NK7-902 TFA 是NEK7的 CRBN 分子胶降解剂。
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NK7-902 TFA is aCRBN molecular gluedegrader ofNEK7. NK7-902 TFA fully degradesNEK7in human primary monocytes and whole blood but only partially inhibits NLRP3-dependent IL-1β production. NK7-902 TFA leads to profound and long-lastingNEK7degradation but only transiently blocksNLRP3inflammasome activation in non-human primates by oral administration. NK7-902 TFA shows activity in murine systems[1].
参考文献:
[1].Sylvain A, et, al. A cereblon (CRBN) molecular glue degrader of NIMA-related kinase 7 (NEK7) reveals a context-dependent role in NLRP3 inflammasome activation. bioRxiv. 2024.11.06.622079.