Central 5-HTR2C in the Control of Metabolic Homeostasis

Author:

Yao Ting,He Jiehui,Cui Zhicheng,Wang Ruwen,Bao Kaixuan,Huang Yiru,Wang Ru,Liu Tiemin

Abstract

The 5-hydroxytryptamine 2C receptor (5-HTR2C) is a class G protein-coupled receptor (GPCR) enriched in the hypothalamus and the brain stem, where it has been shown to regulate energy homeostasis, including feeding and glucose metabolism. Accordingly, 5-HTR2C has been the target of several anti-obesity drugs, though the associated side effects greatly curbed their clinical applications. Dissecting the specific neural circuits of 5-HTR2C-expressing neurons and the detailed molecular pathways of 5-HTR2C signaling in metabolic regulation will help to develop better therapeutic strategies towards metabolic disorders. In this review, we introduced the regulatory role of 5-HTR2C in feeding behavior and glucose metabolism, with particular focus on the molecular pathways, neural network, and its interaction with other metabolic hormones, such as leptin, ghrelin, insulin, and estrogens. Moreover, the latest progress in the clinical research on 5-HTR2C agonists was also discussed.

Funder

National Key Research and Development Program of China

National Natural Science Foundation of China

State Key Laboratory of Pharmaceutical Biotechnology

Publisher

Frontiers Media SA

Subject

Endocrinology, Diabetes and Metabolism

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