Evidence map›Paper›PMID 38642703›Full record

ReviewDrug discovery today2024

Targeting EED as a key PRC2 complex mediator toward novel epigenetic therapeutics.

Qichao Bao, Anil Kumar, Daqing Wu, Jia Zhou

Open access · greenAbstract readReview
In one paragraph

Review in Drug discovery today, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 17 papers.

0numbers the graph read from it
0cells of the map it votes in
17citing papers in PubMed
3.0field-weighted citation impact, top 8% 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

17 citing papers in PubMed, 13 citations in OpenAlex.

  1. Review
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  3. Article
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  7. Article
  8. Epigenetic regulation of EZH2 by ncRNAs: mechanisms and oncogenic implications.Naunyn-Schmiedeberg's archives of pharmacology · 2026
    Review
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  11. Article
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  17. Advancements in Protein Degradation for Cancer Therapy.ACS medicinal chemistry letters · 2024
    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

4 authors at 2 institutions in 1 country.

Qichao BaoChemical Biology Program, Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, TX 77555, USA.
Anil KumarChemical Biology Program, Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, TX 77555, USA.
Daqing WuCenter for Cancer Research and Therapeutic Development and Department of Biological Sciences, Clark Atlanta University, Atlanta, GA 30314, USA.
Jia ZhouChemical Biology Program, Department of Pharmacology and Toxicology, University of Texas Medical Branch, Galveston, TX 77555, USA. Electronic address: jizhou@utmb.edu.
The University of Texas Medical Branch at Galveston · USCenter for Cancer Research · US

Funding

To Investigate Molecular Mechanisms of Aging-Related Growth of the Prostate - Implications in Prostate Tumorigenesis and Cancer TreatmentU54MD007590 · NIMHD · CLARK ATLANTA UNIVERSITY · PI JAIDEEP CHAUDHARY · 2019 to 2026
$17.1M
Targeting chemoresistant prostate cancer with novel EED inhibitorsR01CA256058 · NCI · CLARK ATLANTA UNIVERSITY · PI DAQING WU · 2022 to 2026
$2.1M
Small-molecule therapy for metastatic castration-resistant prostate cancerR42CA217491 · NCI · METCURE THERAPEUTICS, LLC · PI WU, DAQING · 2021 to 2022
$1.9M
NCI NIH HHS R01 CA256058NCI NIH HHS R42 CA217491NIMHD NIH HHS U54 MD007590
6 · The paper itself

Abstract

EED within the PRC2 complex is crucial for chromatin regulation particularly in tumor development, making its inhibition a promising epigenetic therapeutic strategy. Significant advancement in PRC2 inhibitor development has been achieved with an approved EZH2 inhibitor in the market and with others in the clinical trials. However, current EZH2 inhibitors are limited to specific blood cancers and encounter therapeutic resistance. EED stabilizes PRC2 complex and enhances its activity through unique allosteric mechanisms, thereby acting as both a scaffold protein and a recognizer of H3K27me3 making it an attractive drug target. This review provides an overview of epigenetic therapeutic strategies targeting EED, including allosteric inhibitors, PPI inhibitors, and PROTACs, together with brief discussions on the relevant challenges, opportunities, and future directions.

Indexed as

Epigenesis, GeneticPolycomb Repressive Complex 2Allosteric RegulationAnimalsAntineoplastic AgentsHumansMolecular Targeted TherapyNeoplasmsAntineoplastic AgentsEED protein, humanPolycomb Repressive Complex 2cancer therapyEEDepigenetic therapeuticsPRC2PROTACsprotein–protein interaction modulators

Identifiers

PMID38642703
PMCPMC11416859
OpenAlexW4394912477

What Socratic 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 Socratic graph.