ArticleScientific reports2015
Discovery and characterization of novel small-molecule inhibitors targeting nicotinamide phosphoribosyltransferase.
Article in Scientific reports, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 25 papers.
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Who cites it
25 citing papers in PubMed, 54 citations in OpenAlex.
- Pharmacophore-Based QSAR Model of Multi Scaffolds as NAMPT Inhibitors & Scaffold Diversity Analysis.Molecules (Basel, Switzerland) · 2026Article
- The role of NADnpj metabolic health and disease · 2025Review
- Targeting NAD Metabolism: Rational Design, Synthesis and In Vitro Evaluation of NAMPT/PARP1 Dual-Target Inhibitors as Anti-Breast Cancer Agents.Molecules (Basel, Switzerland) · 2024Article
- NAD/NAMPT and mTOR Pathways in Melanoma: Drivers of Drug Resistance and Prospective Therapeutic Targets.International journal of molecular sciences · 2022Review
- Review
- NAMPT-targeting PROTAC promotes antitumor immunityActa pharmaceutica Sinica. B · 2022Article
- Small Molecule Regulators Targeting NADCurrent medicinal chemistry · 2022Article
- FK866 Protects Human Dental Pulp Cells against Oxidative Stress-Induced Cellular Senescence.Antioxidants (Basel, Switzerland) · 2021Article
- Targeting the NADCell communication and signaling : CCS · 2020Article
- Article
- Nicotinamide Phosphoribosyltransferase (NAMPT) Is a New Target of Antitumor Agent Chidamide.ACS medicinal chemistry letters · 2020Article
- Recent Advances in NAMPT Inhibitors: A Novel Immunotherapic Strategy.Frontiers in pharmacology · 2020Review
- Identification of evolutionary and kinetic drivers of NAD-dependent signaling.Proceedings of the National Academy of Sciences of the United States of America · 2019Article
- Targeting NAMPT as a therapeutic strategy against stroke.Stroke and vascular neurology · 2019Review
- Crystal structure-based comparison of two NAMPT inhibitors.Acta pharmacologica Sinica · 2018Article
- Dual NAMPT/HDAC Inhibitors as a New Strategy for Multitargeting Antitumor Drug Discovery.ACS medicinal chemistry letters · 2018Article
- Cancer cell metabolic plasticity allows resistance to NAMPT inhibition but invariably induces dependence on LDHA.Cancer & metabolism · 2018Article
- NAMPT overexpression induces cancer stemness and defines a novel tumor signature for glioma prognosis.Oncotarget · 2017Article
- Article
- Association between hypoxic volume and underlying hypoxia-induced gene expression in oropharyngeal squamous cell carcinoma.British journal of cancer · 2017Article
Corrections and comments
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Authors and funding
10 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Nicotinamide phosphoribosyltransferase (NAMPT) is a promising anticancer target. Using high throughput screening system targeting NAMPT, we obtained a potent NAMPT inhibitor MS0 (China Patent ZL201110447488.9) with excellent in vitro activity (IC50 = 9.87 ± 1.15 nM) and anti-proliferative activity against multiple human cancer cell lines including stem-like cancer cells. Structure-activity relationship studies yielded several highly effective analogues. These inhibitors specifically bound NAMPT, rather than downstream NMNAT. We provided the first chemical case using cellular thermal shift assay to explain the difference between in vitro and cellular activity; MS7 showed best in vitro activity (IC50 = 0.93 ± 0.29 nM) but worst cellular activity due to poor target engagement in living cells. Site-directed mutagenesis studies identified important residues for NAMPT catalytic activity and inhibitor binding. The present findings contribute to deep understanding the action mode of NAMPT inhibitors and future development of NAMPT inhibitors as anticancer agents.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.