Molecular Approaches To Target GPCRs in Cancer Therapy

Pharmaceuticals

Giulio Innamorati²  Maria Teresa Valenti²  Francesco Giovinazzo²  Luca Dalle Carbonare²  Marco Parenti¹ 

[1] Department of Experimental Medicine, University of Milano-Bicocca, Monza 20052, Italy;L.U.R.M. University Laboratory for Medical Research, University of Verona, Piazzale L.A. Scuro 10, Verona 37134, Italy

关键词: molecular pharmacology;    cancer;    G protein coupled receptor;    heterotrimeric G protein;   

DOI  :  10.3390/ph4040567

来源: mdpi

【 摘 要 】

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.

【 授权许可】

CC BY   
© 2011 by the authors; licensee MDPI, Basel, Switzerland.