Peptide receptor targeting in cancer: the somatostatin paradigm.
Peptide receptor targeting in cancer: the somatostatin paradigm.
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DOI：
10.1155/2013/926295
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发表时间：
2013
期刊：
影响因子：
--
通讯作者：
Florio T
中科院分区：
文献类型：
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作者：
Barbieri F;Bajetto A;Pattarozzi A;Gatti M;Würth R;Thellung S;Corsaro A;Villa V;Nizzari M;Florio T
参与病理生理过程的多肽受体是很有希望的治疗靶点。神经肽生长抑素(SST)是由人体大量器官和组织中的特化细胞产生的。SST主要通过激活5种G蛋白偶联受体sst1-5作为内分泌和外分泌的抑制因子，而在中枢神经系统中，SST作为神经递质/神经调节剂，调节运动和认知功能。SST/SST受体生物学的关键点，如单个受体亚型的信号通路、同源和异源二聚化、转运以及与生长因子受体的串扰等，已经得到了广泛的研究，尽管与包括癌症在内的一些病理疾病相关的功能仍未完全揭开。重要的是，SST在体外对癌细胞具有抗增殖和抗血管生成作用，在体内对实验性肿瘤也有抑制作用。此外，SST激动剂可作为抗肿瘤药物用于治疗垂体腺瘤和胃胰腺神经内分泌肿瘤。然而，SST受体在不同肿瘤组织类型的肿瘤细胞中都有表达，它们的药理作用有可能推广到其他类型的癌症，尽管到目前为止还没有得到显著的结果。本文就SST和SST受体在肿瘤细胞中的表达和功能作用的最新研究结果进行了讨论。
Peptide receptors involved in pathophysiological processes represent promising therapeutic targets. Neuropeptide somatostatin (SST) is produced by specialized cells in a large number of human organs and tissues. SST primarily acts as inhibitor of endocrine and exocrine secretion via the activation of five G-protein-coupled receptors, named sst1–5, while in central nervous system, SST acts as a neurotransmitter/neuromodulator, regulating locomotory and cognitive functions. Critical points of SST/SST receptor biology, such as signaling pathways of individual receptor subtypes, homo- and heterodimerization, trafficking, and cross-talk with growth factor receptors, have been extensively studied, although functions associated with several pathological conditions, including cancer, are still not completely unraveled. Importantly, SST exerts antiproliferative and antiangiogenic effects on cancer cells in vitro, and on experimental tumors in vivo. Moreover, SST agonists are clinically effective as antitumor agents for pituitary adenomas and gastro-pancreatic neuroendocrine tumors. However, SST receptors being expressed by tumor cells of various tumor histotypes, their pharmacological use is potentially extendible to other cancer types, although to date no significant results have been obtained. In this paper the most recent findings on the expression and functional roles of SST and SST receptors in tumor cells are discussed.