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Nat Rev Drug Discov. 2011 Jan;10(1):47-60. doi: 10.1038/nrd3320.

G protein-coupled receptors: novel targets for drug discovery in cancer.

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Department of Pharmaco-Biology, University of Calabria, 87030 Rende, Cosenza, Italy.


G protein-coupled receptors (GPCRs) belong to a superfamily of cell surface signalling proteins that have a pivotal role in many physiological functions and in multiple diseases, including the development of cancer and cancer metastasis. Current drugs that target GPCRs - many of which have excellent therapeutic benefits - are directed towards only a few GPCR members. Therefore, huge efforts are currently underway to develop new GPCR-based drugs, particularly for cancer. We review recent findings that present unexpected opportunities to interfere with major tumorigenic signals by manipulating GPCR-mediated pathways. We also discuss current data regarding novel GPCR targets that may provide promising opportunities for drug discovery in cancer prevention and treatment.

[Indexed for MEDLINE]

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