Evidence map›Paper›PMID 41448046›Full record

ArticleEuropean journal of medicinal chemistry2026

Development of cell-active BRD4-D1 selective inhibitors to decode the role of BET proteins in LPS-mediated liver inflammation.

Cole R Scholtz, Luke C Doskey, Sai Giridhar Sarma Kandanur, Nora R Vail, Erika R Roderick, Elliott J Peterson, Zachariah J Hoell, Ke Shi, Hideki Aihara, Enis Kostallari and 3 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in European journal of medicinal chemistry, 2026. 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

13 authors.

Cole R ScholtzDepartment of Chemistry, University of Minnesota, Minneapolis, MN, 55455, United States.
Luke C DoskeyDivision of Gastroenterology and Hepatology, Mayo Clinic, Rochester, MN, United States.
Sai Giridhar Sarma KandanurDepartment of Chemistry, University of Minnesota, Minneapolis, MN, 55455, United States.
Nora R VailDepartment of Chemistry, University of Minnesota, Minneapolis, MN, 55455, United States.
Erika R RoderickDepartment of Chemistry, University of Minnesota, Minneapolis, MN, 55455, United States.
Elliott J PetersonDepartment of Medicinal Chemistry, University of Minnesota, Minneapolis, MN, 55455, United States.
Zachariah J HoellDepartment of Chemistry, University of Minnesota, Minneapolis, MN, 55455, United States.
Ke ShiDepartment of Biochemistry, Molecular Biology, and Biophysics, University of Minnesota, Minneapolis, MN, 55455, United States.
Hideki AiharaDepartment of Biochemistry, Molecular Biology, and Biophysics, University of Minnesota, Minneapolis, MN, 55455, United States.
Enis KostallariDivision of Gastroenterology and Hepatology, Mayo Clinic, Rochester, MN, United States; Department of Biochemistry and Molecular Biology, Mayo Clinic, Rochester, MN, United States.
Vijay H ShahDepartment of Chemistry, University of Minnesota, Minneapolis, MN, 55455, United States.
Harmeet MalhiDivision of Gastroenterology and Hepatology, Mayo Clinic, Rochester, MN, United States.
William C K PomerantzDepartment of Chemistry, University of Minnesota, Minneapolis, MN, 55455, United States. Electronic address: wcp@umn.edu.

Funding

User Training and OutreachP30GM124165 · NIGMS · CORNELL UNIVERSITY · PI STEVEN E EALICK · 2018 to 2026
$34.2M
TRAINING FOR FUTURE BIOTECHNOLOGY DEVELOPMENTT32GM008347 · NIGMS · UNIVERSITY OF MINNESOTA TWIN CITIES · PI SCHMIDT-DANNERT, CLAUDIA · 1990 to 2021
$11.0M
Structural studies of viral replication and invasionR35GM118047 · NIGMS · UNIVERSITY OF MINNESOTA · PI Hideki Aihara · 2016 to 2026
$6.3M
Pathobiology of Liver InjuryR01DK111378 · NIDDK · MAYO CLINIC ROCHESTER · PI MALHI, HARMEET · 2016 to 2025
$3.9M
Molecular Mechanisms of Liver Fibrosis (Diversity Supplement)R37AA021171 · NIAAA · MAYO CLINIC ROCHESTER · PI VIJAY H. SHAH · 2019 to 2026
$3.0M
Chemical Probe Development for Epigenetic Complexes Enabled by Protein-Observed 19F NMRR35GM140837 · NIGMS · UNIVERSITY OF MINNESOTA · PI William Charles Krause Pomerantz · 2021 to 2026
$2.5M
NIAAA NIH HHS R37 AA021171NIDDK NIH HHS R01 DK111378NIGMS NIH HHS P30 GM124165NIGMS NIH HHS R35 GM118047NIGMS NIH HHS R35 GM140837NIGMS NIH HHS T32 GM008347
6 · The paper itself

Abstract

The endogenously expressed BET proteins (BRD2, BRD3, BRD4) are upstream clinical targets for anti-inflammatory treatments, where inhibition of the tandem bromodomains (D1 and D2) have proven efficacious in vitro and in vivo towards NF-κB-mediated inflammation. Despite their efficacy, dose-limiting toxicities associated with BET inhibition have limited clinical progression. One strategy to circumvent these dose-limiting toxicities has included domain- or protein-selective inhibition of the BET bromodomains. Based on previously reported 1,2,4-substituted imidazole scaffolds, we characterize and report on next-generation BRD4-D1 selective inhibitors, 39 and 41. Compound 39 is both highly potent and selective towards BRD4-D1 (K

Indexed as

Anti-Inflammatory AgentsCell Cycle ProteinsDrug DevelopmentInflammationLiverTranscription FactorsAnimalsBromodomain Containing ProteinsDose-Response Relationship, DrugHumansLipopolysaccharidesMolecular StructureStructure-Activity RelationshipAnti-Inflammatory AgentsBRD4 protein, humanBromodomain Containing ProteinsCell Cycle ProteinsLipopolysaccharidesTranscription FactorsAnti-inflammatoryBromodomainCell-activeEpigeneticsLiver disease

Identifiers

PMID41448046
PMCPMC12768458

What OpenQuestion holds

Textmetadata
LicenceTDM
Read underepoch 390

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.