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Chapter 16

The Complex Role of G Protein-coupled Receptor Kinase 2 (GRK2) in Cell Signalling: Beyond GPCR Desensitization

G protein-coupled receptor kinases (GRKs) were initially identified as key players of G protein-coupled receptors (GPCR) desensitization by promoting agonist-induced receptor phosphorylation and subsequent arrestin binding. However, cumulative evidence is putting forward novel roles for GRKs, particularly for the ubiquitous GRK2 isoform. GRK2 can phosphorylate a growing number of non-GPCR substrates and associate with a variety of proteins related to signal transduction, thus suggesting that this kinase could also have diverse, unforeseen ‘effector’ functions. In fact, the increasing complexity of the GRK2 ‘interactome’ suggest that this kinase plays a central, integrative role in signal transduction cascades. Ongoing research is identifying how specific GRK2 interactomes are orchestrated in a stimulus, cell type or context-specific way. This will help to understand how alterations in GRK2 levels or functionality participate in the onset and development of several cardiovascular and inflammatory diseases, and of some types of tumors.

Print publication date: 30 Aug 2011
Copyright year: 2011
Print ISBN: 978-1-84973-183-6
PDF eISBN: 978-1-84973-344-1
From the book series:
RSC Drug Discovery