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Panobinostat

帕比司他
Mechanism of action:
Panobinostat 是一種組蛋白去乙醯酶抑制劑(histone deacetylase inhibitor),為異羥肟酸類(hydroxamic acid)衍生物。正常情況下,組蛋白去乙醯酶(histone deacetylase)對組蛋白去乙醯化(deacetylation),會造成染色質緊縮,基因轉錄受抑。Panobinostat 能抑制 class I、II、IV 的組蛋白去乙醯酶,使組蛋白乙醯化(acetylation)程度上升,染色質結構變得鬆散,能讓被抑制的腫瘤抑制基因重新表達。
Reference(s):
1. Qian DZ et al. (2006). Targeting tumor angiogenesis with histone deacetylase inhibitors: the hydroxamic acid derivative LBH589. Clin Cancer Res.
2. Laubach JP et al. (2015). Panobinostat for the Treatment of Multiple Myeloma. Clin Cancer Res.
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