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Erlotinib

厄洛替尼

Mechanism of action:

Erlotinib 是一種表皮生長因子受體酪胺酸激酶抑制劑(epidermal growth factor receptor tyrosine kinase inhibitor)。當表皮生長因子與表皮生長因子受體結合,會活化下游多條訊息路徑,比如 PI3K-AKT-mTOR、RAS-RAF-MEK-ERK、JAK-STAT,刺激細胞增殖與存活等。Erlotinib 能夠抑制表皮生長因子受體的酪胺酸激酶活性區,阻止訊息傳遞產生,使腫瘤細胞生長與存活相關訊號下降,導致細胞週期停滯、凋亡增加與增殖能力降低。

​Reference(s):

1. Raymond E et al. (2000). Epidermal growth factor receptor tyrosine kinase as a target for anticancer therapy. Drugs. 


2. Li Z et al. (2007). Erlotinib effectively inhibits JAK2V617F activity and polycythemia vera cell growth. J Biol Chem.

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