Synthesis of dimeric cyclic RGD based near-infrared probe for in vivo tumor diagnosis
2012
Cell adhesion molecule integrin α v β 3 is an excellent target for tumor interventions because of its unique
expression on the surface of several types of solid tumor cells and on almost all sprouting tumor vasculatures. In this
manuscript, we describe the synthesis of near-infrared (NIR) fluorochrome ICG-Der-02-labeled dimeric cyclic RGD
peptides (ICG-Der-02-c(RGDyK) 2 ) for in vivo tumor integrin targeting. The optical properties and structure of the probe
were intensively characterized. Afterwards, the integrin specificity of the fluorescent probe was tested in vitro for
receptor binding assay and fluorescence microscopy and in vivo for subcutaneous MDA-MB-231 and U87MG tumor
targeting. The results indicated that after labeling RGD peptide, the optical properties of ICG-Der-02 showed no obvious
change. Besides, in vitro and in vivo tumor targeting experiment indicated that the ICG-Der-02-c(RGDyK) 2 probe with
high integrin affinity showed excellent tumor activity accumulation. Noninvasive NIR fluorescence imaging is able to
detect tumor integrin expression based upon the highly potent RGD peptide probe.
Keywords:
- Correction
- Source
- Cite
- Save
- Machine Reading By IdeaReader
0
References
1
Citations
NaN
KQI