GRK2: multiple roles beyond G protein-coupled receptor desensitization
نویسندگان
چکیده
منابع مشابه
G-protein Coupled Receptor Dimerization
A growing body of evidence suggests that GPCRs exist and function as dimers or higher oligomers. The evidence for GPCR dimerization comes from biochemical, biophysical and functional studies. In addition, researchers have shown the occurrence of heterodimerization between different members of the GPCR family. Two receptors can interact with each other to make a dimer through their extracellular...
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G protein-coupled receptor kinase 2 (GRK2) was initially identified as a key player, together with beta-arrestins, in the regulation of multiple G protein-coupled receptors (GPCR). Further research has revealed a complex GRK2 interactome, that includes a variety of proteins related to cell motility, and a role for GRK2 kinase activity in inhibiting chemokine-induced immune cell migration. In ad...
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For decades we have understood that G-protein-coupled receptors (GPCRs) are crucial links in the relay of information from extracellular stimuli to intracellular responses. Their importance is highlighted by the wide variety of GPCRs encoded in the human genome (Fredriksson et al., 2003; Perez, 2003) and the multiple mechanisms by which they are regulated (Clark, 1986; Palczewski and Benovic, 1...
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The kinetics of G-protein-coupled receptor activation and deactivation has, so far, been measured only indirectly, most frequently by assessing the production of various second messengers. We have developed methods based on fluorescence resonance energy transfer to quantify the kinetics of receptor activation by agonist (measured as conformational change in the receptor), the kinetics of G-prot...
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We examined the role of G-protein coupled receptor kinase-2 (GRK2) in the homologous desensitization of mGlu4 metabotropic glutamate receptors transiently expressed in human embryonic kidney (HEK) 293 cells. Receptor activation with the agonist l-2-amino-4-phosphonobutanoate (l-AP4) stimulated at least two distinct signaling pathways: inhibition of cAMP formation and activation of the mitogen-a...
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ژورنال
عنوان ژورنال: Trends in Pharmacological Sciences
سال: 2012
ISSN: 0165-6147
DOI: 10.1016/j.tips.2011.12.003