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Functional regulation of metabotropic glutamate receptor type 1c: a role for phosphorylation in the desensitization of the receptor
Author(s) -
Ciruela Francisco,
Giacometti Angelo,
McIlhinney R.A.Jeffrey
Publication year - 1999
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/s0014-5793(99)01547-1
Subject(s) - desensitization (medicine) , homologous desensitization , phosphorylation , metabotropic receptor , agonist , metabotropic glutamate receptor , chemistry , metabotropic glutamate receptor 5 , receptor , metabotropic glutamate receptor 2 , metabotropic glutamate receptor 1 , medicine , pharmacology , biochemistry , biology
The phosphorylation and desensitization of metabotropic glutamate receptor type 1c in response to agonist and phorbol esters has been studied. Specific immunoprecipitation of mGluR1c from cells treated with agonist or PMA showed a time‐dependent increase in the phosphorylation of a membrane protein with the same molecular weight as the dimeric form of the receptor. Measurements of inositol phosphate production showed a rapid functional desensitization of about 90% after agonist treatment, whereas treatment with PMA caused only a 30% loss in the same time. The extent of receptor phosphorylation following the different treatments paralleled the desensitization of the receptor. These results strongly suggest that phosphorylation of the dimeric form of mGluR1c, as a functionally active form, may play a role in its rapid desensitization.