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Therapeutic Potential of G Protein‐Coupled Receptors Against Nonalcoholic Steatohepatitis

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Nonalcoholic steatohepatitis (NASH), the advanced stage of nonalcoholic fatty liver disease (NAFLD), affects approximately 6% of the population worldwide and is strongly associated with cardiometabolic disorders, placing subjects at a… Click to show full abstract

Nonalcoholic steatohepatitis (NASH), the advanced stage of nonalcoholic fatty liver disease (NAFLD), affects approximately 6% of the population worldwide and is strongly associated with cardiometabolic disorders, placing subjects at a sharply increased risk of end-stage hepatic diseases and extrahepatic symptoms. Despite the importance of NASH, no NASH-specific drugs have been approved by the FDA. G protein-coupled receptors (GPCRs), which represent the largest group of druggable targets in the human genome, strongly regulate pathophysiological events. Recent structural and molecular studies have further expanded upon the classic pharmacological applications of GPCRs and enabled the use of emerging GPCR agonists or antagonists for the treatment of metabolic diseases. These advances have encouraged new insights regarding the development of GPCR-targeted NASH therapies. In this review, we analyze up-to-date reports of GPCRs in NASH and discuss trends in the use of GPCRs as targets for NASH treatment.

Keywords: protein coupled; therapeutic potential; coupled receptors; nonalcoholic steatohepatitis

Journal Title: Hepatology
Year Published: 2021

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