Global ETD Search
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Showing 1 to 9 of 9 for “"FK866"”.
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Molecular Effects of the Nampt Inhibitor FK866 on Leukemia Cells
… thus considered a promising anti-cancer target. FK866 is a specific NAMPT inhibitor that lowers NAD+ concentration in cancer cells, reducing the activity of NAD+-dependent enzymes, impacting on ATP production and promoting cell death. NAMPT inhibition was proven to be highly effective in both …
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Characterisation of Pharmacological Mechanisms and Potential Therapeutic uses of FK866
… targets for drug development. Recently, FK866, a potent inhibitor of nicotinamide phosphoribosyltransferase (Nampt) an important enzyme in the NAD+ rescue pathway, has been evaluated in clinical trials against cancer. The aim of this study is to further investigate the mechanisms and …
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Preparación, aplicaciones y reactividad de nuevos derivados de iminoazúcares. Síntesis de análogos del FK866 con propiedades anticáncer
… de nuevos análogos del compuesto antitumoral FK866. Estos derivados incorporan uno o dos átomos de flúor o cloro en el anillo de piridina con el objetivo de minimizar la N-oxidación in vivo del compuesto de referencia (FK866), mejorando su biodisponibilidad. Adicionalmente, incorporan …
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Targeting iNAMPT to Break the Obesity-Associated Liver Cancer Link: An In Vitro and In Vivo Approach
… diet-induced obesity (OB) or control chow (CR) + FK866 (iNAMPT inhibitor) in SNU, HepG2 human liver cancer cells and Hepa 1-6 murine cells. Analysis of proteins pAkt and pERK was performed by immunoblot. Proliferation, ROS, cytotoxicity, and invasion were also measured in liver cancer cells. For …
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Protective effect of Nicotinamide on High glucose (HG)/Palmitate (PA)-induced Glucolipotoxicity to INS-1 beta cells
… of NAD salvage pathway by Nampt inhibitor FK866 or knocking down the Nampt or knocking down the Nmnat did not protect against HG/PA-induced cell death. Furthermore, FK866 did not reduced NAM-induced protective effects. Third, We have investigated whether NAM has protective effect against …
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Polystyrene coated iron-platinum drug delivery platforms for theranostics
… Furthermore, there are numerous drugs such as FK866, doxorubicin, gemcitabine, and paclitaxel that are used to treat various types of cancer. Many of these drugs have different mechanisms by which they cause cell death. New derivatives of FK866, considered to be one of the most potent …
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The effects of the adipocyte-secreted proteins resistin and visfatin on the pancreatic beta-cell
… and were reversed by visfatin inhibitor FK866. Visfatin treatment at low concentrations did not have any effect on cell viability however the elevated concentrations resulted in a decline. These data indicate that both resistin and visfatin potentially play important roles in beta-cell …
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The Identification and Targeting of Altered NAD+ Metabolism in Glioblastoma
… inhibition of the salvage pathway with FK866 sustained β-lapachone mediated NAD+ depletion and combination led to synergistic toxicity. These results identified NQO1 expression as a potential marker of susceptibility to β-lapachone. We next investigated targeting of ribose synthesis, the …
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Boron-Mediated Semireduction of Alkynoic Acid Derivatives
… reaction by augmenting the total synthesis of FK866, a potent nicotinamide mononucleotide adenyltransferase (NMNAT) inhibitor, and isolated the cinnamamide product in good yield with >99:1 E:Z stereoselectivity. Using a similar strategy, we investigated the ability of bis(pinacolato)diboron and …