Angewandte Chemie (International ed. in English) · 2022
A Long-Circulating Vector for Aptamers Based upon Polyphosphodiester-Backboned Molecular Brushes.
СтатьяПоддержка правительства СШАПоддержка NIH: внешняя программаНазвание и аннотация: Перевод в очереди
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Wang Yuyan, Wang Dali, Lin Jiachen, Lyu Zidi, Chen Peiru, Sun Tingyu, Xue Chenyang, Mojtabavi Mehrnaz, Vedadghavami Armin, Zhang Zheyu, Wang Ruimeng, Zhang Lei, Park Christopher, Heo Gyu Seong, Liu Yongjian, Dong Sijia S, Zhang Ke
Аннотация
Aptamers face challenges for use outside the ideal conditions in which they are developed. These difficulties are most palpable in vivo due to nuclease activities, rapid clearance, and off-target binding. Herein, we demonstrate that a polyphosphodiester-backboned molecular brush can suppress enzymatic digestion, reduce non-specific cell uptake, enable long blood circulation, and rescue the bioactivity of a conjugated aptamer in vivo. The backbone along with the aptamer is assembled via solid-phase synthesis, followed by installation of poly(ethylene glycol) (PEG) side chains using a two-step process with near-quantitative efficiency. The synthesis allows for precise control over polymer size and architecture. Consisting entirely of building blocks that are generally recognized as safe for therapeutics, this novel molecular brush is expected to provide a highly translatable route for aptamer-based therapeutics.