Regulators of G-protein signaling and their Gα substrates: promises and challenges in their use as drug discovery targets.

@article{Kimple2011RegulatorsOG,
  title={Regulators of G-protein signaling and their Gα substrates: promises and challenges in their use as drug discovery targets.},
  author={Adam J. Kimple and Dustin E. Bosch and Patrick M. Gigu{\`e}re and David P. Siderovski},
  journal={Pharmacological reviews},
  year={2011},
  volume={63 3},
  pages={728-49}
}
Because G-protein coupled receptors (GPCRs) continue to represent excellent targets for the discovery and development of small-molecule therapeutics, it is posited that additional protein components of the signal transduction pathways emanating from activated GPCRs themselves are attractive as drug discovery targets. This review considers the drug discovery potential of two such components: members of the "regulators of G-protein signaling" (RGS protein) superfamily, as well as their substrates… CONTINUE READING

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