Boosting NAD with a small molecule that activates NAMPT
Nature Communications, ISSN: 2041-1723, Vol: 10, Issue: 1, Page: 3241
2019
- 116Citations
- 144Captures
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Example: if you select the 1-year option for an article published in 2019 and a metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019. If you select the 3-year option for the same article published in 2019 and the metric category shows 90%, that means that the article or review is performing better than 90% of the other articles/reviews published in that journal in 2019, 2018 and 2017.
Citation Benchmarking is provided by Scopus and SciVal and is different from the metrics context provided by PlumX Metrics.
Metrics Details
- Citations116
- Citation Indexes114
- 114
- CrossRef63
- Patent Family Citations2
- Patent Families2
- Captures144
- Readers144
- 144
Article Description
Pharmacological strategies that boost intracellular NAD are highly coveted for their therapeutic potential. One approach is activation of nicotinamide phosphoribosyltransferase (NAMPT) to increase production of nicotinamide mononucleotide (NMN), the predominant NAD precursor in mammalian cells. A high-throughput screen for NAMPT activators and hit-to-lead campaign yielded SBI-797812, a compound that is structurally similar to active-site directed NAMPT inhibitors and blocks binding of these inhibitors to NAMPT. SBI-797812 shifts the NAMPT reaction equilibrium towards NMN formation, increases NAMPT affinity for ATP, stabilizes phosphorylated NAMPT at His247, promotes consumption of the pyrophosphate by-product, and blunts feedback inhibition by NAD. These effects of SBI-797812 turn NAMPT into a “super catalyst” that more efficiently generates NMN. Treatment of cultured cells with SBI-797812 increases intracellular NMN and NAD. Dosing of mice with SBI-797812 elevates liver NAD. Small molecule NAMPT activators such as SBI-797812 are a pioneering approach to raise intracellular NAD and realize its associated salutary effects.
Bibliographic Details
Springer Science and Business Media LLC
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