Department of Morphology, Surgery and Experimental Medicine, University of Ferrara, Ferrara, Italy.
Department of Medical Sciences, University of Ferrara, Ferrara, Italy.
J Cell Physiol. 2021 Apr;236(4):2505-2518. doi: 10.1002/jcp.30062. Epub 2020 Sep 28.
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.
最近的研究表明,G 蛋白偶联受体(GPCR)是最大的信号转导受体家族,是不同癌症类型中经常发生突变的靶点。与癌症发展相关的 GPCR 改变代表了发现和推进靶向治疗的重大挑战。在能够激活 GPCR 的不同分子中,我们专注于两种分子,它们通过调节肿瘤发生的许多典型特征(如细胞增殖、存活和侵袭)来发挥其生物学作用:生长抑素和褪黑素。涉及这两种分子的信号通路的调节为癌症治疗开辟了一个有趣的场景,有机会在不同的分子水平上发挥作用。因此,本综述的目的是分析生长抑素和褪黑素的生物学活性和治疗潜力,它们对 GPCR 具有高亲和力,干扰癌症的发展和维持。