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

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Light-Trigerred Cellular Epigenetic Molecule Release To Reverse Tumor Multidrug Resistance
Bioconjugate Chemistry ( IF 4.0 ) Pub Date : 2018-03-07 00:00:00 , DOI: 10.1021/acs.bioconjchem.8b00073
Leilei Shi ₁ , Li Xu ₁ , Qinghua Guan ₁ , Xin Jin ₁ , Jiapei Yang ₁ , Xinyuan Zhu ₁

Affiliation

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.

中文翻译：

光触发细胞表观遗传分子释放以逆转肿瘤多药耐药性

由于光的高空间和时间分辨率，与光有关的生物技术，例如光遗传学，在神经科学中具有广泛的应用，可以控制受试者的行为。迄今为止，直接使用光来控制肿瘤的遗传行为仍然是一个挑战。在这里，我们提出了一种化学光基因组学的策略，其中将表观遗传调节剂（伏立诺他）和紫杉醇（PTX）缀合到光敏化学分子上。伏立诺他的活性可以通过光精确地控制，这可以使脱靶效应最小化。在350 nm下紫外线照射后，以时空方式从缀合物中选择性释放光笼表观遗传调节剂（伏立诺他），抑制组蛋白脱乙酰基酶的活性，然后有效逆转肿瘤细胞对PTX的抵抗力。

更新日期：2018-03-07

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