Results 151 to 160 of about 2,034 (179)
FK866 compromises mitochondrial metabolism and adaptive stress responses in cultured cardiomyocytes [PDF]
Biochemical Pharmacology, 2015 Artículo de publicación ISIAim: FK866 is an inhibitor of the NAD(+) synthesis rate-limiting enzyme nicotinamide phosphoribosyltransferase (NAMPT). Using FK866 to target NAD(+) synthesis has been proposed as a treatment for inflammatory diseases and ...
Gina Sánchez +2 more
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Design of PLGA nanoparticles for sustained release of hydroxyl-FK866 by microfluidics
Biomaterials Advances, 2023 The use of nanoparticle (NP) delivery systems in cancer treatment has received significant interest, however use of such systems in delivery of cytotoxic chemotherapy agents can be limited by low encapsulation efficiency and burst release of the ...
Annalisa Tirella
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Discovery of potent NAMPT-Targeting PROTACs using FK866 as the warhead
Bioorganic and Medicinal Chemistry Letters, 2023Nicotinamide phosphoribosyltransferase (NAMPT) has emerged as a promising target for cancer therapy due to its strong correlation with nicotinamide adenine dinucleotide (NAD+) metabolism and tumorigenesis. Proteolysis targeting chimeras (PROTACs) provided an attractive strategy for developing NAMPT-targeting NAD+-depleting cancer drugs.
Chunquan Sheng, Defeng Xu, Guoqiang Dong
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Lipopolysaccharide-Induced Microglial Neuroinflammation: Attenuation by FK866
Neurochemical Research, 2021Alleviating microglia-mediated neuroinflammation bears great promise to reduce neurodegeneration. Nicotinamide phosphoribosyltransferase (NAMPT) may exert cytokine-like effect in the brain. However, it remains unclear about role of NAMPT in microglial inflammation. Also, it remains unknown about effect of NAMPT inhibition on microglial inflammation. In
Lijia Yu
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Crystal structure of Rattus norvegicus Visfatin/PBEF/Nampt in complex with an FK866-based inhibitor
Molecules and Cells, 2009 Visfatin (Nampt/PBEF) plays a pivotal role in the salvage pathway for NAD(+) biosynthesis. Its potent inhibitor, FK866, causes cellular NAD(+) levels to decline, thereby inducing apoptosis in tumor cells. In an effort to improve the solubility and binding interactions of FK866, we designed and synthesized IS001, in which a ribose group is attached to ...
Soo Hyun Eom +2 more
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Inhibition of NAMPT pathway by FK866 activates the function of p53 in HEK293T cells
Biochemical and Biophysical Research Communications, 2012Inactivation of p53 protein by endogenous and exogenous carcinogens is involved in the pathogenesis of different human malignancies. In cancer associated with SV-40 DNA tumor virus, p53 is considered to be non-functional mainly due to its interaction with the large T-antigen. Using the 293T cell line (HEK293 cells transformed with large T antigen) as a
Karl Heinrich Welte +2 more
exaly +3 more sources
Synthesis and Biological Evaluation of Isosteric Analogues of FK866, an Inhibitor of NAD Salvage
ChemMedChem, 2008AbstractOne of the great challenges of medicinal chemistry is to create novel, effective, chemotherapeutic agents that show specificity for cancer cells combined with low systemic toxicity. A novel idea is to target the enzymes of the NAD biosynthesis and recycling pathways given that cancer cells display a higher NAD turnover rate than healthy cells ...
Gian Cesare Tron +2 more
exaly +6 more sources
International Immunopharmacology, 2020
Dynamin-related protein 1 (Drp1) mediates mitochondrial fission and triggers NLRP3 inflammasome activation. FK866 (a NAMPT inhibitor) exerts a neuroprotective effect in ischemia/reperfusion injury through the suppression of mitochondrial dysfunction. We explored the effects of FK866 on pyroptosis and inflammation mediated by Drp1 in a cardiac arrest ...
Meng-Hua Chen, Xinyue Tian, Lu Xie
exaly +3 more sources
Dynamin-related protein 1 (Drp1) mediates mitochondrial fission and triggers NLRP3 inflammasome activation. FK866 (a NAMPT inhibitor) exerts a neuroprotective effect in ischemia/reperfusion injury through the suppression of mitochondrial dysfunction. We explored the effects of FK866 on pyroptosis and inflammation mediated by Drp1 in a cardiac arrest ...
Meng-Hua Chen, Xinyue Tian, Lu Xie
exaly +3 more sources
FK866 inhibits colorectal cancer metastasis by reducing NAD+ levels in cancer-associated fibroblasts
Genes & Genomics, 2022Extraintestinal metastasis is the main therapeutic challenge for colorectal cancer, the third most common cancer worldwide. Various components of the tumor microenvironment, especially cancer-associated fibroblasts (CAFs), play important roles in tumor metastasis.
Hanhan Xie +6 more
openaire +2 more sources
Investigational New Drugs, 2007
FK866 is a potent inhibitor or NAD synthesis. This first-in-human study was performed to determine the maximum-tolerated dose, toxicity profile, and pharmacokinetics on a 96-h continuous infusion schedule.Twenty four patients with advanced solid tumor malignancies refractory to standard therapies were treated with escalating doses of FK866 as a ...
Leonard B. Saltz +2 more
exaly +3 more sources
FK866 is a potent inhibitor or NAD synthesis. This first-in-human study was performed to determine the maximum-tolerated dose, toxicity profile, and pharmacokinetics on a 96-h continuous infusion schedule.Twenty four patients with advanced solid tumor malignancies refractory to standard therapies were treated with escalating doses of FK866 as a ...
Leonard B. Saltz +2 more
exaly +3 more sources