Neuroendocrine tumors (NETs) arise from neuroendocrine cells and manifest in diverse organs. Key players in their regulation are somatostatin and its receptors (SSTR1–SSTR5). Understanding receptor–ligand interactions and signaling pathways is vital for elucidating their role in tumor development and therapeutic potential. This review highlights SSTR characteristics, localization, and expression in tissues, impacting physiological functions. Mechanisms of somatostatin and synthetic analogue binding to SSTRs, their selectivity, and their affinity were analyzed. Upon activation, somatostatin initiates intricate intracellular signaling, involving cAMP, PLC, and MAP kinases and influencing growth, differentiation, survival, and hormone secretion in NETs. This review explores SSTR expression in different tumor types, examining receptor activation effects on cancer cells. SSTRs’ significance as therapeutic targets is discussed. Additionally, somatostatin and analogues’ role in hormone secretion regulation, tumor growth, and survival is emphasized, presenting relevant therapeutic examples. In conclusion, this review advances the knowledge of receptor–ligand interactions and signaling pathways in somatostatin receptors, with potential for improved neuroendocrine tumor treatments.
神经内分泌肿瘤(NETs)起源于神经内分泌细胞,可发生于多种器官。生长抑素及其受体(SSTR1–SSTR5)在其调控中起关键作用。理解受体-配体相互作用及信号通路对于阐明其在肿瘤发展和治疗潜力中的作用至关重要。本综述重点阐述了SSTR的特性、组织定位及表达情况,及其对生理功能的影响。分析了生长抑素及其合成类似物与SSTR的结合机制、选择性和亲和力。激活后,生长抑素启动复杂的细胞内信号传导,涉及cAMP、PLC和MAP激酶,并影响NETs的生长、分化、存活和激素分泌。本综述探讨了不同肿瘤类型中SSTR的表达,考察了受体激活对癌细胞的影响。讨论了SSTR作为治疗靶点的重要性。此外,强调了生长抑素及其类似物在激素分泌调节、肿瘤生长和存活中的作用,并提供了相关治疗实例。总之,本综述增进了对生长抑素受体中受体-配体相互作用及信号通路的认识,具有改善神经内分泌肿瘤治疗的潜力。