Division of Cell Biology and Experimental Cancer Research, Institute of Pathology, University of Berne, Berne, Switzerland.
Mol Cell Endocrinol. 2012 Nov 25;364(1-2):46-53. doi: 10.1016/j.mce.2012.08.008. Epub 2012 Aug 19.
Peptide hormones of the glucagon-like peptide (GLP) family play an increasing clinical role, as reported for GLP-1 in diabetes therapy and insulinoma diagnostics. GLP-2, despite its known trophic and anti-inflammatory intestinal actions translated into preliminary clinical studies using the GLP-2 analogue teduglutide for treatment of short bowel syndrome and Crohn's disease, remains poorly characterized in terms of expression of its receptor in tissues of interest. Therefore, the GLP-2 receptor expression was assessed in 237 tumor and 148 non-neoplastic tissue samples with in vitro receptor autoradiography. A GLP-2 receptor expression was present in 68% of gastrointestinal stromal tumors (GIST). Furthermore, GLP-2 receptors were identified in the intestinal myenteric plexus, with significant up-regulation in active Crohn's disease. The GLP-2 receptors in GIST may be used for clinical applications like in vivo targeting with radiolabelled GLP-2 analogues for imaging and therapy. Moreover, the over-expressed GLP-2 receptor in the myenteric plexus may represent the morphological correlate of the clinical target of teduglutide in Crohn's disease.
胰高血糖素样肽 (GLP) 家族的肽类激素在临床中的作用日益凸显，GLP-1 在糖尿病治疗和胰岛素瘤诊断中的应用就是很好的例证。GLP-2 尽管其已知的营养和抗炎肠道作用已在初步临床研究中得到证实，这些研究使用 GLP-2 类似物特利格鲁肽治疗短肠综合征和克罗恩病，但就其在感兴趣的组织中受体的表达而言，仍未得到充分描述。因此，通过体外受体放射自显影术评估了 237 个肿瘤和 148 个非肿瘤组织样本中的 GLP-2 受体表达。胃肠道间质瘤 (GIST) 中有 68%存在 GLP-2 受体。此外，在肠肌间神经丛中也发现了 GLP-2 受体，在活动性克罗恩病中其表达显著上调。GIST 中的 GLP-2 受体可用于临床应用，例如用放射性标记的 GLP-2 类似物进行体内靶向成像和治疗。此外，在肌间神经丛中过度表达的 GLP-2 受体可能代表了特利格鲁肽在克罗恩病中的临床作用靶点的形态学相关物。
