期刊
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
卷 144, 期 4, 页码 1493-1497出版社
AMER CHEMICAL SOC
DOI: 10.1021/jacs.1c09574
关键词
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资金
- National Key Research and Development Program of China [2018YFA0902600, 2018YFC1106102]
- National Natural Science Foundation of China [51973112, 51690151, 22175116, 21805129, 21905170]
- Science Foundation of The Shanghai Municipal Science and Technology Commission [18JC1410800, 19JC1410300]
Aptamer-drug conjugates (ApDCs) are a promising drug delivery system for targeted cancer therapy. However, the conventional ApDC has limited drug loading capacity. To address this challenge, researchers have developed drugtamers, whole drug-constituted DNA-like oligomers, which have 100% drug loading ratio, active targeting capability, and enzyme-mediated release of active therapeutics.
Owing to the specific and high binding affinity of aptamers to their targets, aptamer-drug conjugates (ApDCs) have emerged as a promising drug delivery system for targeted cancer therapy. However, in a conventional ApDC, the aptamer segment usually just serves as a targeting moiety, and only a limited number of drug molecules are sequentially conjugated to the oligonucleotide, giving a relatively low drug loading capacity. To address this challenge, herein we employ four clinically approved nucleoside analogues, including clofarabine (Clo), ara-guanosine (AraG), gemcitabine (Ge), and floxuridine (FdU), to replace all natural nucleosides in aptamer sequences, generating a series of whole drug-constituted DNA-like oligomers that are termed drugtamers. Similar to their parent aptamers, the obtained drugtamers maintain the targeting capability and can specifically bind to the target receptors overexpressed on the cancer cell surface. With 100% drug loading ratio, active targeting capability, and enzyme-mediated release of active therapeutics, our drugtamers can strongly induce the apoptosis of cancer cells and inhibit the tumor progression, which enables a new potential for a better targeted cancer therapy.
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