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可见光诱导配体结合模式切换表明 G-四链体 DNA 是光药理的靶点。

Visible-light photoswitching of ligand binding mode suggests G-quadruplex DNA as a target for photopharmacology.

机构信息

School of Chemistry, University of Bristol, Cantock's Close, Bristol BS81TS, UK.

出版信息

Chem Commun (Camb). 2020 May 11;56(38):5186-5189. doi: 10.1039/d0cc01581d. Epub 2020 Apr 8.

Abstract

We report the selective targeting of telomeric G4 DNA with a dithienylethene ligand and demonstrate the robust visible-light mediated switching of the G4 ligand binding mode and G-tetrad structure in physiologically-relevant conditions. The toxicity of the ligand to cervical cancer cells is modulated by the photoisomeric state of the ligand, indicating for the first time the potential of G4 to serve as a target for photopharmacological strategies.

摘要

我们报告了一种二噻吩乙烯配体对端粒 G4 DNA 的选择性靶向,并在生理相关条件下证明了 G4 配体结合模式和 G-四联体结构的强可见光介导切换。配体对宫颈癌细胞的毒性受配体光异构体状态的调节,这首次表明 G4 作为光药理策略靶标的潜力。

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