Discovery of a highly potent and orally available importin-β1 inhibitor that overcomes enzalutamide-resistance in advanced prostate cancer

• Главные авторы: Jia-Luo Huang (Автор), Xue-Long Yan (Автор), Dong Huang (Автор), Lu Gan (Автор), Huahua Gao (Автор), Run-Zhu Fan (Автор), Shen Li (Автор), Fang-Yu Yuan (Автор), Xinying Zhu (Автор), Gui-Hua Tang (Автор), Hong-Wu Chen (Автор), Junjian Wang (Автор), Sheng Yin (Автор)
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• Опубликовано: Elsevier, 2023-12-01T00:00:00Z.
• Предметы: article
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Nuclear transporter importin-β1 is emerging as an attractive target by virtue of its prevalence in many cancers. However, the lack of druggable inhibitors restricts its therapeutic proof of concept. In the present work, we optimized a natural importin-β1 inhibitor DD1 to afford an improved analog DD...