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

Aurora Kinase A Mitophagy Protein Kinase Inhibitors / pharmacology

Journal

Chemical communications (Cambridge, England)
ISSN: 1364-548X
Titre abrégé: Chem Commun (Camb)
Pays: England
ID NLM: 9610838

Informations de publication

Date de publication:
07 Sep 2023
Historique:
medline: 8 9 2023
pubmed: 18 8 2023
entrez: 18 8 2023
Statut: epublish

Résumé

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.

Identifiants

DOI: 10.1039/d3cc03530a PMID: 37594149
pubmed: 37594149
doi: 10.1039/d3cc03530a
doi:

Substances chimiques

Aurora Kinase A EC 2.7.11.1
Protein Kinase Inhibitors 0

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

10789-10792

Auteurs

Wei Wang (W)

School of Pharmaceutical Sciences (Shenzhen), Shenzhen Campus of Sun Yat-sen University, Shenzhen 518000, China. gaolq@mail.sysu.edu.cn.
Department of Chemistry, National University of Singapore, Singapore 117543, Singapore. chmyaosq@nus.edu.sg.

Xuan Wang (X)

School of Pharmaceutical Sciences (Shenzhen), Shenzhen Campus of Sun Yat-sen University, Shenzhen 518000, China. gaolq@mail.sysu.edu.cn.

Guanghui Tang (G)

Department of Chemistry, National University of Singapore, Singapore 117543, Singapore. chmyaosq@nus.edu.sg.

Chengjun Zhu (C)

School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China. 13632107756@163.com.

Menghua Xiang (M)

School of Pharmaceutical Sciences (Shenzhen), Shenzhen Campus of Sun Yat-sen University, Shenzhen 518000, China. gaolq@mail.sysu.edu.cn.

Qicai Xiao (Q)

School of Pharmaceutical Sciences (Shenzhen), Shenzhen Campus of Sun Yat-sen University, Shenzhen 518000, China. gaolq@mail.sysu.edu.cn.

Zhi-Min Zhang (ZM)

School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China. 13632107756@163.com.

Liqian Gao (L)

School of Pharmaceutical Sciences (Shenzhen), Shenzhen Campus of Sun Yat-sen University, Shenzhen 518000, China. gaolq@mail.sysu.edu.cn.

Shao Q Yao (SQ)

Department of Chemistry, National University of Singapore, Singapore 117543, Singapore. chmyaosq@nus.edu.sg.
ORCID: 0000-0003-4715-769X

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Classifications MeSH

questionsmedicales.fr › Acides aminés, peptides et protéines › Protéines › Protéines et peptides de signalisation intracellulaire › Protein-Serine-Threonine Kinases › Aurora kinases › Aurora kinase A › Multitarget inhibitors/probes that target...
questionsmedicales.fr › Phénomènes physiologiques cellulaires › Renouvellement des mitochondries › Dégradation des mitochondries › Multitarget inhibitors/probes that target...
questionsmedicales.fr › Actions chimiques et utilisations › Actions pharmacologiques › Mécanismes moléculaires de l'action pharmacologique › Antienzymes › Inhibiteurs de protéines kinases › Multitarget inhibitors/probes that target...