School of Pharmaceutical Sciences (Shenzhen), Shenzhen Campus of Sun Yat-sen University, Shenzhen 518000, China.
Department of Chemistry, National University of Singapore, Singapore 117543, Singapore.
Chem Commun (Camb). 2023 Sep 7;59(72):10789-10792. doi: 10.1039/d3cc03530a.
Herein, we report a salicylaldehyde-based, reversible covalent inhibitor (A2) that possesses moderate cellular activity against AURKA with a prolonged residence time and shows significant non-covalent inhibition towards LRRK2. Our results indicated that this multitarget kinase inhibitor may be used as the starting point for future development of more potent, selective and dual-targeting covalent kinase inhibitors against AURKA and LRRK2 for mitophagy.
在此，我们报告了一种基于水杨醛的、可逆的共价抑制剂（A2），它对 AURKA 具有中等的细胞活性，停留时间长，并对 LRRK2 表现出显著的非共价抑制作用。我们的研究结果表明，这种多靶点激酶抑制剂可能可作为进一步开发针对 AURKA 和 LRRK2 的更有效、更选择性和双靶向共价激酶抑制剂用于线粒体自噬的起点。
