4.7 Article

Light-Trigerred Cellular Epigenetic Molecule Release To Reverse Tumor Multidrug Resistance

Journal

BIOCONJUGATE CHEMISTRY
Volume 29, Issue 4, Pages 1344-1351

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.bioconjchem.8b00073

Keywords

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Funding

  1. National Natural Science Foundation of China [51690151, 51503122, 51473093]
  2. National Basic Research Program [2015CB931801]
  3. Shanghai Rising-Star Program [17QC1401100]

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Owing to the high spatial and temporal resolution of light, light related biotechnologies, for example, optogenetics, has wide ranging applications in neuroscience to control a subject's behavior. Applying light to control tumors' genetic behavior directly was still a challenge so far. Herein, we put forward a strategy of chemical optoepigenomics, in which an epigenetic regulator (vorinostat) and paclitaxel (PTX) were conjugated onto a light-sensitive chemical molecule. The activity of vorinostat could be precisely controlled by the light, which could minimize the off-target effect. After UV irradiation under 350 nm, the photocaged epigenetic regulator (vorinostat) was selectively released from the conjugate in a spatiotemporal manner, inhibiting the activity of histone deacetylase and then reversing the PTX resistance of tumor cells effectively.

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