Pharmaceuticals 2011, 4(4), 567-589; doi:10.3390/ph4040567
Review

Molecular Approaches To Target GPCRs in Cancer Therapy

1 L.U.R.M. University Laboratory for Medical Research, University of Verona, Piazzale L.A. Scuro 10, Verona 37134, Italy 2 Department of Pathology and Diagnostic, G.B. Rossi Hospital, University of Verona, Piazzale L.A. Scuro 10, Verona 37134, Italy 3 Department of Medicine, G.B. Rossi Hospital, University of Verona, Piazzale L.A. Scuro 10, Verona 37134, Italy 4 Department of Surgery, G.B. Rossi Hospital, University of Verona, Piazzale L.A. Scuro 10, Verona 37134, Italy 5 Department of Experimental Medicine, University of Milano-Bicocca, Monza 20052, Italy
* Author to whom correspondence should be addressed.
Received: 11 March 2011; in revised form: 22 March 2011 / Accepted: 22 March 2011 / Published: 25 March 2011
(This article belongs to the Special Issue GPCR Based Drug Discovery)
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Abstract: Hundreds of G protein coupled receptor (GPCR) isotypes integrate and coordinate the function of individual cells mediating signaling between different organs in our bodies. As an aberration of the normal relationships that organize cells’ coexistence, cancer has to deceive cell-cell communication in order to grow and spread. GPCRs play a critical role in this process. Despite the fact that GPCRs represent one of the most common drug targets, current medical practice includes only a few anticancer compounds directly acting on their signaling. Many approaches can be envisaged to target GPCRs involved in oncology. Beyond interfering with GPCRs signaling by using agonists or antagonists to prevent cell proliferation, favor apoptosis, induce maturation, prevent migration, etc., the high specificity of the interaction between the receptors and their ligands can be exploited to deliver toxins, antineoplastic drugs or isotopes to transformed cells. In this review we describe the strategies that are in use, or appear promising, to act directly on GPCRs in the fight against neoplastic transformation and tumor progression.
Keywords: molecular pharmacology; cancer; G protein coupled receptor; heterotrimeric G protein

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MDPI and ACS Style

Innamorati, G.; Valenti, M.T.; Giovinazzo, F.; Dalle Carbonare, L.; Parenti, M.; Bassi, C. Molecular Approaches To Target GPCRs in Cancer Therapy. Pharmaceuticals 2011, 4, 567-589.

AMA Style

Innamorati G, Valenti MT, Giovinazzo F, Dalle Carbonare L, Parenti M, Bassi C. Molecular Approaches To Target GPCRs in Cancer Therapy. Pharmaceuticals. 2011; 4(4):567-589.

Chicago/Turabian Style

Innamorati, Giulio; Valenti, Maria Teresa; Giovinazzo, Francesco; Dalle Carbonare, Luca; Parenti, Marco; Bassi, Claudio. 2011. "Molecular Approaches To Target GPCRs in Cancer Therapy." Pharmaceuticals 4, no. 4: 567-589.

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