Andrej Kovacevic, Aleksandar Salim, Crisálida Borges, Patrick Meraldi and Sascha Hoogendoorn
RSC Chem. Biol., 2026, Advance Article
Abstract
Bifunctional degraders based on the PLK4 inhibitor centrinone exhibit diverging cellular profiles of stabilization through inhibition and degradation through a PROTAC-mechanism – depending on the cellular localization of PLK4.
Pengkun Sun, Cunzheng Fan, Nian Liu, Minghui Tong, Xuan Shi, Han Wang, Shuyi Mu, Ningyuan Hu, Yixiang Sun, Haoyu Zhang, Zixuan Gao, Dongmei Zhao and Maosheng Cheng
RSC Med. Chem., 2025,16, 3551-3566
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Abstract
PLK4 is a serine/threonine protein kinase situated at the centrosome, acting as a crucial regulatory element in the regulation of cell mitosis and significantly contributing to the preservation of genomic integrity.
Yanli Xue, Shuyi Mu, Pengkun Sun, Yin Sun, Nian Liu, Yu Sun, Lin Wang, Dongmei Zhao and Maosheng Cheng
RSC Med. Chem., 2023,14, 1787-1802
Abstract
A structurally novel and highly efficient PLK4 inhibitor was synthesized.
Cunzheng Fan, Nian Liu, Ningyuan Hu, Minghui Tong, Xuan Shi, Han Wang, Wenqiang Sun, Zehui Qi, Haoyu Zhang, Yixiang Sun, Zixuan Gao, Dongmei Zhao and Maosheng Cheng
RSC Med. Chem., 2025,16, 5717-5735
Abstract
Polo-like kinase 4 (PLK4), a member of the serine/threonine protein kinase family, serves as a central regulator of centriole duplication and plays a critical role in eukaryotic mitosis.
Yixiang Sun, Zixuan Gao, Ruifeng Wang, Guoqi Zhang, Tianxiao Wu, Wenbo Yin, Yin Sun, Qiaohua Qin, Dongmei Zhao and Maosheng Cheng
RSC Med. Chem., 2023,14, 2301-2314
Abstract
We designed and synthesized a series of novel diaminopyrimidine compounds as FAK inhibitors. Among them, A12 could be used as a valuable lead compound for the discovery of novel FAK-targeted anticancer drugs.