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Neratinib

來那替尼

Mechanism of action:

Neratinib 是一種 HER 家族酪胺酸激酶抑制劑（irreversible pan-HER tyrosine kinase inhibitor）。Neratinib 能不可逆地抑制多個人類表皮生長因子受體（human epidermal growth factor receptor），例如 EGFR（epidermal growth factor receptor）和 HER2。Neratinib 能結合在這些受體的酪胺酸激酶的 ATP 結合位點，阻止受體的自我磷酸化（autophosphorylation），阻斷下游訊號傳遞，如 MAPK、PI3K/AKT，降低腫瘤細胞增殖、存活能力。

​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.

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