Synthesis and Evaluation of Reactive Oxygen Species Sensitive Prodrugs of a NAMPT Inhibitor FK866 [PDF]
NAMPT is an attractive target in cancer therapy and numerous NAMPT inhibitors have been developed. However, the clinical activities of NAMPT inhibitors have displayed disappointing results in clinical trials for their dose-limiting toxicities.
Zili Xu +4 more
doaj +3 more sources
A Novel NAMPT Inhibitor-Based Antibody-Drug Conjugate Payload Class for Cancer Therapy. [PDF]
[Image: see text] Inhibition of intracellular nicotinamide phosphoribosyltransferase (NAMPT) represents a new mode of action for cancer-targeting antibody–drug conjugates (ADCs) with activity also in slowly proliferating cells.
Böhnke N +23 more
europepmc +3 more sources
NAMPT haploinsufficiency is a therapeutic vulnerability to NAMPT inhibition in -7/-7q MDS [PDF]
Chromosome 7 abnormalities -7 and -7q define a high-risk subset of myelodysplastic syndromes (MDS) with poor prognosis. The NAMPT gene, located at 7q22.3, encodes a rate limiting enzyme (nicotinamide phosphoribosyl transferase) in the NAD+ salvage ...
Nemo Ikonen +7 more
doaj +2 more sources
Inhibition of NAMPT by PAK4 Inhibitors
The serine/threonine kinase PAK4 plays a crucial role in regulating cell proliferation, survival, migration, and invasion. Overexpression of PAK4 correlates with poor prognosis in some cancers. KPT-9274, a PAK4 inhibitor, significantly reduces the growth
Audrey Minden, Yiling Wang
core +3 more sources
The nicotinamide phosphoribosyltransferase inhibitor FK866 restricts influenza A virus replication by perturbing viral polymerase activity [PDF]
Nicotinamide phosphoribosyltransferase (NAMPT), a key rate-limiting enzyme in NAD+ synthesis, plays important roles in various physiological and pathological processes.
Changjie Lv +5 more
doaj +2 more sources
NAPRT loss promotes lung tumor initiation and growth through AKT signaling independently of NAD+ biosynthesis [PDF]
Loss of NAPRT promotes lung tumor initiation and growth through a noncanonical mechanism, independent of its role in NAD+ biosynthesis. Mechanistically, NAPRT depletion activates the mTORC2‐driven AKT/β‐catenin signaling axis to enhance clonogenic and invasive phenotypes. Furthermore, lung‐specific Naprt deletion significantly increases tumor burden in
Myung Joon Oh +11 more
wiley +2 more sources
Background Nicotinamide phosphoribosyltransferase (NAMPT) and nicotinamide adenine dinucleotide (NAD) levels are crucial for liver function. The saturated fatty acid palmitate and the unsaturated fatty acid oleate are the main free fatty acids in adipose
Melanie Penke +5 more
doaj +2 more sources
Inhibiting Nampt signaling promotes M2 macrophage polarization to enhance bone regeneration in periodontitis [PDF]
BackgroundDysregulated macrophage polarization is a fundamental cause of bone loss in periodontitis. However, the role of nicotinamide phosphoribosyltransferase (NAMPT) in macrophage regulation within periodontitis remains unclear.
Yixin Xia +4 more
doaj +2 more sources
Molecular Effects of the Nampt Inhibitor FK866 on Leukemia Cells [PDF]
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
Review of various NAMPT inhibitors for the treatment of cancer
Nicotinamide phosphoribosyltransferase (NAMPT) is a rate-limiting enzyme in the NAD salvage pathway of mammalian cells and is overexpressed in numerous types of cancers. These include breast cancer, ovarian cancer, prostate cancer, gastric cancer, colorectal cancer, glioma, and b-cell lymphoma.
Yichen Wei +3 more
openaire +3 more sources

