Cargando…
Ibrutinib selectively and irreversibly targets EGFR (L858R, Del19) mutant but is moderately resistant to EGFR (T790M) mutant NSCLC Cells
Through comprehensive comparison study, we found that ibrutinib, a clinically approved covalent BTK kinase inhibitor, was highly active against EGFR (L858R, del19) mutant driven NSCLC cells, but moderately active to the T790M ‘gatekeeper’ mutant cells and not active to wild-type EGFR NSCLC cells. Ib...
Autores principales: | Wu, Hong, Wang, Aoli, Zhang, Wei, Wang, Beilei, Chen, Cheng, Wang, Wenchao, Hu, Chen, Ye, Zi, Zhao, Zheng, Wang, Li, Li, Xixiang, Yu, Kailin, Liu, Juan, Wu, Jiaxin, Yan, Xiao-E, Zhao, Peng, Wang, Jinhua, Wang, Chu, Weisberg, Ellen L., Gray, Nathanael S., Yun, Cai-Hong, Liu, Jing, Chen, Liang, Liu, Qingsong |
---|---|
Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Impact Journals LLC
2015
|
Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4741607/ https://www.ncbi.nlm.nih.gov/pubmed/26375053 |
Ejemplares similares
-
Ibrutinib targets mutant-EGFR kinase with a distinct binding conformation
por: Wang, Aoli, et al.
Publicado: (2016) -
Discovery and characterization of a novel irreversible EGFR mutants selective and potent kinase inhibitor CHMFL-EGFR-26 with a distinct binding mode
por: Hu, Chen, et al.
Publicado: (2017) -
YL143, a novel mutant selective irreversible EGFR inhibitor, overcomes EGFR(L858R, T790M)‐mutant resistance in vitro and in vivo
por: Zhang, Zhang, et al.
Publicado: (2018) -
Recruitment of hexahydroquinoline as anticancer scaffold targeting inhibition of wild and mutants EGFR (EGFR(WT), EGFR(T790M), and EGFR(L858R))
por: Abo Al-Hamd, Mahmoud G., et al.
Publicado: (2023) -
Structure-activity exploration of a small-molecule allosteric inhibitor of T790M/L858R double mutant EGFR
por: Foschi, Francesca, et al.
Publicado: (2022)