Article
Target enzyme mutations are the molecular basis for resistance towards pharmacological inhibition of nicotinamide phosphoribosyltransferase.
BMC cancer - 12 Dec 2010
Olesen Uffe H, Petersen Jakob G, Garten Antje, Kiess Wieland, Yoshino Jun, Imai Shin-Ichiro, Christensen Mette K, Fristrup Peter, Thougaard Annemette V, Björkling Fredrik, Jensen Peter B, Nielsen Søren J, Sehested Maxwell
Abstract excerpt
BACKGROUND: Inhibitors of nicotinamide phosphoribosyltransferase (NAMPT) are promising cancer drugs currently in clinical trials in oncology, including APO866, CHS-828 and the CHS-828 prodrug EB1627/GMX1777, but cancer cell resistance to these drugs has not been studied in detail. METHODS: Here, we introduce an analogue of CHS-828 called TP201565 with increased potency in cellular assays. Further, we describe and...
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