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

• Main Authors: Jia-Luo Huang (Author), Xue-Long Yan (Author), Dong Huang (Author), Lu Gan (Author), Huahua Gao (Author), Run-Zhu Fan (Author), Shen Li (Author), Fang-Yu Yuan (Author), Xinying Zhu (Author), Gui-Hua Tang (Author), Hong-Wu Chen (Author), Junjian Wang (Author), Sheng Yin (Author)
• Format: Book
• Published: Elsevier, 2023-12-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

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...