The Sound of Evolution
Neratinib
Mechanism of action:
Neratinib is an irreversible pan-HER tyrosine kinase inhibitor. Neratinib irreversibly inhibits multiple human epidermal growth factor receptors, such as EGFR and HER2. Neratinib binds to the ATP-binding site of the tyrosine kinase domain of these receptors, preventing receptor autophosphorylation and blocking downstream signaling pathways such as MAPK and PI3K/AKT, thereby reducing tumor cell proliferation and survival.
Reference(s):
1. Zhou Y et al. (2024). TTD: Therapeutic Target Database describing target druggability information. Nucleic Acids Res.
2. Lategahn J et al. (2020). Targeting Her2-insYVMA with Covalent Inhibitors-A Focused Compound Screening and Structure-Based Design Approach. J Med Chem.
3. Liu T et al. (2025). BindingDB in 2024: a FAIR knowledgebase of protein-small molecule binding data. Nucleic Acids Res.