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Nicotinamide Phosphoribosyltransferase (NAMPT) Is a New Target of Antitumor Agent Chidamide.
ACS Medicinal Chemistry Letters ( IF 4.2 ) Pub Date : 2019-12-13 , DOI: 10.1021/acsmedchemlett.9b00407
Ying Wu 1 , Lei Wang 1 , Yahui Huang 1 , Shuqiang Chen 1 , Shanchao Wu 1 , Guoqiang Dong 1 , Chunquan Sheng 1, 2
Affiliation  

Chidamide is a histone deacetylase (HDAC) inhibitor that is currently used to treat cutaneous T-cell lymphoma in clinic. Herein nicotinamide phosphoribosyltransferase (NAMPT) was identified to be a new target of chidamide on the basis of the pharmacophore analysis, molecular docking, biological assays, inhibitor design, and structure-activity relationship study. The polypharmacology of chidamide will provide important information for better understanding its antitumor mechanism. Also, design of dual NAMPT/HDAC inhibitors may serve as an effective strategy to develop novel antitumor agents.

中文翻译:

烟酰胺磷酸核糖基转移酶(NAMPT)是抗肿瘤药物Chidamide的新目标。

Chidamide是一种组蛋白脱乙酰基酶(HDAC)抑制剂,目前在临床上用于治疗皮肤T细胞淋巴瘤。在此,基于药效团分析,分子对接,生物学分析,抑制剂设计和结构-活性关系研究,烟酰胺磷酸核糖基转移酶(NAMPT)被确定为几丁质的新靶标。Chidamide的多药理学将为更好地了解其抗肿瘤机制提供重要信息。而且,双重NAMPT / HDAC抑制剂的设计可以作为开发新型抗肿瘤剂的有效策略。
更新日期:2019-12-23
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