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• W4308037678 abstract "<h2>Summary</h2> Aberrant overexpression of nicotinamide phosphoribosyltransferase (NAMPT) has been reported in a variety of tumor cells and is a poor prognosis factor for patient survival. It plays an important role in tumor cell proliferation, acting concurrently as an nicotinamide adenine dinucleotide (NAD⁺) synthase and, unexpectedly, as an extracellular signaling molecule for several tumor-promoting pathways. Although previous efforts to modulate NAMPT activity were limited to enzymatic inhibitors with low success in clinical studies, protein degradation offers the possibility to simultaneously disrupt NAMPT's enzyme activity and ligand capabilities. Here we report the development of two highly selective proteolysis-targeting chimeras (PROTACs) that promote NAMPT degradation in a cereblon-dependent manner. Both PROTAC degraders outperform a clinical candidate, FK866, in killing effect on hematological tumor cells. These results emphasize the importance and feasibility of applying PROTACs as a superior strategy for targeting proteins with multiple tumor-promoting functions like NAMPT, which is not easily achieved by conventional enzymatic inhibitors." @default.
• W4308037678 created "2022-11-07" @default.
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• W4308037678 date "2022-11-01" @default.
• W4308037678 modified "2023-10-16" @default.
• W4308037678 title "Addressing the Enzyme-independent tumor-promoting function of NAMPT via PROTAC-mediated degradation" @default.
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• W4308037678 doi "https://doi.org/10.1016/j.chembiol.2022.10.007" @default.
• W4308037678 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/36323324" @default.
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