4.6 Review

Regulatory roles of G-protein coupled receptors in adipose tissue metabolism and their therapeutic potential

Journal

ARCHIVES OF PHARMACAL RESEARCH
Volume 44, Issue 2, Pages 133-145

Publisher

PHARMACEUTICAL SOC KOREA
DOI: 10.1007/s12272-021-01314-w

Keywords

GPCR; Obesity; Adipose tissue; Adrenoceptor; Adenosine receptor; Frizzled receptor; Lysophospholipid receptor

Funding

  1. National Research Foundation of Korea (NRF) - Korean government (MSIT) [NRF-2019R1C1C1002014, NRF-2018R1A5A2024425]
  2. National Research Foundation of Korea [4199990814417] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)

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The high incidence of obesity has led to an increased need to discover new therapeutic targets. Recent research has shown that G-protein coupled receptors (GPCRs) could be potential therapeutic targets to regulate adipose tissue metabolism.
The high incidence of obesity has increased the need to discover new therapeutic targets to combat obesity and obesity-related metabolic diseases. Obesity is defined as an abnormal accumulation of adipose tissue, which is one of the major metabolic organs that regulate energy homeostasis. However, there are currently no approved anti-obesity therapeutics that directly target adipose tissue metabolism. With recent advances in the understanding of adipose tissue biology, molecular mechanisms involved in brown adipose tissue expansion and metabolic activation have been investigated as potential therapeutic targets to increase energy expenditure. This review focuses on G-protein coupled receptors (GPCRs) as they are the most successful class of druggable targets in human diseases and have an important role in regulating adipose tissue metabolism. We summarize recent findings on the major GPCR classes that regulate thermogenesis and mitochondrial metabolism in adipose tissue. Improved understanding of GPCR signaling pathways that regulate these processes could facilitate the development of novel pharmacological approaches to treat obesity and related metabolic disorders.

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