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Thalidomide

沙利度胺
Mechanism of action:
Thalidomide 是一種免疫調節劑(immunomodulatory agent)。Thalidomide 會與 CRBN 蛋白(cereblon)結合,改變 CRL4(CRBN) 泛素化複合體的受質選擇性,影響特定轉錄因子與調控蛋白的穩定性,進而抑制促發炎細胞激素,例如 TNF-α 的生成;提升 IL-2、IFN-γ 的產生等等。
Reference(s):
1. Eriksson T et al. (2001). Clinical pharmacology of thalidomide. Eur J Clin Pharmacol.
2. Kronke J et al. (2014). Lenalidomide causes selective degradation of IKZF1 and IKZF3 in multiple myeloma cells. Science.
3. Lepper ER et al. (2006). Thalidomide metabolism and hydrolysis: mechanisms and implications. Curr Drug Metab.
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