Evidence map›Paper›PMID 29764755›Full record

ReviewBioorganic & medicinal chemistry2018

Investigations on small molecule inhibitors targeting the histone H3K4 tri-methyllysine binding PHD-finger of JmjC histone demethylases.

Bhaskar Bhushan, Alexandre Erdmann, Yijia Zhang, Roman Belle, Catrine Johannson, Udo Oppermann, Richard J Hopkinson, Christopher J Schofield, Akane Kawamura

Open access · hybridAbstract readReview
In one paragraph

Review in Bioorganic & medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.

0numbers the graph read from it
0cells of the map it votes in
14citing papers in PubMed
1.1field-weighted citation impact, top 23% 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

14 citing papers in PubMed, 34 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
  4. Review
  5. Article
  6. Chemical tools targeting readers of lysine methylation.Current opinion in chemical biology · 2023
    Review
  7. Review
  8. Article
  9. Review
  10. Article
  11. Article
  12. Targeting protein methylation: from chemical tools to precision medicines.Cellular and molecular life sciences : CMLS · 2019
    Review
  13. Article
  14. 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 at 2 institutions in 1 country.

Bhaskar BhushanDepartment of Chemistry, University of Oxford, Mansfield Road, Oxford OX1 3TA, United Kingdom; Radcliffe Department of Medicine, Division of Cardiovascular Medicine, University of Oxford, The Wellcome Trust Centre for Human Genetics, Roosevelt Drive, Oxford OX3 7BN, United Kingdom.
Alexandre ErdmannDepartment of Chemistry, University of Oxford, Mansfield Road, Oxford OX1 3TA, United Kingdom.
Yijia ZhangDepartment of Chemistry, University of Oxford, Mansfield Road, Oxford OX1 3TA, United Kingdom.
Roman BelleDepartment of Chemistry, University of Oxford, Mansfield Road, Oxford OX1 3TA, United Kingdom.
Catrine JohannsonDepartment of Chemistry, University of Oxford, Mansfield Road, Oxford OX1 3TA, United Kingdom; Botnar Research Centre, NIHR Oxford Biomedical Research Unit, University of Oxford, Oxford, United Kingdom.
Udo OppermannBotnar Research Centre, NIHR Oxford Biomedical Research Unit, University of Oxford, Oxford, United Kingdom.
Richard J HopkinsonDepartment of Chemistry, University of Oxford, Mansfield Road, Oxford OX1 3TA, United Kingdom.
Christopher J SchofieldDepartment of Chemistry, University of Oxford, Mansfield Road, Oxford OX1 3TA, United Kingdom.
Akane KawamuraDepartment of Chemistry, University of Oxford, Mansfield Road, Oxford OX1 3TA, United Kingdom; Radcliffe Department of Medicine, Division of Cardiovascular Medicine, University of Oxford, The Wellcome Trust Centre for Human Genetics, Roosevelt Drive, Oxford OX3 7BN, United Kingdom. Electronic address: akane.kawamura@chem.ox.ac.uk.
University of Oxford · GBCentre for Human Genetics · GB

Funding

Arthritis Research UK 20522British Heart FoundationCancer Research UK 18245Cancer Research UK A18245Cancer Research UK C8717/A18245Versus Arthritis 20522Wellcome Trust 106244Wellcome Trust 203141/Z/16/Z
6 · The paper itself

Abstract

Plant homeodomain (PHD) containing proteins are important epigenetic regulators and are of interest as potential drug targets. Inspired by the amiodarone derivatives reported to inhibit the PHD finger 3 of KDM5A (KDM5A(PHD3)), a set of compounds were synthesised. Amiodarone and its derivatives were observed to weakly disrupt the interactions of a histone H3K4me3 peptide with KDM5A(PHD3). Selected amiodarone derivatives inhibited catalysis of KDM5A, but in a PHD-finger independent manner. Amiodarone derivatives also bind to H3K4me3-binding PHD-fingers from the KDM7 subfamily. Further work is required to develop potent and selective PHD finger inhibitors.

Indexed as

Drug Delivery SystemsAmiodaroneDrug Evaluation, PreclinicalHistone DemethylasesHistonesLysineMolecular StructurePhylogenyPlant ProteinsProtein BindingSmall Molecule LibrariesAmiodaroneHistone DemethylasesHistonesLysinePlant ProteinsSmall Molecule LibrariesEpigeneticsHistone demethylasesJmjC-KDMsPHD-finger inhibitorPlant Homeodomain

Identifiers

PMID29764755
PMCPMC6380468
OpenAlexW2790490201

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.