Results 21 to 30 of about 2,034 (179)

Reciprocal Potentiation of the Antitumoral Activities of FK866, an Inhibitor of Nicotinamide Phosphoribosyltransferase, and Etoposide or Cisplatin in Neuroblastoma Cells [PDF]

The Journal of Pharmacology and Experimental Therapeutics, 2011
: NAD is an essential coenzyme involved in numerous metabolic pathways. Its principal role is in redox reactions, and as such it is not heavily "consumed" by cells. Yet a number of signaling pathways that bring about its consumption have recently emerged.
Maldi E, Nina Kaludercic, BOLDORINI, Renzo Luciano, Valentina Drago, GALLI, Ubaldina, Armando A. Genazzani, Di Lisa F, DRAGO, VALENTINA, Kaludercic N, Ubaldina Galli, Renzo Boldorini, CANONICO, Pier Luigi, Cristina Travelli, Gian Cesare Tron, GENAZZANI, Armando, Genazzani, Armando A, Pier Luigi Canonico, Elena Maldi, TRAVELLI, Cristina, Fabio Di Lisa, Kaludercic, Nina, TRON, Gian Cesare, Maldi, Elena, Di Lisa, Fabio, Boldorini, Renzo   +24 more
core   +7 more sources

Molecular Effects of the Nampt Inhibitor FK866 on Leukemia Cells [PDF]

, 2016
Aberrant activation of metabolic pathways has emerged as an hallmark of proliferating cancer cells and pharmaceutical approaches targeting cell metabolism hold great potential for cancer treatment.
Zucal, Chiara
core   +2 more sources

IDO Downregulation Induces Sensitivity to Pemetrexed, Gemcitabine, FK866, and Methoxyamine in Human Cancer Cells. [PDF]

PLoS ONE, 2015
Indoleamine 2,3-dioxygenase-1 (IDO) is an immune regulatory enzyme expressed by most human tumors. IDO levels in tumor cells correlate with increased metastasis and poor patient outcome and IDO is linked to tumor cell resistance to immunotherapy ...
Saman Maleki Vareki, Di Chen, Christine Di Cresce, Peter J Ferguson, Rene Figueredo, Macarena Pampillo, Mateusz Rytelewski, Mark Vincent, Weiping Min, Xiufen Zheng, James Koropatnick   +10 more
doaj   +4 more sources

Molecular Mechanisms and Insights into the Nampt Inhibitor (FK866) Resistance in Cancers [PDF]

, 2017
Nicotinamide phosphoribosyltransferase (NAMPT), the rate-limiting enzyme in NAD+ biosynthesis from nicotinamide, is one of the major factors regulating cell metabolism and NAMPT is considered a promising target for treating cancer.
Thongon, Natthakan
core   +2 more sources

Efficacy of NAMPT inhibition in T-cell acute lymphoblastic leukemia. [PDF]

PLoS ONE
Novel agents targeting upregulated signaling pathways are needed to improve outcomes in T-cell acute lymphoblastic leukemia (T-ALL), since conventional cytotoxic chemotherapy regimens have reached the limits of tolerability.
Chelsea Vrana, Matthew Zhang, Max Rochette, Michelle Alozie, Hailey Oviedo, Alan Gonzalez, Jaden Sherman, Barry Zorman, Pavel Sumazin, Karen R Rabin, Jacob J Junco   +10 more
doaj   +2 more sources

Quantitative Analysis of Daporinad (FK866) and Its In Vitro and In Vivo Metabolite Identification Using Liquid Chromatography-Quadrupole-Time-of-Flight Mass Spectrometry

Molecules, 2022
Daporinad (FK866) is one of the highly specific inhibitors of nicotinamide phosphoribosyl transferase (NAMPT) and known to have its unique mechanism of action that induces the tumor cell apoptosis.
Byeong Ill Lee, Young G Shin, Yuri Park
exaly   +3 more sources

NAD⁺ Metabolic Reprogramming Drives CD8⁺ T Cells Senescence and Exacerbates Ulcerative Colitis. [PDF]

Aging Cell
Nicotinamide adenine dinucleotide (NAD+) depletion induces mitochondrial dysfunction and cytosolic mtDNA leakage in CD8+ T cells, activating the cGAS‐STING pathway and promoting a senescence‐associated secretory phenotype (SASP). The resulting pro‐inflammatory CD8+ T cells release IFN‐γ and TNF‐α, disrupt the intestinal epithelial barrier, and ...
Ye M, Zhou Q, Kong M, Zhao S, Lin L, Chen L, Yu J, Luo F, Liu J, Zhang J.   +9 more
europepmc   +2 more sources

Synthesis of a C-Iminoribofuranoside Analog of the Nicotinamide Phosphoribosyltransferase (NAMPT) Inhibitor FK866

Helvetica Chimica Acta, 2012
FK866 (also named APO866 or WK175) is a potent NAMPT inhibitor being evaluated (Phase II) as a potential anticancer drug. The preparation of the C-iminoribofuranoside analog (2E)-N-[4-(1-benzoylpiperidin-4-yl)butyl]-3-{3-[(2S,3S,4R,5R)-3,4-dihydroxy-5 ...
Gillig, Annabelle, Majjigapu, Somi Reddy, Sordat, Bernard, Vogel, Pierre   +3 more
core   +3 more sources

Intracellular NAD⁺ Depletion Increases Prostanoid Production via p38/COX2 Signalling in FK866-Induced Senescent Human Umbilical Vein Endothelial Cells. [PDF]

J Cell Mol Med
ABSTRACT Vascular endothelial cells maintain vascular homeostasis by releasing mediators with vasoconstrictive and vasorelaxant effects. Prostanoids are bioactive substances synthesised by cyclooxygenase2 (COX2); they preserve vascular function and can increase the risk of cardiovascular disease (CVD) associated with ageing.
Kitajima N, Nakajo T, Katayoshi T, Tsuji K.   +3 more
europepmc   +2 more sources

New Analogues of the Nicotinamide Phosphoribosyltransferase Inhibitor FK866 as Potential Anti-Pancreatic Cancer Agents

Medicinal Chemistry
International audienceBackground: During the past two decades, many nicotinamide phosphoribosyltransferase (NAMPT) inhibitors were prepared and tested because this enzyme is overexpressed in pancreatic cancer. Although FK866 is a well-known, strong NAMPT
Marra, Alberto, Benzi, Andrea, Caffa, Irene, Bruzzone, Santina, Conforti, Irene, Nencioni, Alessio   +5 more
core   +4 more sources