MOL Highlight: G-Protein–Coupled Receptor Kinase 2 as a Potential Modulator of the Hallmarks of Cancer
G protein-coupled receptors (GPCRs) are well known to contribute to cancer through classical second messenger signaling pathways, including via activation of small molecular weight G proteins. In this mini-review, Nogues et al. explore emerging evidence that regulators of GPCRs can serve as key “oncomodulators” that can either collaborate with cancer-driving pathways or modulate adaptive responses to these pathways. GPCR kinase 2 (GRK2) is one such regulator that phosphorylates and thereby promotes the desensitization of activated GPCRs, but the enzyme has also been reported to form a network of interactions with other cellular proteins, including those involved in cell proliferation, survival, motility and angiogenesis. In fact, altered GRK2 levels are now reported in different specific tumoral contexts. A better understanding of how GRK2 and related enzymes operate as oncomodulators will help in the design of future therapeutic strategies.
See the article by Nogués et al. at Molecular Pharmacology March 2017, 91 (3) 220-228; DOI: https://doi.org/10.1124/mol.116.107185