Sivolapenko G B, Skarlos D, Pectasides D, Stathopoulou E, Milonakis A, Sirmalis G, Stuttle A, Courtenay-Luck N S, Konstantinides K, Epenetos A A
Encephalos Research and Therapeutic Institute, Athens, Greece.
Eur J Nucl Med. 1998 Oct;25(10):1383-9. doi: 10.1007/s002590050312.
Integrins are cell-surface glycoproteins found in different forms on all cells except erythrocytes. Integrins bind to cell adhesion molecules and to proteins found in the extracellular matrix. A tripeptidic sequence Arg-Gly-Asp (RGD) is often the primary site of recognition by integrins which are expressed on tumour cells and are responsible for tumour invasion and metastasis. A synthetic decapeptide designated alpha P2 containing two RGD sequences radiolabelled with technetium-99m was used to image malignant melanoma in vivo. Fourteen patients previously diagnosed with metastatic melanoma underwent gamma camera imaging 20-180 min following intravenous administration of the radiolabelled synthetic decapeptide alpha P2. Six out of eight (6/8) of the lymph node metastases (75%) and all other neoplastic sites (11 sites) were successfully imaged, with the exception of three sites in the mediastinal area which were not positively imaged. In two cases there was false positive uptake in the rounded pigmented areolar/nipple area. In three cases (seven sites) the peptide scan confirmed the absence of disease in suspected lesions (true-negative). The synthetic peptide was rapidly removed from the circulation by filtration through the kidneys and excretion in the urine. No toxicity or adverse events were recorded. Radiolabelled alpha P2 peptide, which binds specifically to adhesion molecules on tumours, can be used for the in vivo detection of neoplastic metastases.
整合素是一种细胞表面糖蛋白,除红细胞外,在所有细胞中均有不同形式存在。整合素可与细胞黏附分子及细胞外基质中的蛋白质结合。肿瘤细胞上表达的、负责肿瘤侵袭和转移的整合素,其识别的主要位点通常是一个三肽序列精氨酸 - 甘氨酸 - 天冬氨酸(RGD)。一种名为αP2的合成十肽含有两个用锝 - 99m标记的RGD序列,用于在体内对恶性黑色素瘤进行成像。14例先前诊断为转移性黑色素瘤的患者在静脉注射放射性标记的合成十肽αP2后20 - 180分钟接受了γ相机成像。除纵隔区域三个未呈阳性显像的部位外,8个淋巴结转移灶中的6个(6/8,75%)以及所有其他肿瘤部位(11个部位)均成功显像。在两例中,圆形色素沉着乳晕/乳头区域出现假阳性摄取。在三例(七个部位)中,肽扫描证实疑似病变无疾病(真阴性)。合成肽通过肾脏滤过并经尿液排泄迅速从循环中清除。未记录到毒性或不良事件。放射性标记的αP2肽可特异性结合肿瘤上的黏附分子,可用于体内肿瘤转移灶的检测。