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Light-Trigerred Cellular Epigenetic Molecule Release To Reverse Tumor Multidrug Resistance.
Bioconjugate Chemistry 2018 April 19
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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