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

✍ Scribed by Yunpeng Ye; Lei Zhu; Ying Ma; Gang Niu; Xiaoyuan Chen

• Book ID: 104005279
• Publisher: Elsevier Science
• Year: 2011
• Tongue: English
• Weight: 635 KB
• Volume: 21
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/j.bmcl.2010.12.112

✦ Synopsis

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 Ò 800CW)-iRGD (1), and its dual labeling analog DOTA-Cys(IR-Dye Ò 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 tumorbearing mice. The potential of such iRGD compounds in tumor-targeted imaging and drug delivery deserves further exploration.