Glucagon-like peptide-1 receptor overexpression in cancer and its impact on clinical applications.
Glucagon-like peptide-1 receptor overexpression in cancer and its impact on clinical applications.
复制标题
DOI：
10.3389/fendo.2012.00158
复制
发表时间：
2012
影响因子：
5.2
通讯作者：
Reubi JC
中科院分区：
文献类型：
--
作者：
Körner M;Christ E;Wild D;Reubi JC
胰升糖素样肽(GLP)家族的多肽激素在临床上发挥着越来越重要的作用，如GLP-1在糖尿病治疗中的作用。此外，GLP受体在各种人类肿瘤类型中都有过表达，因此是重要的临床应用的分子靶点。特别是，几乎所有良性胰岛素瘤都高度过度表达GLP-1受体(GLP-1R)。用稳定的GLP-1类似物111In-DOTA/DPTA-exendin-4靶向GLP-1R为成功定位这些小肿瘤提供了一种新的途径。这种非侵入性技术有可能通过选择性动脉刺激和静脉采样来取代胰岛素瘤的侵袭性定位。恶性胰岛素瘤与良性胰岛素瘤相比，只有三分之一的病例表达GLP-1R，而它们更多地表达生长抑素2型受体。重要的是，两种受体中的一种似乎总是在恶性胰岛素瘤中表达。考虑到越来越多的GLP-1类似物用于糖尿病治疗，GLP-1R在部分癌症中的过度表达值得记住。虽然GLP-1R在肿瘤形成中的功能作用尚不清楚，但仔细监测接受GLP-1治疗的患者可能是安全的。
Peptide hormones of the glucagon-like peptide (GLP) family play an increasing clinical role, such as GLP-1 in diabetes therapy. Moreover, GLP receptors are overexpressed in various human tumor types and therefore represent molecular targets for important clinical applications. In particular, virtually all benign insulinomas highly overexpress GLP-1 receptors (GLP-1R). Targeting GLP-1R with the stable GLP-1 analogs 111In-DOTA/DPTA-exendin-4 offers a new approach to successfully localize these small tumors. This non-invasive technique has the potential to replace the invasive localization of insulinomas by selective arterial stimulation and venous sampling. Malignant insulinomas, in contrast to their benign counterparts, express GLP-1R in only one-third of the cases, while they more often express the somatostatin type 2 receptors. Importantly, one of the two receptors appears to be always expressed in malignant insulinomas. The GLP-1R overexpression in selected cancers is worth to be kept in mind with regard to the increasing use of GLP-1 analogs for diabetes therapy. While the functional role of GLP-1R in neoplasia is not known yet, it may be safe to monitor patients undergoing GLP-1 therapy carefully.