bibw-2992 has been researched along with Leukemia--Promyelocytic--Acute* in 1 studies
1 other study(ies) available for bibw-2992 and Leukemia--Promyelocytic--Acute
| Article | Year |
|---|---|
Discovery of Novel Benzothiazepinones as Irreversible Covalent Glycogen Synthase Kinase 3β Inhibitors for the Treatment of Acute Promyelocytic Leukemia.
Recently, irreversible inhibitors have attracted great interest in antitumors due to their advantages of forming covalent bonds to target proteins. Herein, some benzothiazepinone compounds (BTZs) have been designed and synthesized as novel covalent GSK-3β inhibitors with high selectivity for the kinase panel. The irreversible covalent binding mode was identified by kinetics and mass spectrometry, and the main labeled residue was confirmed to be the unique Cys14 that exists only in GSK-3β. The candidate Topics: Animals; Apoptosis; Benzothiazoles; Cell Line, Tumor; Cell Proliferation; Female; Glycogen Synthase Kinase 3 beta; Half-Life; Humans; Isoenzymes; Kinetics; Leukemia, Promyelocytic, Acute; Male; Mice; Mice, Inbred ICR; Mice, Nude; Protein Kinase Inhibitors; Structure-Activity Relationship; Xenograft Model Antitumor Assays | 2021 |