1. Synthesis and evaluation of new iRGD peptide analogs for tumor optical imaging
- Author
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Ye, Yunpeng, Zhu, Lei, Ma, Ying, Niu, Gang, and Chen, Xiaoyuan
- Subjects
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BIOSYNTHESIS , *IMAGING of cancer , *NEUROPILINS , *DRUG efficacy , *PEPTIDES , *LABORATORY mice , *DRUG delivery systems , *FLUORESCENT probes , *ANTINEOPLASTIC agents , *TARGETED drug delivery - Abstract
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. [Copyright &y& Elsevier]
- Published
- 2011
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