A5100434889- Acute Myeloid Leukemia Research
- Chronic Myeloid Leukemia Treatments
- Bioactive Compounds and Antitumor Agents
- Chronic Lymphocytic Leukemia Research
- Click Chemistry and Applications
- Protein Tyrosine Phosphatases
- Synthesis and biological activity
Jinzhou Medical University
2016-2023
Shenyang Pharmaceutical University
2016
Objective. FMS-like tyrosine kinase 3 (FLT3) is an attractive therapeutic target in acute myeloid leukemia. Unfortunately, secondary FLT3 mutations that developed resistance to inhibitors have become a severe problem. Specifically, ASP-835 (D835F/H/V/Y) mutant within the activation loop of most commonly encountered drug-resistant and observed mutations. In this study, we carried out set computational approaches explore how mutation influenced conformation dynamics DFG motif manner altered...
FMS-like tyrosine kinase (FLT3) has become the legitimate molecular therapeutic target for acute myeloid leukemia therapy. Though FLT3 inhibitors have impact on disease progression, drug resistance induced by secondary point mutations is primary mechanism and urgent to overcome. Herein, we sought decipher of HM43239 inhibiting mutant F691L resistant gilteritinib in FLT3. A series modeling studies, including dynamics (MD) simulation, dynamic cross-correlation (DCC) analysis, binding free...