Synthesis and evaluation of new iRGD peptide analogs for tumor optical imaging |
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| Authors: | Ye Yunpeng Zhu Lei Ma Ying Niu Gang Chen Xiaoyuan |
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| Institution: | Laboratory of Molecular Imaging & Nanomedicine, National Institute of Biomedical Imaging and Bioengineering, National Institutes of Health, Bethesda, MD 20892, USA |
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| Abstract: | Recently, a disulfide-based cyclic RGD peptide called iRGD, that is, 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, that is, 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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| Keywords: | iRGD peptide Integrin receptor Near-infrared fluorescent probe Optical imaging Tumor targeting |
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