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Carfilzomib

卡非佐米

Mechanism of action:

Carfilzomib 是一種第二代蛋白酶體抑制劑(proteasome inhibitor),屬於環氧酮肽類(epoxyketone peptide)。Carfilzomib 會與 26S 蛋白酶體的 β5 亞基結合並不可逆地抑制其活性,導致錯誤蛋白無法被分解而累積,誘發內質網壓力(ER stress) 與凋亡途徑啟動。

​Reference(s):

1. Kortuem KM et al. (2013). Carfilzomib. Blood. 


2. Kuhn DJ et al. (2007). Potent activity of carfilzomib, a novel, irreversible inhibitor of the ubiquitin-proteasome pathway, against preclinical models of multiple myeloma. Blood.

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