The roles of GRP81 as a metabolic sensor and inflammatory mediator |
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| Authors: | Jingyun Hu Ming Cai Yuran Liu Beibei Liu Xiangli Xue Ruifang Ji Xuepeng Bian Shujie Lou |
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| Institution: | 1. Key Laboratory of Exercise and Health Sciences of Ministry of Education, Shanghai University of Sport, Shanghai, China;2. College of Rehabilitation Sciences, Shanghai University of Medicine & Health Sciences, Shanghai, China;3. Key Laboratory of Exercise and Health Sciences of Ministry of Education, Shanghai University of Sport, Shanghai, China
Department of Clinical Medicine, Weifang Medical College, Weifang, Shandong, China |
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| Abstract: | GPR81 (also named as HCA1) is a member of a subfamily of orphan G-protein coupled receptors (GPCRs), coupled to Gi-type G proteins. GPR81 was discovered in 2001 and identified as the only known endogenous receptor of lactate under physiological conditions in 2008, which opened a new field of research on how lactate may act as a signal molecule along with the GPR81 expression in the roles of metabolic process and inflammatory response. Recent studies showed that the physiological functions of GPR81 include lipid metabolism in adipose tissues, metabolic excitability in the brain, cellular development, and inflammatory response modulation. These findings may reveal a novel therapeutic strategy to treat clinical, metabolic, and inflammatory diseases. This article will summarize past research on GPR81, including its characteristics of distribution and expression, functional residues, pharmacological, and physiological agonists, involvement in signal transduction, and pharmacological applications. |
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| Keywords: | GRP81 inflammation metabolism |
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