Evidence map›Paper›PMID 38291964›Full record

ArticleACS chemical biology2024

Development of Potent Dual BET/HDAC Inhibitors via Pharmacophore Merging and Structure-Guided Optimization.

Nicolas Bauer, Dimitrios-Ilias Balourdas, Joel R Schneider, Xin Zhang, Lena M Berger, Benedict-Tilman Berger, Martin P Schwalm, Nick A Klopp, Jens T Siveke, Stefan Knapp and 1 more

Open access · hybridAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in ACS chemical biology, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.

0numbers the graph read from it
0cells of the map it votes in
8citing papers in PubMed
3.3field-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

8 citing papers in PubMed, 14 citations in OpenAlex.

  1. Review
  2. Review
  3. Article
  4. Review
  5. Review
  6. [Design, Synthesis, and Efficacy Evaluation of a Novel BRD4/HDAC Dual-Target Small-Molecule Inhibitor in Prostate Cancer].Sichuan da xue xue bao. Yi xue ban = Journal of Sichuan University. Medical science edition · 2025
    Article
  7. Article
  8. Epigenetics-targeted drugs: current paradigms and future challenges.Signal transduction and targeted therapy · 2024
    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

11 authors at 2 institutions in 1 country.

Nicolas BauerInstitute of Pharmaceutical Chemistry, Goethe University, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany.ORCID 0009-0004-3448-9796
Dimitrios-Ilias BalourdasInstitute of Pharmaceutical Chemistry, Goethe University, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany.ORCID 0000-0002-1790-2268
Joel R SchneiderBridge Institute of Experimental Tumor Therapy, West German Cancer Center, University Hospital Essen, University of Duisburg-Essen, 45147 Essen, Germany.
Xin ZhangBridge Institute of Experimental Tumor Therapy, West German Cancer Center, University Hospital Essen, University of Duisburg-Essen, 45147 Essen, Germany.
Lena M BergerInstitute of Pharmaceutical Chemistry, Goethe University, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany.ORCID 0000-0002-7835-8067
Benedict-Tilman BergerInstitute of Pharmaceutical Chemistry, Goethe University, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany.ORCID 0000-0002-3314-2617
Martin P SchwalmInstitute of Pharmaceutical Chemistry, Goethe University, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany.ORCID 0000-0002-1252-1829
Nick A KloppBridge Institute of Experimental Tumor Therapy, West German Cancer Center, University Hospital Essen, University of Duisburg-Essen, 45147 Essen, Germany.
Jens T SivekeBridge Institute of Experimental Tumor Therapy, West German Cancer Center, University Hospital Essen, University of Duisburg-Essen, 45147 Essen, Germany.
Stefan KnappInstitute of Pharmaceutical Chemistry, Goethe University, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany.ORCID 0000-0001-5995-6494
Andreas C JoergerInstitute of Pharmaceutical Chemistry, Goethe University, Max-von-Laue-Str. 9, 60438 Frankfurt am Main, Germany.ORCID 0000-0002-1232-0138
Goethe University Frankfurt · DEGerman Cancer Research Center · DE

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Bromodomain and extra-terminal domain (BET) proteins and histone deacetylases (HDACs) are prime targets in cancer therapy. Recent research has particularly focused on the development of dual BET/HDAC inhibitors for hard-to-treat tumors, such as pancreatic cancer. Here, we developed a new series of potent dual BET/HDAC inhibitors by choosing starting scaffolds that enabled us to optimally merge the two functionalities into a single compound. Systematic structure-guided modification of both warheads then led to optimized binders that were superior in potency to both parent compounds, with the best molecules of this series binding to both BRD4 bromodomains as well as HDAC1/2 with EC

Indexed as

Antineoplastic AgentsCarcinomaPancreatic NeoplasmsBromodomain Containing ProteinsCell Cycle ProteinsCell Line, TumorHistone Deacetylase InhibitorsHumansNuclear ProteinsPharmacophoreRNA-Binding ProteinsTranscription FactorsAntineoplastic AgentsBRD4 protein, humanBromodomain Containing ProteinsCell Cycle ProteinsHEXIM1 protein, humanHistone Deacetylase InhibitorsNuclear ProteinsRNA-Binding ProteinsTranscription Factors

Identifiers

PMID38291964
PMCPMC10878397
OpenAlexW4391401640

What OpenQuestion holds

Textmetadata
LicenceCC BY
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.