期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 61, 期 33, 页码 -出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.202109500
关键词
aptamers; antitumor agents; cancer; drug delivery; oligonucleotides
资金
- National Key R&D Program of China [2018YFA0902300]
- NSFC [21827811, 91753109]
- Huxiang Young Talent Program from Hunan Province [2019RS2022]
- Science and Technology Innovation Program of Hunan Province [2020RC2022]
This study describes the development of a novel dual-targeting circular aptamer that can recognize two different biomarkers on living cells, enhancing the recognition of target cells. This improvement not only boosts the binding and internalization abilities of the aptamer, but also expands its recognition spectrum to different leukemia cells.
Currently, the broad use of monovalent aptamers in oncology faces challenges, including insufficient recognition and internalization caused by a finite number of receptors on the cell surface, as well as a confined recognition spectrum. Herein, we describe the development of a dual-targeting circular aptamer (DTCA) that can recognize two different biomarkers on living cells to augment aptamer-receptor interactions, thus enhancing recognition of the target cells. This improvement not only boosts binding and internalization abilities, but also expands the recognition spectrum of these aptamers to different leukemia cells. Moreover, the stability of DTCA in serum can be significantly improved by an enzyme-promoted terminal ligation strategy. The chemical incorporation of 5-fluorodeoxyuridine into DTCA resulted in a pharmaceutically functional aptamer that exhibited excellent selectivity, as demonstrated by its high cytotoxicity against target cancer cells, but not to normal cells. The superiority of our newly developed strategy was further highlighted by its precise tumor-imaging capability.
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