Synthesis of dimeric cyclic RGD based near-infrared probe for in vivo tumor diagnosis

Jie Cao; Shunan Wan; Junmei Tian; Xuemei Chi; Changli Du; Dawei Deng; Wei R. Chen; Yueqing Gu

doi:10.1117/12.907567

15 February 2012 Synthesis of dimeric cyclic RGD based near-infrared probe for in vivo tumor diagnosis

Jie Cao, Shunan Wan, Junmei Tian, Xuemei Chi, Changli Du, Dawei Deng, Wei R. Chen, Yueqing Gu

Proceedings Volume 8224, Biophotonics and Immune Responses VII; 82240T (2012) https://doi.org/10.1117/12.907567
Event: SPIE BiOS, 2012, San Francisco, California, United States

Abstract

Cell adhesion molecule integrin α_vβ₃ 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.

Citation Download Citation

Jie Cao, Shunan Wan, Junmei Tian, Xuemei Chi, Changli Du, Dawei Deng, Wei R. Chen, and Yueqing Gu "Synthesis of dimeric cyclic RGD based near-infrared probe for in vivo tumor diagnosis", Proc. SPIE 8224, Biophotonics and Immune Responses VII, 82240T (15 February 2012); https://doi.org/10.1117/12.907567

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