Reubi J C, Kvols L, Krenning E, Lamberts S W
Sandoz Research Institute, Berne, Switzerland.
Metabolism. 1990 Sep;39(9 Suppl 2):78-81. doi: 10.1016/0026-0495(90)90217-z.
Specific receptors for somatostatin (SS), mediating the various actions of this peptide, have been described in SS target tissues in animal and man. Using homogenate binding assays, as well as receptor autoradiography, the presence of SS receptors has been demonstrated in various regions of the brain (cortex, limbic system, basal ganglia), the anterior pituitary, the endocrine and exocrine pancreas, the gastrointestinal tract, and the adrenals. There are species-, as well as age-, related variations. Furthermore, there is evidence for different SS receptor subtypes. Interestingly, a large variety of human tumors also contain SS receptors with similar characteristics as those found in normal tissue; in numerous tumors, the SS receptor density is even higher than in healthy tissue counterparts. Most GH- and TSH-producing pituitary adenomas, but also a subgroup of endocrine inactive pituitary adenomas, have SS receptors; most carcinoids and islet cell carcinomas, as well as their metastases, also contain SS receptors. Several differentiated (usually EGF receptor negative) glia tumors possess SS receptors, whereas undifferentiated (EGF receptor positive) glia tumors lack such receptors. Furthermore, a subgroup of breast tumors, usually steroid receptor positive and neuroendocrine-differentiated, contain SS receptors. Finally, small cell lung carcinomas, but not non-small cell carcinomas, often possess SS receptors. These receptors are likely to be functional since in 11 acromegalics and 18 gastroenteropancreatic tumor patients, a positive correlation was observed between their SS receptor status and their hormone secretion sensitivity to Sandostatin.
生长抑素(SS)的特异性受体可介导该肽的多种作用,动物和人类的SS靶组织中已对其进行了描述。通过匀浆结合测定以及受体放射自显影技术,已证实在大脑的各个区域(皮质、边缘系统、基底神经节)、垂体前叶、内分泌和外分泌胰腺、胃肠道以及肾上腺中存在SS受体。存在物种以及年龄相关的差异。此外,有证据表明存在不同的SS受体亚型。有趣的是,多种人类肿瘤也含有与正常组织中发现的具有相似特征的SS受体;在许多肿瘤中,SS受体密度甚至高于健康组织对应物。大多数产生生长激素和促甲状腺激素的垂体腺瘤,以及内分泌无活性垂体腺瘤的一个亚组,都有SS受体;大多数类癌和胰岛细胞癌及其转移灶也含有SS受体。一些分化型(通常表皮生长因子受体阴性)神经胶质瘤具有SS受体,而未分化型(表皮生长因子受体阳性)神经胶质瘤则缺乏此类受体。此外,通常类固醇受体阳性且神经内分泌分化的乳腺肿瘤亚组含有SS受体。最后,小细胞肺癌而非非小细胞肺癌通常具有SS受体。这些受体可能具有功能,因为在11名肢端肥大症患者和18名胃肠胰肿瘤患者中,观察到他们的SS受体状态与其对善得定的激素分泌敏感性之间存在正相关。