Medicinal Chemistry of Nicotinamide Phosphoribosyltransferase (NAMPT) Inhibitors

被引：127

作者：

Galli, Ubaldina ^{[1
]}

Travelli, Cristina ^{[1
]}

Massarotti, Alberto ^{[1
]}

Fakhfouri, Gohar ^{[2
]}

Rahimian, Reza ^{[3
]}

Tron, Gian Cesare ^{[1
]}

Genazzani, Armando A. ^{[1
]}

机构：

[1] Univ Piemonte Orientale, Dipartimento Sci Farmaco, I-28100 Novara, Italy

[2] Shahid Beheshti Univ Med Sci, Neurosci Res Ctr, Tehran, Iran

[3] Univ Tehran Med Sci, Sch Med, Dept Pharmacol, Tehran, Iran

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2013年 / 56卷 / 16期

关键词：

NAD BIOSYNTHESIS INHIBITOR; POTENT ANTITUMOR-ACTIVITY; COLONY-ENHANCING FACTOR; PHARMACOLOGICAL INHIBITION; ADENINE-DINUCLEOTIDE; METABOLIC SYNDROME; SALVAGE PATHWAY; MOLECULAR-BASIS; GASTRIC-CANCER; SERUM VISFATIN;

D O I：

10.1021/jm4001049

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：6279 / 6296

页数：18

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