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Chemoproteomic discovery of a brain-penetrant, covalent NLRP3 inhibitor that binds a novel allosteric pocket

delete2026-08-10
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OA
AI
D
Donald C. Rogness
E
Evelyn Sievert
V
Vincent F. Vartabedian
S
Steffen M. Bernard
E
Erick Aitchison
W
William Tao
M
Mikaela Lindvall
J
Jing Qian
C
Christie L. Eissler
B
Brian E. Nordin
B
Benjamin D. Horning
C
Cian Kingston
K
Kelsey N. Lamb
J
Joshua C. Bell
B
Bingwen Lu
J
Jonathan Pollock
J
Jun Shi
R
Roli Khattri
D
David S. Weinstein
M
Matthew P. Patricelli
B
Brian N. Cook *
G
Gabriel M. Simon *
DOI:10.1111/bph.70626delete
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Abstract

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
AI Summary

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Key information extracted from the uploaded paper, including a brief overview, abstract, background, key highlights, visual analysis, and future outlook.

Journal

British Journal of Pharmacology cover
British Journal of Pharmacology
IF:
7.7
Papers:
1.4W
Citations:
3.7W

Organization

V
Vividion Therapeutics
Scholars:
30
Papers: 6
Citations: 0
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