Evidence map›Paper›PMID 34982556›Full record

ArticleJournal of medicinal chemistry2022

Discovery, X-ray Crystallography, and Anti-inflammatory Activity of Bromodomain-containing Protein 4 (BRD4) BD1 Inhibitors Targeting a Distinct New Binding Site.

Zhiqing Liu, Yi Li, Haiying Chen, Hsien-Tsung Lai, Pingyuan Wang, Shwu-Yuan Wu, Eric A Wold, Paul G Leonard, Sarah Joseph, Haitao Hu and 4 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.

0numbers the graph read from it
0cells of the map it votes in
24citing papers in PubMed
4.2field-weighted citation impact, top 5% of its field
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

24 citing papers in PubMed, 50 citations in OpenAlex.

  1. Review
  2. Article
  3. Review
  4. Article
  5. Article
  6. Article
  7. Article
  8. Targeting lysine acetylation readers and writers.Nature reviews. Drug discovery · 2025
    Review
  9. An updated patent review of BRD4 degraders.Expert opinion on therapeutic patents · 2024
    Review
  10. Review
  11. Article
  12. Article
  13. Article
  14. Review
  15. Review
  16. Bromodomain inhibitors and therapeutic applications.Current opinion in chemical biology · 2023
    Review
  17. Review
  18. Article
  19. Review
  20. 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

14 authors at 4 institutions in 1 country.

Yi Li
Haiying Chen
Hsien-Tsung Lai
Pingyuan Wang
Shwu-Yuan Wu
Paul G LeonardCore for Biomolecular Structure and Function, MD Anderson Cancer Center, 1881 East Road, Houston, Texas 77054, United States.
Sarah JosephCore for Biomolecular Structure and Function, MD Anderson Cancer Center, 1881 East Road, Houston, Texas 77054, United States.
Haitao Hu
Cheng-Ming ChiangORCID 0000-0002-4968-3282
Allan R BrasierInstitute for Clinical and Translational Research (ICTR), University of Wisconsin-Madison School of Medicine and Public Health, 4248 Health Sciences Learning Center, Madison, Wisconsin 53705, United States.ORCID 0000-0002-5012-4090
Bing Tian
The University of Texas Medical Branch at Galveston · USThe University of Texas Southwestern Medical Center · USThe University of Texas MD Anderson Cancer Center · USUniversity of Wisconsin–Madison · US

Funding

Virus, Tissue Culture and ImmunoassayP01AI062885 · NIAID · UNIVERSITY OF TEXAS MEDICAL BR GALVESTON · PI CASOLA, ANTONELLA · 2005 to 2022
$23.9M
Modulation of BRD4 to epigenetically suppress HIVR01AI157852 · NIAID · UNIVERSITY OF TEXAS MED BR GALVESTON · PI HU, HAITAO · 2021 to 2025
$3.0M
Opposing Functions of BRD4 Isoforms in Breast CancerR01CA251698 · NCI · UT SOUTHWESTERN MEDICAL CENTER · PI CHIANG, CHENG-MING · 2020 to 2024
$2.3M
NCI NIH HHS R01 CA251698NIAID NIH HHS P01 AI062885NIAID NIH HHS R01 AI157852
6 · The paper itself

Abstract

Bromodomain-containing protein 4 (BRD4) is an emerging epigenetic drug target for intractable inflammatory disorders. The lack of highly selective inhibitors among BRD4 family members has stalled the collective understanding of this critical system and the progress toward clinical development of effective therapeutics. Here we report the discovery of a potent BRD4 bromodomain 1 (BD1)-selective inhibitor ZL0590 (

Indexed as

AnimalsAnti-Inflammatory AgentsBinding SitesBromodomain Containing ProteinsCell Cycle ProteinsCell LineCrystallography, X-RayGene ExpressionHumansInterleukin-6MaleMiceMice, Inbred C57BLNuclear ProteinsOxidoreductases Acting on CH-CH Group DonorsPhenylurea CompoundsAnti-Inflammatory AgentsBRD4 protein, humanBrd4 protein, mouseBromodomain Containing ProteinsCell Cycle ProteinsIL6 protein, humanInterleukin-6Nuclear ProteinsOxidoreductases Acting on CH-CH Group DonorsPhenylurea CompoundsRSAD2 protein, humanTranscription FactorsViperin Protein

Identifiers

PMID34982556
PMCPMC8989062
OpenAlexW4206573617

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.