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The roles of GRP81 as a metabolic sensor and inflammatory mediator
Author(s) -
Hu Jingyun,
Cai Ming,
Liu Yuran,
Liu Beibei,
Xue Xiangli,
Ji Ruifang,
Bian Xuepeng,
Lou Shujie
Publication year - 2020
Publication title -
journal of cellular physiology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.529
H-Index - 174
eISSN - 1097-4652
pISSN - 0021-9541
DOI - 10.1002/jcp.29739
Subject(s) - g protein coupled receptor , mediator , receptor , biology , signal transduction , subfamily , inflammation , lipid signaling , microbiology and biotechnology , adipose tissue , endogeny , pharmacology , biochemistry , immunology , gene
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.