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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.
AuthorsYunpeng Ye, Lei Zhu, Ying Ma, Gang Niu, Xiaoyuan Chen
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 21 Issue 4 Pg. 1146-50 (Feb 15 2011) ISSN: 1464-3405 [Electronic] England
PMID21251820 (Publication Type: Journal Article, Research Support, N.I.H., Intramural)
CopyrightPublished by Elsevier Ltd.
Chemical References
  • Fluorescent Dyes
  • Heterocyclic Compounds, 1-Ring
  • Integrin alphaVbeta3
  • Oligopeptides
  • Peptides, Cyclic
  • 1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid
  • arginyl-glycyl-aspartic acid
Topics
  • Amino Acid Sequence
  • Animals
  • Fluorescent Dyes (chemistry)
  • Heterocyclic Compounds, 1-Ring (chemistry)
  • Integrin alphaVbeta3 (chemistry, metabolism)
  • Mice
  • Mice, Nude
  • Neoplasms (diagnosis)
  • Oligopeptides (chemistry)
  • Peptides, Cyclic (chemical synthesis, chemistry)
  • Positron-Emission Tomography
  • Transplantation, Heterologous

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