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J Org Chem. 2019 May 17;84(10):6126-6133. doi: 10.1021/acs.joc.9b00331. Epub 2019 May 2.

Rational Design and Synthesis of a Metalloproteinase-Activatable Probe for Dual-Modality Imaging of Metastatic Lymph Nodes in Vivo.

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Department of Chemistry and Chemical Engineering , Jining University , Qufu 273155 , P. R. China.
Department of Nuclear Medicine , The First Affiliated Hospital of Soochow University , Suzhou 215006 , P. R. China.
Institute of Chemistry , Chinese Academy of Sciences , BeiYiJie 2, Zhong Guan Cun , Beijing 100190 , P. R. China.


Lymphatic metastasis is an important prognostic indicator for cancer progression. It is therefore considerably meaningful to develop molecularly targeted imaging probes for noninvasive and accurate identification of metastatic lymph nodes (MLNs) at early stages of tumor metastasis. Herein, we report a novel matrix metalloproteinase-2 (MMP-2)-activatable probe constructed with a near-infrared dye (Cy5), a quencher (QSY21), and a tumor-targeting peptide cRGD covalently linked through a radionuclide (125I)-labeled peptide substrate for accurate detection of MLNs. Upon cleavage with activated MMP-2, the above probe emitted MMP-2 concentration-dependent near-infrared fluorescence, which allows sensitive and specific visualization of MLNs via both optical and single-photon emission computed tomography imaging techniques. We thus envision that this probe would serve as a useful tool for studying tumor-induced lymphangiogenesis.


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