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Succinate receptor GPR91, a Gα i coupled receptor that increases intracellular calcium concentrations through PLCβ
Author(s) -
Sundström Linda,
Greasley Peter J.,
Engberg Susanna,
Wallander Malin,
Ryberg Erik
Publication year - 2013
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/j.febslet.2013.05.067
Subject(s) - inositol phosphate , intracellular , pertussis toxin , receptor , inositol , agonist , adenosine , chemistry , cyclic adenosine monophosphate , g protein coupled receptor , calcium in biology , microbiology and biotechnology , biochemistry , g protein , biology
Succinate has been reported as the endogenous ligand for GPR91. In this study, succinate was confirmed to activate GPR91 resulting in both 3′–5′‐cyclic adenosine monophosphate (cAMP) inhibition and inositol phosphate formation in a pertussis toxin (PTX)‐sensitive manner. GPR91 agonist‐mediated effects detected using dynamic mass redistribution (DMR) were inhibited with PTX, edelfosine and U73122 demonstrating the importance of not only the Gα i pathway but also PLCβ. These results show that GPR91 when expressed in HEK293s cells couples exclusively through the Gα i pathway and acts through Gα i not only to inhibit cAMP production but also to increase intracellular Ca 2+ in an inositol phosphate dependent mechanism via PLCβ activation.