Identification of the Raf kinase inhibitor TAK‐632 and its analogues as potent inhibitors of necroptosis by targeting RIPK1 and RIPK3

Background and Purpose Necroptosis is a form of programmed, caspase‐independent, cell death, mediated by receptor‐interacting protein kinases, RIPK1 and RIPK3, and the mixed lineage kinase domain‐like (MLKL). Necroptosis contributes to the pathophysiology of various inflammatory, infectious, and deg...

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Veröffentlicht in:	British journal of pharmacology 2019-06, Vol.176 (12), p.2095-2108
Hauptverfasser:	Chen, Xiaofei, Zhuang, Chunlin, Ren, Yibin, Zhang, Hao, Qin, Xia, Hu, Longmiao, Fu, Jing, Miao, Zhenyuan, Chai, Yifeng, Liu, Zheng‐gang, Zhang, Haibing, Cai, Zhenyu, Wang, Hong‐yang
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Apoptosis Assaying Benzothiazoles - administration & dosage Benzothiazoles - chemistry Benzothiazoles - pharmacology Caspase Cell death Cell Survival - drug effects Cell viability Cells, Cultured Degenerative diseases Dose-Response Relationship, Drug Drug Evaluation, Preclinical Enzyme inhibitors Female HEK293 Cells HT29 Cells Humans Immunoprecipitation Inflammatory response Inhibitors Kinases Lead compounds MAP kinase Mice Mice, Inbred C57BL Molecular Structure Necroptosis Necroptosis - drug effects Nitriles - administration & dosage Nitriles - chemistry Nitriles - pharmacology Pathophysiology Protein Kinase Inhibitors - administration & dosage Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Raf protein Receptor-Interacting Protein Serine-Threonine Kinases - antagonists & inhibitors Receptor-Interacting Protein Serine-Threonine Kinases - metabolism Research Paper Research Papers Signal transduction Structure-Activity Relationship Systemic inflammatory response syndrome Tumor necrosis factor Western blotting
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