GRK6 is a Ser/Thr protein kinase and a member of the G protein-coupled receptor kinase subfamily. GRK6 is present in all tissues with strongest expression in placenta and skeletal muscle. GRK6 can phosphorylate proteins such as rhodopsin, ADRB2 and the leukotriene B4 receptor BLT1. GRK6 phosphorylates G protein-coupled dopamine receptors, thereby regulating their activity and mediating desensitization of the receptors. GRK6 knockout mice showed supersensitivity to the locomotor-stimulating effects of psychostimulants, including cocaine and amphetamine.
Brain dopaminergic transmission is a critical component in numerous vital functions, and its dysfunction is involved in several disorders, including addiction and Parkinson's disease. Responses to dopamine are mediated via G protein-coupled dopamine receptors (D1-D5). Desensitization of G protein-coupled receptors
The Journal of biological chemistry, 277(35), 31567-31576 (2002-06-22)
Desensitization of G-protein-coupled receptors may involve phosphorylation of serine and threonine residues. The leukotriene B(4) (LTB(4)) receptor (BLT1) contains 14 intracellular serines and threonines, 8 of which are part of consensus target sequences for protein kinase C (PKC) or casein
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