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Chemoproteomic discovery of a brain-penetrant, covalent NLRP3 inhibitor that binds a novel allosteric pocket
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DOI:10.1111/bph.70626.png)
Abstract
En 中文
The NLRP3 inflammasome is an attractive therapeutic target for multiple inflammatory conditions. Although inhibitors have been developed, their chemical diversity is limited, and their properties are not ideal for brain penetrance, which is desirable for treating neuroinflammatory disorders.
Keywords:
additional Area(s)
allosteric modulation
biochemical pharmacology
cross-cutting area
drug discovery/target validation
inflammasome
inflammation
NLRP3
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