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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Ye Y,Zhu L,Ma Y,Niu G,Chen X

doi

10.1016/j.bmcl.2010.12.112

subject

Has Abstract

pub_date

2011-02-15 00:00:00

pages

1146-50

issue

4

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(10)01876-7

journal_volume

21

pub_type

杂志文章

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