4.8 Article

A Telomerase-Specific Doxorubicin-Releasing Molecular Beacon for Cancer Theranostics

Journal

ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 55, Issue 10, Pages 3304-3308

Publisher

WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201509182

Keywords

drug delivery; molecular beacons; nanoparticles; telomerase; theranostics

Funding

  1. National Natural Science Foundation of China [NSFC 81220108012, 61335007, 81371684, 81000666, 81171395, 81328012]
  2. 973 Key Project [2015CB755504]
  3. Priority Academic Program Development of Jiangsu Higher Education

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A molecular beacon-based drug delivery system was designed for both detection of telomerase activity in living cells and telomerase-triggered drug release for precise cancer treatment. This system is composed of a gold nanoparticle core densely packed with FITC-labeled hairpin DNA sequences hybridized with telomerase primers. Molecules of the anticancer drug doxorubicin were intercalated into the stem region of the DNA sequence. The presence of telomerase will elongate the primers, leading to inner chain substitution followed by the release of the FITC fluorescence and the trapped doxorubicin. This molecular beacon could specifically distinguish tumor cells and normal cells based on telomerase activity, precisely release doxorubicin in response to telomerase activity in the tumor cells, and prevent toxicity to normal organs.

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