In vitro and in vivo evaluation of a 99mTc(I)-labeled bombesin analogue for imaging of gastrin releasing peptide receptor-positive tumors

In vitro and in vivo evaluation of a 99mTc(I)-labeled bombesin analogue for imaging of gastrin releasing peptide receptor-positive tumors
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DOI:
10.1016/s0969-8051(02)00314-1
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发表时间:
2002-07-01
影响因子:
3.1
通讯作者:
Schubiger, PA
Schubiger, PA
中科院分区:
医学4区
文献类型:
--
作者:
La Bella, R;Garcia-Garayoa, E;Schubiger, PA

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合成了一种新的标记蛙皮素类似物[(99 m)-Tc(I)-PADA-AVA]蛙皮素(7-14),并进行了体内外表征。在结合测定中获得高亲和力和快速内化。对胃泌素释放肽受体阳性组织的特异性结合。在携带PC-3前列腺腺癌异种移植物的CD-1 nu/nu小鼠中观察到胰腺和肿瘤。因此,我们得出结论,[Tc-99 m(I)-PADA-AVA]蛙皮素(7-14)可能具有在核医学中应用的有希望的特性,即用于诊断GRP受体过表达的肿瘤。(C)2002年爱思唯尔科技有限公司All rights reserved.
A new radiolabeled bombesin analogue, [(99m)-Tc(I)-PADA-AVA]bombesin (7-14), was synthesized and in vitro and in vivo characterized. High affinity and rapid internalization were obtained in binding assays. A specific binding towards gastrin releasing peptide receptors-positive tissues. pancreas and tumor, was observed in CD-1 nu/nu mice bearing PC-3 prostate adenocarcinoma xenografts. We therefore conclude that [Tc-99m(I)-PADA-AVA]bombesin (7-14) might have promising characteristics for applications in nuclear medicine, namely for diagnosis of GRP receptor overexpressing tumors. (C) 2002 Elsevier Science Inc. All rights reserved.