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Cell Communication and Signaling

Cell Communication and Signaling

IF: 8.2
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Identification of a covalent NEK7 inhibitor to alleviate NLRP3 inflammasome-driven metainflammation.

Published:25 November 2024 DOI: 10.1186/s12964-024-01919-w PMID: 39587676
Xiangyu Jin,?Yanqing Yang,?Didi Liu,?Xinru Zhou,?Yi Huang

Abstract

Aberrant activation of NLRP3 inflammasome is associated with a variety of inflammatory diseases. Advances in understanding the molecular mechanisms of NLRP3 inflammasome have revealed that NEK7 is an essential component for its activation, but the development of drugs specifically targeting NEK7 remains challenging. Here we identify rociletinib (ROC), an anticancer drug in phase III clinical trial with high safety profile, as a highly potent and specific small-molecule antagonists of NEK7. Mechanistically, ROC covalent binds to the cysteine 79 of NEK7 through its reactive α, β-unsaturated carbonyl group, thereby inhibiting the interaction between NLRP3 and NEK7, and the subsequent assembly and activation of NLRP3 inflammasome. Furthermore, ROC alleviates the pathological features of metainflammation on the mouse model of type 2 diabetes (T2D). In summary, our results identify ROC as a covalent inhibitor of NEK7 and demonstrates that targeting NEK7 provides a potential and promising strategy for the treatment of NLRP3 inflammasome-driven T2D.

Substances (26)

Materials
Procduct Name CAS Molecular Formula Supplier Price
WZ4002 1213269-23-8 C25H27ClN6O3 226 suppliers $8.00-$4050.00
WZ4002 1213269-23-8 C25H27ClN6O3 226 suppliers $8.00-$4050.00
WZ4002 1213269-23-8 C25H27ClN6O3 226 suppliers $8.00-$4050.00
WZ4002 1213269-23-8 C25H27ClN6O3 226 suppliers $8.00-$4050.00
CO-1686 1374640-70-6 C27H28F3N7O3 226 suppliers $9.00-$3510.00
CO-1686 1374640-70-6 C27H28F3N7O3 226 suppliers $9.00-$3510.00
CO-1686 1374640-70-6 C27H28F3N7O3 226 suppliers $9.00-$3510.00
CO-1686 1374640-70-6 C27H28F3N7O3 226 suppliers $9.00-$3510.00
Canertinib 267243-28-7 C24H25ClFN5O3 182 suppliers $29.00-$1828.00
Canertinib 267243-28-7 C24H25ClFN5O3 182 suppliers $29.00-$1828.00

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