AI Article Synopsis
- Nicotinamide phosphoribosyltransferase (NAMPT) plays a crucial role in recycling nicotinamide to keep NAD levels stable in cells and is seen as a potential target for cancer and inflammatory disease treatments.
- A new class of NAMPT inhibitors has been developed, with the compound 30c showing strong activity in both tumor models and significantly improving colitis in mice.
- This research suggests that NAMPT inhibitors could not only be effective against tumors but may also have new therapeutic applications, like treating inflammatory conditions.
Article Abstract
Nicotinamide phosphoribosyltransferase (NAMPT) is a key enzyme involved in the recycling of nicotinamide to maintain adequate NAD levels inside the cells. It has been postulated to be a pharmacological target, as it is overexpressed in cancer cells as well as in inflammatory diseases. We describe the synthesis and characterization of a novel class of one-digit nanomolar NAMPT inhibitors based on in vitro characterization. The most active compound tested, 30c, displayed activity in xenograft and allograft models, strengthening the potential of NAMPT inhibitors as antitumoral drugs. Furthermore, in the present contribution we describe the ability of 30c to significantly improve the outcome of colitis in mice. Given that this is the first report of an effect of NAMPT inhibitors in colitis, this result paves the way for novel applications for this class of compounds.
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| http://dx.doi.org/10.1021/acs.jmedchem.6b01392 | DOI Listing |
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