Evidence map›Paper›PMID 28527406›Full record

ArticleEuropean journal of medicinal chemistry2017

The relevance of K

Hannah Wapenaar, Thea van den Bosch, Niek G J Leus, Petra E van der Wouden, Nikolaos Eleftheriadis, Jos Hermans, Gebremedhin Solomon Hailu, Dante Rotili, Antonello Mai, Alexander Dömling and 3 more

Open access · bronzeAbstract read
In one paragraph

Article in European journal of medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 6 papers.

0numbers the graph read from it
0cells of the map it votes in
6citing papers in PubMed
0.4field-weighted citation impact, top 37% 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

6 citing papers in PubMed, 10 citations in OpenAlex.

  1. Review
  2. Reversible Acetylation of Non-histone Proteins in Human Cancers.Results and problems in cell differentiation · 2025
    Review
  3. Article
  4. Article
  5. Article
  6. 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

13 authors at 2 institutions in 2 countries.

Hannah WapenaarUniversity of Groningen, Groningen Research Institute of Pharmacy, Department of Chemical and Pharmaceutical Biology, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands.
Thea van den BoschUniversity of Groningen, Groningen Research Institute of Pharmacy, Department of Chemical and Pharmaceutical Biology, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands.
Niek G J LeusUniversity of Groningen, Groningen Research Institute of Pharmacy, Department of Chemical and Pharmaceutical Biology, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands.
Petra E van der WoudenUniversity of Groningen, Groningen Research Institute of Pharmacy, Department of Chemical and Pharmaceutical Biology, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands.
Nikolaos EleftheriadisUniversity of Groningen, Groningen Research Institute of Pharmacy, Department of Chemical and Pharmaceutical Biology, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands.
Jos HermansUniversity of Groningen, Groningen Research Institute of Pharmacy, Department of Analytical Biochemistry, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands.
Gebremedhin Solomon HailuDepartment of Drug Chemistry and Technologies, Sapienza University of Rome, P.le A. Moro 5, 00185 Rome, Italy.
Dante RotiliDepartment of Drug Chemistry and Technologies, Sapienza University of Rome, P.le A. Moro 5, 00185 Rome, Italy.
Antonello MaiDepartment of Drug Chemistry and Technologies, Sapienza University of Rome, P.le A. Moro 5, 00185 Rome, Italy.
Alexander DömlingUniversity of Groningen, Groningen Research Institute of Pharmacy, Department of Drug Design, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands.
Rainer BischoffUniversity of Groningen, Groningen Research Institute of Pharmacy, Department of Analytical Biochemistry, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands.
Hidde J HaismaUniversity of Groningen, Groningen Research Institute of Pharmacy, Department of Chemical and Pharmaceutical Biology, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands.
Frank J DekkerUniversity of Groningen, Groningen Research Institute of Pharmacy, Department of Chemical and Pharmaceutical Biology, Antonius Deusinglaan 1, 9713 AV Groningen, The Netherlands. Electronic address: f.j.dekker@rug.nl.
University of Groningen · NLSapienza University of Rome · IT

Funding

European Research Council 309782
6 · The paper itself

Abstract

Histone acetyltransferases (HATs) are important mediators of epigenetic post-translational modifications of histones that play important roles in health and disease. A disturbance of these modifications can result in disease states, such as cancer or inflammatory diseases. Inhibitors of HATs (HATi) such as lysine (K) acetyltransferase 8 (KAT8), could be used to study the epigenetic processes in diseases related to these enzymes or to investigate HATs as therapeutic targets. However, the development of HATi is challenged by the difficulties in kinetic characterization of HAT enzymes and their inhibitors to enable calculation of a reproducible inhibitory potency. In this study, a fragment screening approach was used, enabling identification of 4-amino-1-naphthol, which potently inhibited KAT8. The inhibitor was investigated for enzyme inhibition using kinetic and calorimetric binding studies. This allowed for calculation of the K

Indexed as

Dose-Response Relationship, DrugEnzyme InhibitorsHistone AcetyltransferasesHumansKineticsMolecular StructureNaphtholsStructure-Activity RelationshipEnzyme InhibitorsHistone AcetyltransferasesKAT8 protein, humanNaphtholsEnzyme kineticsFragment screeningHistone acetylationHistone acetyltransferasesInhibitorKAT8

Identifiers

PMID28527406
PMCPMC5720340
OpenAlexW2610664061

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.