Willets et al., Mol Pharmacol 2001
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We have investigated the effects of G protein coupled receptor kinase ( GRK ) 3 and GRK6 on the phosphorylation and regulation of the M3 muscarinic acetylcholine receptor (mACh) endogenously expressed in SH-SY5Y cells
Willets et al., J Neurosci 2004
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Manipulation of endogenous GRK2 activity through introduction of either wild-type or catalytically inactive GRK2 ( ( K220R ) GRK2 ) almost completely inhibited agonist stimulated IP3 production, implying a phosphorylation independent regulation of M1 mACh receptor signaling, most probably mediated by a GRK2 N-terminal RGS-like ( regulator of G-protein signaling ) domain interaction with GTP bound Galpha ( q/11 )
Willets et al., J Biol Chem 2005
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Depletion of neuronal GRK2 using an antisense strategy almost completely inhibited M1 mACh receptor desensitization without enhancing acute agonist stimulated phospholipase C activity