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Int. J. Mol. Sci. 2018, 19(12), 3840;

GPCR Modulation in Breast Cancer

Department of Pharmacy, Health and Nutritional Sciences, University of Calabria, 87036 Rende, Italy
Laboratoire des Biomolécules, CNRS-UM7203, Sorbonne University, Ecole Normale Supérieure, F-75252 Paris, France
Authors to whom correspondence should be addressed.
Received: 3 November 2018 / Revised: 22 November 2018 / Accepted: 27 November 2018 / Published: 2 December 2018
(This article belongs to the Special Issue Cancer-Driver G Protein-Coupled Receptors as Therapeutic Targets)
PDF [5606 KB, uploaded 13 December 2018]


Breast cancer is the most prevalent cancer found in women living in developed countries. Endocrine therapy is the mainstay of treatment for hormone-responsive breast tumors (about 70% of all breast cancers) and implies the use of selective estrogen receptor modulators and aromatase inhibitors. In contrast, triple-negative breast cancer (TNBC), a highly heterogeneous disease that may account for up to 24% of all newly diagnosed cases, is hormone-independent and characterized by a poor prognosis. As drug resistance is common in all breast cancer subtypes despite the different treatment modalities, novel therapies targeting signaling transduction pathways involved in the processes of breast carcinogenesis, tumor promotion and metastasis have been subject to accurate consideration. G protein-coupled receptors (GPCRs) are the largest family of cell-surface receptors involved in the development and progression of many tumors including breast cancer. Here we discuss data regarding GPCR-mediated signaling, pharmacological properties and biological outputs toward breast cancer tumorigenesis and metastasis. Furthermore, we address several drugs that have shown an unexpected opportunity to interfere with GPCR-based breast tumorigenic signals. View Full-Text
Keywords: GPCRs; breast cancer; signal transduction GPCRs; breast cancer; signal transduction

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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).

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Lappano, R.; Jacquot, Y.; Maggiolini, M. GPCR Modulation in Breast Cancer. Int. J. Mol. Sci. 2018, 19, 3840.

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