Synthesis and evaluation of new iRGD peptide analogs for tumor optical imaging.

Synthesis and evaluation of new iRGD peptide analogs for tumor optical imaging.
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肿瘤光学成像的新IRGD肽类似物的合成和评估。

DOI:
10.1016/j.bmcl.2010.12.112
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发表时间:
2011-02-15
影响因子:
2.7
通讯作者:
Chen, Xiaoyuan
Chen, Xiaoyuan
中科院分区:
医学4区
文献类型:
--
作者:
Ye, Yunpeng;Zhu, Lei;Ma, Ying;Niu, Gang;Chen, Xiaoyuan

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最近,一种基于二硫键的环状RGD肽,称为iRGD,即c(CRGDKGPDC),已被报道与整合素和神经纤毛蛋白-1受体相互作用,用于细胞和深部组织渗透,以提高成像灵敏度和治疗效果。在这项研究中,两个新的近红外荧光iRGD缀合物,即,Ac-Cys(IRDye® 800 CW)-iRGD(1)及其双标记类似物DOTA-Cys(IRDye® 800 CW)-iRGD(2)通过特异性巯基-马来酰亚胺反应合成,用于肿瘤成像。在MDA-MB-435荷瘤小鼠的光学成像中,1和2均显示出显著的肿瘤定位。这种iRGD化合物在肿瘤靶向成像和药物递送中的潜力值得进一步探索。
Recently, a disulfide-based cyclic RGD peptide called iRGD, i.e. c(CRGDKGPDC), has been reported to interact with both integrin and neuropilin-1 receptors for cellular and deep tissue penetration to improve the imaging sensitivity and therapeutic efficacy. In this study, two new near-infrared fluorescent iRGD conjugates, i.e., Ac-Cys(IRDye®800CW)-iRGD (1), and its dual labeling analog DOTA-Cys(IRDye®800CW)-iRGD (2) were synthesized via the specific mercapto-maleimide reaction for tumor imaging. Both 1 and 2 showed significant tumor localization in optical imaging of MDA-MB-435 tumor-bearing mice. The potential of such iRGD compounds in tumor-targeted imaging and drug delivery deserves further exploration.
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期刊: PROTEIN SCIENCE
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