Van de Wiele C, Dumont F, van Belle S, Slegers G, Peers S H, Dierckx R A
Division of Nuclear Medicine, University Hospital Ghent, Belgium.
Nucl Med Commun. 2001 Jan;22(1):5-15. doi: 10.1097/00006231-200101000-00002.
Gastrin-releasing peptide (GRP) has been shown to be a tumour growth stimulating agent for a number of normal and human cancer cell lines. The tumour growth effect is a direct result of GRP binding to membrane G-protein coupled GRP receptors (GRP-R) on the cell surface. Available data on the role of GRP and GRP-R in human lung, prostate, breast, colorectal and gastric carcinoma are reviewed and it is suggested that radiolabelled agonists are preferable to antagonists for imaging and therapy as they appear to be internalised, yielding a higher target/background ratio. The use of rhenium or indium radiolabels for therapy may provide a new approach to GRP/bombesin expressing tumours.
胃泌素释放肽（GRP）已被证明是多种正常细胞系和人类癌细胞系的肿瘤生长刺激剂。肿瘤生长效应是GRP与细胞表面膜G蛋白偶联的GRP受体（GRP-R）结合的直接结果。本文综述了GRP和GRP-R在人类肺癌、前列腺癌、乳腺癌、结直肠癌和胃癌中的作用的现有数据，并表明放射性标记的激动剂在成像和治疗方面比拮抗剂更可取，因为它们似乎会被内化，从而产生更高的靶标/背景比。使用铼或铟放射性标记进行治疗可能为表达GRP/蛙皮素的肿瘤提供一种新的方法。
