Evidence map›Paper›PMID 24859458›Full record

ReviewBiochimica et biophysica acta2014

Targeting histone lysine demethylases - progress, challenges, and the future.

Cyrille C Thinnes, Katherine S England, Akane Kawamura, Rasheduzzaman Chowdhury, Christopher J Schofield, Richard J Hopkinson

Open access · hybridAbstract readReview
In one paragraph

Review in Biochimica et biophysica acta, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 97 papers.

0numbers the graph read from it
0cells of the map it votes in
97citing papers in PubMed
12.5field-weighted citation impact, top 1% 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

97 citing papers in PubMed, 188 citations in OpenAlex.

  1. Article
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  15. Article
  16. Chemical modulation ofWellcome open research · 2023
    Article
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37 more citing papers are in PubMed but not listed here.

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

6 authors at 1 institution in 1 country.

Cyrille C ThinnesThe Chemistry Research Laboratory, Mansfield Road, Oxford, OX1 3TA, UK.
Katherine S EnglandThe Chemistry Research Laboratory, Mansfield Road, Oxford, OX1 3TA, UK.
Akane KawamuraThe Chemistry Research Laboratory, Mansfield Road, Oxford, OX1 3TA, UK.
Rasheduzzaman ChowdhuryThe Chemistry Research Laboratory, Mansfield Road, Oxford, OX1 3TA, UK.
Christopher J SchofieldThe Chemistry Research Laboratory, Mansfield Road, Oxford, OX1 3TA, UK. Electronic address: christopher.schofield@chem.ox.ac.uk.
Richard J HopkinsonThe Chemistry Research Laboratory, Mansfield Road, Oxford, OX1 3TA, UK. Electronic address: richard.hopkinson@chem.ox.ac.uk.
Oxford Research Group · GB

Funding

Biotechnology and Biological Sciences Research Council BB/D011523/1British Heart Foundation RE/13/1/30181Cancer Research UK 18245Wellcome TrustWellcome Trust 086482/Z/08/Z
6 · The paper itself

Abstract

N-Methylation of lysine and arginine residues has emerged as a major mechanism of transcriptional regulation in eukaryotes. In humans, N(ε)-methyllysine residue demethylation is catalysed by two distinct subfamilies of demethylases (KDMs), the flavin-dependent KDM1 subfamily and the 2-oxoglutarate- (2OG) dependent JmjC subfamily, which both employ oxidative mechanisms. Modulation of histone methylation status is proposed to be important in epigenetic regulation and has substantial medicinal potential for the treatment of diseases including cancer and genetic disorders. This article provides an introduction to the enzymology of the KDMs and the therapeutic possibilities and challenges associated with targeting them, followed by a review of reported KDM inhibitors and their mechanisms of action from kinetic and structural perspectives.

Indexed as

AnimalsEnzyme InhibitorsHistone DemethylasesHumansModels, MolecularMolecular Targeted TherapyNeoplasmsProtein BindingEnzyme InhibitorsHistone DemethylasesDemethylaseEpigeneticsHistoneInhibitionLysineMethylation

Identifiers

PMID24859458
PMCPMC4316176
OpenAlexW2026848327

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.