Medicinal chemistry of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors

Ubaldina Galli, Cristina Travelli, Alberto Massarotti, Gohar Fakhfouri, Reza Rahimian, Gian Cesare Tron, Armando A. Genazzani

Research output: Contribution to journalReview articlepeer-review

Abstract

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.

Original languageEnglish
Pages (from-to)6279-6296
Number of pages18
JournalJournal of Medicinal Chemistry
Volume56
Issue number16
DOIs
Publication statusPublished - 22 Aug 2013

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