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

Authors :
Ye Y
Zhu L
Ma Y
Niu G
Chen X
Source :
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 Feb 15; Vol. 21 (4), pp. 1146-50. Date of Electronic Publication: 2010 Dec 28.
Publication Year :
2011

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.<br /> (Published by Elsevier Ltd.)

Details

Language :
English
ISSN :
1464-3405
Volume :
21
Issue :
4
Database :
MEDLINE
Journal :
Bioorganic & medicinal chemistry letters
Publication Type :
Academic Journal
Accession number :
21251820
Full Text :
https://doi.org/10.1016/j.bmcl.2010.12.112