Irreversible inhibition of BTK kinase by a novel highly selective inhibitor CHMFL-BTK-11 suppresses inflammatory response in rheumatoid arthritis model
Abstract BTK plays a critical role in the B cell receptor mediated inflammatory signaling in the rheumatoid arthritis (RA). Through a rational design approach we discovered a highly selective and potent BTK kinase inhibitor (CHMFL-BTK-11) which exerted its inhibitory efficacy through a covalent bond...
Guardado en:
Autores principales: | Hong Wu, Qiong Huang, Ziping Qi, Yongfei Chen, Aoli Wang, Cheng Chen, Qianmao Liang, Jinghua Wang, Wensheng Chen, Jin Dong, Kailin Yu, Chen Hu, Wenchao Wang, Xiaochuan Liu, Yuanxin Deng, Li Wang, Beilei Wang, Xiaoxiang Li, Nathanael S. Gray, Jing Liu, Wei Wei, Qingsong Liu |
---|---|
Formato: | article |
Lenguaje: | EN |
Publicado: |
Nature Portfolio
2017
|
Materias: | |
Acceso en línea: | https://doaj.org/article/ace32d39a1da436aaa24ae8fb665ca2d |
Etiquetas: |
Agregar Etiqueta
Sin Etiquetas, Sea el primero en etiquetar este registro!
|
Ejemplares similares
-
Clonal evolution in patients with chronic lymphocytic leukaemia developing resistance to BTK inhibition
por: Jan A. Burger, et al.
Publicado: (2016) -
Monitoring and Managing BTK Inhibitor Treatment-Related Adverse Events in Clinical Practice
por: Susan M. O’Brien, et al.
Publicado: (2021) -
Target modulation and pharmacokinetics/pharmacodynamics translation of the BTK inhibitor poseltinib for model-informed phase II dose selection
por: Joo-Yun Byun, et al.
Publicado: (2021) -
Cooperative miRNA-dependent PTEN regulation drives resistance to BTK inhibition in B-cell lymphoid malignancies
por: Isha Kapoor, et al.
Publicado: (2021) -
Btk SH2-kinase interface is critical for allosteric kinase activation and its targeting inhibits B-cell neoplasms
por: Daniel P. Duarte, et al.
Publicado: (2020)