Regulating miRNA-21 Biogenesis By Bifunctional Small Molecules.

Regulating miRNA-21 Biogenesis By Bifunctional Small Molecules.
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通过双功能小分子调节miRNA-21生物合成。

DOI:
10.1021/jacs.7b00610
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发表时间:
2017-04-12
影响因子:
15
通讯作者:
Liang FS
Liang FS
中科院分区:
化学1区
文献类型:
--
作者:
Yan H;Bhattarai U;Guo ZF;Liang FS

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We report a new strategy to regulate microRNAs (miRNAs) biogenesis by using bi-functional small molecules that consist of a pre-miRNA binding unit connected by a linker to a Dicer inhibiting unit. In this effort, fluorescence polarization-based screening was used to identify neomycin as a pre-miR-21 binding ligand. Although neomycin cannot inhibit miR-21 maturation, linking it to the RNase inhibitor 1 forms the bi-functional conjugate 7A, which inhibits the production of miR-21. We expect that this strategy will be applicable to design other molecules for miRNA regulation.
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