Words similar to grk
Example sentences for: grk
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One of these is Grk2 , a member of the family of ionotropic glutamate receptor genes that is thought to play a role in modulating Huntington disease [ 44].
Two molecular loci recently have been implicated as potential modulators of GnRH receptor signaling: one is the receptor itself [ 23 ] , and the other is the G protein that transduces the signal generated by binding of the receptor to its agonist [ 9 ] . With respect to the former locus, G protein coupled receptor kinases (GRKs) act in an agonist-specific manner to phosphorylate intracellular regions of the receptor thus permitting β arrestin binding that sterically inhibits G protein association with the receptor [ 1 45 ] . We have reported previously that experimental expression of GRKs in GnRH receptor-expressing heterologous cells (COS-1) suppressed GnRH-stimulated IP 3 production, and that co-expression of GRK2 and β-arrestin 2 suppressed GnRH receptor signaling more than that of either alone [ 23 ] . Stronger evidence that the GRK/β arrestin paradigm may play a role in regulating GnRH receptor signaling is our recent finding that adenovirus-mediated gene transfer of GRK2 into normal pituitary gonadotropes suppressed GnRH-stimulated LH secretion and IP 3 production [ 31 ] . However, no evidence has been presented for a direct interaction between β-arrestin and the GnRH receptor.
Site-directed mutagenesis studies indicate that all four of these serines are phosphorylated by GRK, and all four are needed for desensitization [ 12 ] . The influence of this motif on down-regulation was not investigated, however.
The results of the current investigation as well as those presented earlier [ 31 ] nominate two molecular mechanisms as playing roles in setting the responsiveness level of GnRH receptor signaling; i.e., the RGS3 system acts at the G protein transducing step and the GRK/β arrestin system acts at the level of the receptor.
Initial uncoupling of the beta-2 receptor from the G protein after agonist binding is mediated by phosphorylation by G protein-coupled receptor kinase (GRK) of specific residues in the carboxyl tail of the receptor.
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