Abstract
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.
Highlights
G protein-coupled receptors (GPCRs) are hepta-transmembranar proteins playing a crucial role in membrane-initiated signaling processes
When a GPCR is activated, its conformation rapidly changes to allow it to couple to a Gα, Gβ and Gγ-containing heterotrimeric G-protein, which is anchored at the inner face of
We will discuss the current understanding of certain GPCRs that could be targeted to halt the growth of breast tumors, including triple-negative breast cancer (TNBC), and that could constitute a new generation of diagnostic tools for breast cancer
Summary
G protein-coupled receptors (GPCRs) are hepta-transmembranar proteins playing a crucial role in membrane-initiated signaling processes They display a key role in a variety of physiological features including cardiac functions, immune responses, metabolism and neurotransmission. We will discuss the current understanding of certain GPCRs that could be targeted to halt the growth of breast tumors, including TNBC, and that could constitute a new generation of diagnostic tools for breast cancer. In such a context, we will focus on GPCR-based drugs that have been designed, synthesized and evaluated for their efficacy in breast cancer
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