title: Medicinal chemistry of nicotinamide phosphoribosyltransferase (NAMPT) inhibitors.
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.
authors.affiliation: Dipartimento di Scienze del Farmaco, Università degli Studi del Piemonte Orientale "A. Avogadro", Largo Donegani 2, 28100 Novara, Italy.
authors.forename: Ubaldina
authors.initials: U
authors.lastname: Galli
authors.forename: Cristina
authors.initials: C
authors.lastname: Travelli
authors.forename: Alberto
authors.initials: A
authors.lastname: Massarotti
authors.forename: Gohar
authors.initials: G
authors.lastname: Fakhfouri
authors.forename: Reza
authors.initials: R
authors.lastname: Rahimian
authors.forename: Gian Cesare
authors.initials: GC
authors.lastname: Tron
authors.forename: Armando A
authors.initials: AA
authors.lastname: Genazzani
mesh_terms: D018360:Crystallography, X-Ray; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008958:Models, Molecular; D054409:Nicotinamide Phosphoribosyltransferase / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D004791:Enzyme Inhibitors; D054409:Nicotinamide Phosphoribosyltransferase