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Synthesis and evaluation of new iRGD peptide analogs for tumor optical imaging.
- 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.)
- Subjects :
- Amino Acid Sequence
Animals
Fluorescent Dyes chemistry
Heterocyclic Compounds, 1-Ring chemistry
Integrin alphaVbeta3 chemistry
Integrin alphaVbeta3 metabolism
Mice
Mice, Nude
Peptides, Cyclic chemistry
Positron-Emission Tomography
Transplantation, Heterologous
Neoplasms diagnosis
Oligopeptides chemistry
Peptides, Cyclic chemical synthesis
Subjects
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