Yuxin Tan, Lilan Xin, Qian Wang, Rong Xu, Xiqin Tong, Guopeng Chen, Linlu Ma, Fuwei Yang, Hongqiang Jiang, Nan Zhang, Jinxian Wu, Xinqi Li, Xinyi Guo, Chao Wang, Haibing Zhou, Fuling Zhou
Acute myeloid leukemia (AML) patients carrying Fms-like tyrosine kinase 3-internal tandem duplication (FLT3-ITD) mutations often face a poor prognosis. While some FLT3 inhibitors have been used clinically, challenges such as short efficacy and poor specificity persist. Proteolytic targeting chimera (PROTAC), with its lower ligand affinity requirement for target proteins, offers higher and rapid targeting capability. Gilteritinib, used as the ligand for the target protein, was connected with different E3 ligase ligands to synthesize several series of PROTAC targeting FLT3-ITD...
May 3, 2024: Cancer Letters