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

Authors :
Wang, Wei
Wang, Xuan
Tang, Guanghui
Zhu, Chengjun
Xiang, Menghua
Xiao, Qicai
Zhang, Zhi-Min
Gao, Liqian
Yao, Shao Q.
Source :
Chemical Communications. 9/16/2023, Vol. 59 Issue 72, p10789-10792. 4p.
Publication Year :
2023

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. [ABSTRACT FROM AUTHOR]

Details

Language :
English
ISSN :
13597345
Volume :
59
Issue :
72
Database :
Academic Search Index
Journal :
Chemical Communications
Publication Type :
Academic Journal
Accession number :
171807655
Full Text :
https://doi.org/10.1039/d3cc03530a