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Multitarget inhibitors/probes that target LRRK2 and AURORA A kinases noncovalently and covalently.
Wang, Wei; Wang, Xuan; Tang, Guanghui; Zhu, Chengjun; Xiang, Menghua; Xiao, Qicai; Zhang, Zhi-Min; Gao, Liqian; Yao, Shao Q.
Afiliação
  • Wang W; School of Pharmaceutical Sciences (Shenzhen), Shenzhen Campus of Sun Yat-sen University, Shenzhen 518000, China. gaolq@mail.sysu.edu.cn.
  • Wang X; Department of Chemistry, National University of Singapore, Singapore 117543, Singapore. chmyaosq@nus.edu.sg.
  • Tang G; School of Pharmaceutical Sciences (Shenzhen), Shenzhen Campus of Sun Yat-sen University, Shenzhen 518000, China. gaolq@mail.sysu.edu.cn.
  • Zhu C; Department of Chemistry, National University of Singapore, Singapore 117543, Singapore. chmyaosq@nus.edu.sg.
  • Xiang M; School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China. 13632107756@163.com.
  • Xiao Q; School of Pharmaceutical Sciences (Shenzhen), Shenzhen Campus of Sun Yat-sen University, Shenzhen 518000, China. gaolq@mail.sysu.edu.cn.
  • Zhang ZM; School of Pharmaceutical Sciences (Shenzhen), Shenzhen Campus of Sun Yat-sen University, Shenzhen 518000, China. gaolq@mail.sysu.edu.cn.
  • Gao L; School of Pharmacy, Jinan University, 601 Huangpu Avenue West, Guangzhou 510632, China. 13632107756@163.com.
  • Yao SQ; School of Pharmaceutical Sciences (Shenzhen), Shenzhen Campus of Sun Yat-sen University, Shenzhen 518000, China. gaolq@mail.sysu.edu.cn.
Chem Commun (Camb) ; 59(72): 10789-10792, 2023 Sep 07.
Article em En | MEDLINE | ID: mdl-37594149
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.
Assuntos

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Mitofagia / Aurora Quinase A Idioma: En Revista: Chem Commun (Camb) Assunto da revista: QUIMICA Ano de publicação: 2023 Tipo de documento: Article País de afiliação: China

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Mitofagia / Aurora Quinase A Idioma: En Revista: Chem Commun (Camb) Assunto da revista: QUIMICA Ano de publicação: 2023 Tipo de documento: Article País de afiliação: China