首页|Hydrophobic tagging-induced degradation of NAMPT in leukemia cells
Hydrophobic tagging-induced degradation of NAMPT in leukemia cells
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Nicotinamide phosphoribosyl transferase(NAMPT)is considered as a promising target for cancer ther-apy to its crucial role in cancer metabolism.Despite the therapeutic potential of NAMPT enzymatic in-hibitors,their effectiveness is limited by dose-related toxicity and the inability to suppress nonenzymatic functions of extracellular NAMPT(eNAMPT).Herein,we designed and synthesized the first hydrophobic tagging NAMPT degraders.Among them,compound NH-11 selectively degraded NAMPT in leukemia cells through the ubiquitin-proteasome system.Compound NH-11 effectively induced apoptosis and showed low toxicity to normal cells,representing a promising anti-leukemia lead compound.
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