Medicinal Chemistry of Nicotinamide Phosphoribosyltransferase (NAMPT) Inhibitors
Medicinal Chemistry of Nicotinamide Phosphoribosyltransferase (NAMPT) Inhibitors
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DOI：
10.1021/jm4001049
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发表时间：
2013-08-22
影响因子：
7.3
通讯作者：
Genazzani, Armando A.
中科院分区：
文献类型：
--
作者：
Galli, Ubaldina;Travelli, Cristina;Genazzani, Armando A.
烟酰胺磷酸核糖转移酶（NAMPT）在细胞内NAD库的补充中起着关键作用。这反过来又使这种酶在生物能量学和调节NAD使用酶（如PARP和sirtuins）中发挥重要作用。此外，现在有充分的证据表明NAMPT是分泌的，并具有细胞因子的作用。NAMPT的细胞内或细胞外形式的重要作用已在癌症、炎症和代谢疾病中显示。第一个NAMPT抑制剂（FK866和CHS828）已经进入临床试验，对合成新分子的兴趣激增。本文综述了这一领域的最新进展。
Nicotinamide phoshophoribosyltransferase (NAMPT) plays a key role in the replenishment of the NAD pool in cells. This in turn makes this enzyme an important player in bioenergetics and in the regulation of NAD-using enzymes, such as PARPs and sirtuins. Furthermore, there is now ample evidence that NAMPT is secreted and has a role as a cytokine. An important role of either the intracellular or extracellular form of NAMPT has been shown in cancer, inflammation, and metabolic diseases. The first NAMPT inhibitors (FK866 and CHS828) have already entered clinical trials, and a surge in interest in the synthesis of novel molecules has occurred. The present review summarizes the recent progress in this field.