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

Chem Commun (Camb). 2023 Sep 7;59(72):10789-10792. doi: 10.1039/d3cc03530a.

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.

MeSH terms

  • Aurora Kinase A*
  • Mitophagy*
  • Protein Kinase Inhibitors / pharmacology

Substances

  • Aurora Kinase A
  • Protein Kinase Inhibitors