Department of Nuclear Medicine, Radboud University Nijmegen Medical Centre, Nijmegen, The Netherlands.
Amino Acids. 2011 Nov;41(5):1049-58. doi: 10.1007/s00726-010-0501-y. Epub 2010 Mar 3.
Cholecystokinin (CCK) receptors are overexpressed in numerous human cancers, like medullary thyroid carcinomas, small cell lung cancers and stromal ovarian cancers. The specific receptor-binding property of the endogenous ligands for these receptors can be exploited by labeling peptides with a radionuclide and using these as carriers to guide the radioactivity to the tissues that express the receptors. In this way, tumors can be visualized using positron emission tomography and single photon emission computed tomography imaging. A variety of radiolabeled CCK/gastrin-related peptides has been synthesized and characterized for imaging. All peptides have the C-terminal CCK receptor-binding tetrapeptide sequence Trp-Met-Asp-Phe-NH(2) in common or derivatives thereof. This review focuses on the development and application of radiolabeled CCK/gastrin peptides for radionuclide imaging and radionuclide therapy of tumors expressing CCK receptors. We discuss both preclinical studies as well as clinical studies with CCK and gastrin peptides.
胆囊收缩素（CCK）受体在许多人类癌症中过度表达，如髓样甲状腺癌、小细胞肺癌和卵巢基质癌。这些受体的内源性配体的特异性受体结合特性可以通过用放射性核素标记肽并将其用作载体来引导放射性物质到表达受体的组织来利用。通过这种方式，可以使用正电子发射断层扫描和单光子发射计算机断层扫描成像来可视化肿瘤。已经合成并表征了多种放射性标记的 CCK/胃泌素相关肽用于成像。所有肽都具有共同的 C 末端 CCK 受体结合四肽序列 Trp-Met-Asp-Phe-NH(2)或其衍生物。这篇综述重点介绍了放射性标记的 CCK/胃泌素肽在放射性核素成像和表达 CCK 受体的肿瘤放射性核素治疗中的开发和应用。我们讨论了 CCK 和胃泌素肽的临床前研究和临床研究。
