期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 58, 期 6, 页码 1621-1625出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201809010
关键词
aptamers; cell adhesion; inhibitors; membrane proteins; molecular evolution
资金
- NSFC [21827811, 61527806, 21675120, 21804037, 21327009]
- Science and Technology Project of Hunan Province [2017XK2103]
- NIH [GM R35 127130]
- National Key R&D Program of China [2017YFA0208000]
- start-up Research Fund [531107050973, 531109010053]
- NSF [1645215]
Regulation of protein activity is essential for revealing the molecular mechanisms of biological processes. DNA and RNA achieve many uniquely efficient functions, such as genetic expression and regulation. The chemical capability to synthesize artificial nucleotides can expand the chemical space of nucleic acid libraries and further increase the functional diversity of nucleic acids. Herein, a versatile method has been developed for modular expansion of the chemical space of nucleic acid libraries, thus enabling the generation of aptamers able to regulate protein activity. Specifically, an aptamer that targets integrin alpha3 was identified and this aptamer can inhibit cell adhesion and migration. Overall, this chemical-design-assisted invitro selection approach enables the generation of functional nucleic acids for elucidating the molecular basis of biological activities and uncovering a novel basis for the rational design of new protein-inhibitor pharmaceuticals.
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