Discovery of novel BCR-ABL PROTACs based on the cereblon E3 ligase design, synthesis, and biological evaluation

Keyphrases

• E3 Ligase 100%
• BCR-ABL 100%
• Design Evaluation 100%
• Biological Evaluation 100%
• Proteolysis Targeting chimera (PROTAC) 100%
• Cereblon 100%
• Synthetic Evaluation 100%
• Degrader 80%
• Linker 40%
• Pomalidomide 40%
• Clinically Significant 20%
• Tumor Regression 20%
• Leukemia 20%
• Protein Degradation 20%
• Structure-activity Relationship Studies 20%
• Drug Development 20%
• Chronic Myeloid Leukemia 20%
• In Vitro Activity 20%
• Lenalidomide 20%
• Oncogenic Fusion Protein 20%
• Resistance mutations 20%
• Small Molecular 20%
• K562 20%
• Xenograft Tumor 20%
• Promising Strategies 20%
• Dasatinib 20%
• BCR-ABL Inhibitors 20%
• Hijacking 20%
• Carbon Chain 20%
• Extensive Structure 20%
• Potential Degradation 20%
• Degradation Performance 20%
• Pharmacokinetics in Vivo 20%
• Universal Degradation 20%
• Sulphur-substituted 20%
• Degradation Activity 20%

Pharmacology, Toxicology and Pharmaceutical Science

• Ligase 100%
• Pomalidomide 100%
• Neoplasm 50%
• Drug Development 50%
• Pharmacokinetics 50%
• Structure Activity Relationship 50%
• Tumor Regression 50%
• Leukemia 50%
• Chronic Myeloid Leukemia 50%
• Fusion Protein 50%
• Lenalidomide 50%
• Dasatinib 50%
• Sulfur 50%

Biochemistry, Genetics and Molecular Biology

• Protein Catabolism 100%
• Ligase 100%
• Cereblon 100%
• Molecular Weight 20%
• Myeloid 20%
• Structure Activity Relation 20%
• Fusion Protein 20%
• Pharmacokinetics 20%
• Dasatinib 20%