Virgolini I
Department of Nuclear Medicine, University of Vienna, Austria.
Eur J Clin Invest. 1997 Oct;27(10):793-800. doi: 10.1046/j.1365-2362.1997.1990742.x.
The multiple aspects of radioligand-receptor interactions do not only show a major impact of certain cell surface-bound receptors in the pathophysiology of human disease: the concept of radioligand-receptor interactions has also been extended to the clinic. In particular, naturally occurring peptides, when radiolabelled, are clinically useful for the imaging diagnosis of human disease and have future implications for the treatment of tumour expressing certain target receptors using radiolabelled peptide tracers. The finding that receptors for VIP (vasoactive intestinal peptide) and SST (somatostatin) are overexpressed on tumour cells presents a breakthrough into this direction. Recent data indicate that [123I]-VIP receptor scintigraphy is clinically useful for the in vivo localization of small primary adenocarcinomas, liver metastases and certain endocrine tumours of the gastrointestinal tract. After the successful clinical introduction of the SST analogues [123I]-Tyr3-octreotide and [111In]-DTPA-D-Phe1-octreotide for localization diagnosis of neuroendocrine tumours in 1989, P829, labelled with the more cost-effective radionuclide 99mTc, nowadays promises to be a potential novel diagnostic imaging agent for tumours expressing SST/VIP receptors. Furthermore, the novel SST analogue [90Y]-MAURITIUS is entering the clinic for treatment of VIP/SST receptor-expressing tumours.
放射性配体 - 受体相互作用的多个方面不仅显示出某些细胞表面结合受体在人类疾病病理生理学中的重大影响:放射性配体 - 受体相互作用的概念也已扩展到临床。特别是,天然存在的肽在放射性标记后,在人类疾病的成像诊断中具有临床应用价值,并且对于使用放射性标记的肽示踪剂治疗表达某些靶受体的肿瘤具有未来意义。血管活性肠肽(VIP)和生长抑素(SST)的受体在肿瘤细胞上过度表达这一发现为这一方向带来了突破。最近的数据表明,[123I]-VIP受体闪烁扫描在体内定位小的原发性腺癌、肝转移瘤和某些胃肠道内分泌肿瘤方面具有临床应用价值。在1989年SST类似物[123I]-Tyr3-奥曲肽和[111In]-DTPA-D-Phe1-奥曲肽成功临床应用于神经内分泌肿瘤的定位诊断之后,用成本效益更高的放射性核素99mTc标记的P829如今有望成为一种潜在的用于表达SST/VIP受体肿瘤的新型诊断成像剂。此外,新型SST类似物[90Y]-MAURITIUS正在进入临床用于治疗表达VIP/SST受体的肿瘤。