Issue 72, 2023

Multitarget inhibitors/probes that target LRRK2 and AURORA A kinases noncovalently and covalently

Abstract

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.

Graphical abstract: Multitarget inhibitors/probes that target LRRK2 and AURORA A kinases noncovalently and covalently

Supplementary files

Article information

Article type
Communication
Submitted
22 Jul 2023
Accepted
04 Aug 2023
First published
07 Aug 2023

Chem. Commun., 2023,59, 10789-10792

Multitarget inhibitors/probes that target LRRK2 and AURORA A kinases noncovalently and covalently

W. Wang, X. Wang, G. Tang, C. Zhu, M. Xiang, Q. Xiao, Z. Zhang, L. Gao and S. Q. Yao, Chem. Commun., 2023, 59, 10789 DOI: 10.1039/D3CC03530A

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