The overexpression of MMP-2 is a characteristic of tumor cells and therefore can be used for developing new strategies for cancer diagnosis and therapeutics. Many enzyme-responsive molecular beacons are water-soluble which can yield false signals due to nonspecific degradation. A hydrophobic quencher and a corresponding fluorophore were conjugated to a hydrophilic oligopeptide with the cleavable MMP-2 linker to create amphiphilic molecular probes. The spontaneous self-assembly of the probes into nanobeacons prevents premature degradation and promotes accumulation inside tumors by the EPR effect, with conversion back to its monomeric form triggered by dilution or pH. The beacons form nanoparticles that showed efficacy in imaging tumor cells <i>in vitro</i> and <i>ex vivo </i>after cleavage by MMP-2. The design of this molecular probe will allow for precise evaluation of tumor progression and staging.

Fluorescence imaging of tumor cells with matrix metalloproteinase-2 (MMP-2) cleavable supramolecular nanobeacons

254th National Meeting (2017)

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