Journal
CHEMICAL COMMUNICATIONS
Volume 59, Issue 72, Pages 10789-10792Publisher
ROYAL SOC CHEMISTRY
DOI: 10.1039/d3cc03530a
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Here, a salicylaldehyde-based reversible covalent inhibitor (A2) with moderate cellular activity against AURKA and prolonged residence time is reported. The inhibitor also shows significant non-covalent inhibition towards LRRK2. This multitarget kinase inhibitor may serve as a starting point for developing more potent, selective, and dual-targeting covalent kinase inhibitors against AURKA and LRRK2 for mitophagy.
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.
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