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Two neuroendocrine G protein‐coupled receptor molecules, somatostatin and melatonin: Physiology of signal transduction and therapeutic perspectives
Ist Teil von
Journal of cellular physiology, 2021-04, Vol.236 (4), p.2505-2518
Ort / Verlag
United States: Wiley Subscription Services, Inc
Erscheinungsjahr
2021
Link zum Volltext
Quelle
Wiley Online Library - AutoHoldings Journals
Beschreibungen/Notizen
Recent studies have shown that G protein‐coupled receptors (GPCRs), the largest signal‐conveying receptor family, are targets for mutations occurring frequently in different cancer types. GPCR alterations associated with cancer development represent significant challenges for the discovery and the advancement of targeted therapeutics. Among the different molecules that can activate GPCRs, we focused on two molecules that exert their biological actions regulating many typical features of tumorigenesis such as cellular proliferation, survival, and invasion: somatostatin and melatonin. The modulation of signaling pathways, that involves these two molecules, opens an interesting scenario for cancer therapy, with the opportunity to act at different molecular levels. Therefore, the aim of this review is the analysis of the biological activity and the therapeutic potential of somatostatin and melatonin, displaying a high affinity for GPCRs, that interfere with cancer development and maintenance.
Schematic illustration of the G‐protein‐coupled receptor (GPCR)‐mediated signaling pathway. Upon activation by extracellular ligands, including biogenic amines, amino acids, ions, lipids, peptides, and proteins, GPCRs stimulate cytoplasmic and nuclear targets through signaling pathways mediated by the G proteins subunits (α, β, and γ). The signaling pathways involved regulate key biological functions, such as cell proliferation and survival, differentiation, motility, tumor progression, invasion, metastasis and angiogenesis processes.