
• 刊名：Molecular and Cellular Endocrinology
• 出版年：2011
• 出版时间：15 January 2011
• 年：2011
• 卷：331
• 期：2
• 页码：232-240
• 全文大小：760 K

文摘

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.