Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10595573 | Bioorganic & Medicinal Chemistry Letters | 2013 | 5 Pages |
Abstract
Retinoid X receptor (RXR) and Histone deacetylase (HDAC) are considered important targets for anti-cancer therapy due to their crucial roles in genetic or epigenetic regulations of cancer development and progression. Here, we have designed and synthesized a novel compound which targets both RXR and HADC. This dual-targeting agent is derived from bexarotene and suberoylanilide hydroxamic acid (SAHA), prototypical RXR agonist and HDAC inhibitor, respectively. Molecular docking studies demonstrate that this agent has a relatively strong affinity to RXR and HADC. Importantly, it presents the potentials of activation of RXR and inhibition of HDAC in both cell-free and whole-cell assays, and displays anti-proliferative effect on representative cancer cell lines and drug-resistant cancer cell lines.
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Authors
Guo-Liang Chen, Li-Hui Wang, Jian Wang, Kang Chen, Man Zhao, Zhao-Zhu Sun, Shuang Wang, Hong-Li Zheng, Jing-Yu Yang, Chun-Fu Wu,