Evidence map›Paper›PMID 39668548›Full record

ArticleChemical biology & drug design2024

Expansion of the Structure-Activity Relationship Profile of Triaminopyrimidines as Inhibitors of Caspase-1.

Amanda East, Callista G Polasek, Elizabeth A Miller, Srirajkumar Ranganathan, Isabella D Reda, Aisha Patel, Christopher D Ahlers, Sarah K Zingales, Caitlin E Karver

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Chemical biology & drug design, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing 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

1 citing paper in PubMed.

  1. Article
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

9 authors.

Amanda EastDepartment of Chemistry, DePaul University, Chicago, Illinois, USA.
Callista G PolasekDepartment of Chemistry, DePaul University, Chicago, Illinois, USA.
Elizabeth A MillerDepartment of Chemistry, DePaul University, Chicago, Illinois, USA.
Srirajkumar RanganathanDepartment of Chemistry, DePaul University, Chicago, Illinois, USA.
Isabella D RedaDepartment of Chemistry, DePaul University, Chicago, Illinois, USA.
Aisha PatelDepartment of Chemistry, DePaul University, Chicago, Illinois, USA.
Christopher D AhlersDepartment of Chemistry, DePaul University, Chicago, Illinois, USA.
Sarah K ZingalesUnited States Coast Guard Academy, New London, Connecticut, USA.
Caitlin E KarverDepartment of Chemistry, DePaul University, Chicago, Illinois, USA.ORCID 0000-0003-1249-7395

Funding

Uncovering the biological roles of inflammatory caspases through chemical approachesR15GM132990 · NIGMS · DE PAUL UNIVERSITY · PI KARVER, CAITLIN E., SOUTHERN, CATHRINE ANN · 2020 to 2020
$438k
DePaul University Academic Initiatives Pool 601305DePaul University College of Science and Health Undergraduate Summer Research ProgramDePaul University Department of Chemistry and BiochemistryDePaul University Research Council Competitive Research 601227DePaul University Research Council Competitive Research 602183NIGMS NIH HHS R15 GM132990NIH HHS 1R15GM13299001A1
6 · The paper itself

Abstract

Caspase-1 is a sought-after therapeutic target for inflammatory conditions due to its role in activation and release of pro-inflammatory cytokines, but there has been little success getting drugs into the clinic. We have previously shown triaminopyrimidines such as CK-1-41 are potent, reversible small molecule inhibitors of caspase-1, likely binding in an allosteric site within the enzyme. A series of analogs of CK-1-41 were synthesized and tested against caspase-1 to develop a more robust structure-activity relationship profile. In general, alkyl and aryl groups were well tolerated via an ethylene or methylene linkage to the piperazine nitrogen, with IC

Indexed as

Caspase 1Caspase InhibitorsPyrimidinesAllosteric SiteHumansMolecular Docking SimulationStructure-Activity RelationshipCaspase 1Caspase InhibitorsPyrimidinescaspase‐1dockinginhibitorsmedicinal chemistrystructure–activity relationships

Identifiers

PMID39668548
PMCPMC11649019

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Registered trials

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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.