Journal
JOURNAL OF CELLULAR PHYSIOLOGY
Volume 235, Issue 12, Pages 8938-8950Publisher
WILEY
DOI: 10.1002/jcp.29739
Keywords
GRP81; inflammation; metabolism
Categories
Funding
- Shanghai University of Medicine & Health Sciences [SFP-18-21-03-001]
- National Natural Science Foundation of China [31971098]
- Key Laboratory of Exercise and Health Sciences of Ministry of Education, Shanghai University of Sport
- Key project of Shanghai University Youth Research Fund for Teacher Training [ZZJKYX18005]
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GPR81 (also named as HCA1) is a member of a subfamily of orphan G-protein coupled receptors (GPCRs), coupled to G(i)-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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