Evidence map›Paper›PMID 38901282›Full record

ArticleBioorganic chemistry2024

Characterization of a small molecule inhibitor of the NLRP3 inflammasome and its potential use for acute lung injury.

Yiming Xu, Savannah Biby, Chunqing Guo, Zheng Liu, Jinyang Cai, Xiang-Yang Wang, Shijun Zhang

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
–field-weighted citation impact
1 · What the graph read from it

What it found

Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.

The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.

2 · The registry

The trial behind it

Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

3 citing papers in PubMed.

  1. Article
  2. Review
  3. Review
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

7 authors.

Yiming XuDepartment of Medicinal Chemistry, Virginia Commonwealth University, Richmond, VA 23298, USA.
Savannah BibyDepartment of Medicinal Chemistry, Virginia Commonwealth University, Richmond, VA 23298, USA.
Chunqing GuoDepartment of Human and Molecular Genetics, Virginia Commonwealth University, Richmond, VA 23298, USA.
Zheng LiuDepartment of Human and Molecular Genetics, Virginia Commonwealth University, Richmond, VA 23298, USA.
Jinyang CaiDepartment of Human and Molecular Genetics, Virginia Commonwealth University, Richmond, VA 23298, USA.
Xiang-Yang WangDepartment of Human and Molecular Genetics, Virginia Commonwealth University, Richmond, VA 23298, USA.
Shijun ZhangDepartment of Medicinal Chemistry, Virginia Commonwealth University, Richmond, VA 23298, USA. Electronic address: szhang2@vcu.edu.

Funding

Development of novel NLRP3 inflammasome inhibitors for intervening in Alzheimer's diseaseU01AG076481 · NIA · VIRGINIA COMMONWEALTH UNIVERSITY · PI Shijun Zhang · 2022 to 2026
$7.5M
Probing neuroinflammation in Alzheimer's disease with NLRP3 PET radiotracersRF1AG076912 · NIA · VIRGINIA COMMONWEALTH UNIVERSITY · PI ZHANG, SHIJUN · 2023 to 2023
$1.9M
BLRD VA I01 BX003275NIA NIH HHS RF1 AG076912NIA NIH HHS U01 AG076481
6 · The paper itself

Abstract

Accumulating data support the key roles of the NLRP3 inflammasome, an essential component of the innate immune system, in human pathophysiology. As an emerging drug target and a potential biomarker for human diseases, small molecule inhibitors of the NLRP3 inflammasome have been actively pursued. Our recent studies identified a small molecule, MS-II-124, as a potent NLRP3 inhibitor and potential imaging probe. In this report, MS-II-124 was further characterized by an unbiased and comprehensive analysis through Eurofins BioMAP Diversity PLUS panel that contains 12 human primary cell-based systems. The analysis revealed promising activities of MS-II-124 on inflammation and immune functions, further supporting the roles of the NLRP3 inflammasome in these model systems. Further studies of MS-II-124 in mouse model of acute lung injury (ALI)/acute respiratory distress syndrome (ARDS) and NLRP3 knockout mice demonstrated its target engagement, efficacy to suppress inflammatory cytokines and infiltration of immune cells in the lung tissues. In summary, the results support the therapeutic potential of MS-II-124 as a NLRP3 inhibitor and warrant future studies of this compound and its analogs to develop therapeutics for ALI/ARDS.

Indexed as

Acute Lung InjuryInflammasomesMice, KnockoutNLR Family, Pyrin Domain-Containing 3 ProteinSmall Molecule LibrariesAnimalsDose-Response Relationship, DrugHumansMiceMice, Inbred C57BLMolecular StructureStructure-Activity RelationshipInflammasomesNLR Family, Pyrin Domain-Containing 3 ProteinNLRP3 protein, humanNlrp3 protein, mouseSmall Molecule LibrariesAcute lung injury (ALI)/acute respiratory distress syndrome (ARDS)BioMAPInfiltrationInflammatory cytokinesInhibitorNLRP3 inflammasome

Identifiers

PMID38901282
PMCPMC11270536

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Registered trials

None linked

Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.