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Bortezomib

硼替佐米
Mechanism of action:
Bortezomib 是一種可逆性蛋白酶體抑制劑(reversible proteasome inhibitor)。由於腫瘤細胞依賴 26S 蛋白酶體(26S proteasome)系統清除錯誤摺疊或調節蛋白以維持快速生長,bortezomib 可逆性地結合 26S 蛋白酶體 β5 亞基,導致錯誤摺疊的蛋白累積,觸發內質網壓力(ER stress),使細胞週期停滯(G₂/M phase arrest),並啟動細胞凋亡相關路徑。
Reference(s):
1. Voorhees PM et al. (2003). The proteasome as a target for cancer therapy. Clin Cancer Res.
2. Adams J et al. (1999). Proteasome inhibitors: a novel class of potent and effective antitumor agents. Cancer Res.
3. Berkers CR et al. (2005). Activity probe for in vivo profiling of the specificity of proteasome inhibitor bortezomib. Nat Methods.
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