Evidence map›Paper›PMID 26603496›Full record

ArticleChemMedChem2016

Why Hydroxamates May Not Be the Best Histone Deacetylase Inhibitors--What Some May Have Forgotten or Would Rather Forget?

Sida Shen, Alan P Kozikowski

Open access · greenAbstract read
In one paragraph

Article in ChemMedChem, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 117 papers.

0numbers the graph read from it
0cells of the map it votes in
117citing papers in PubMed
4.8field-weighted citation impact, top 4% 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

117 citing papers in PubMed, 248 citations in OpenAlex.

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  16. Biology of novel LpxC inhibitors forMicrobiology spectrum · 2026
    Article
  17. Review
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  19. Article
  20. Article

57 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

2 authors at 1 institution in 1 country.

Sida ShenDrug Discovery Program, Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, Chicago, IL, 60612, USA.
Alan P KozikowskiDrug Discovery Program, Department of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, University of Illinois at Chicago, Chicago, IL, 60612, USA. kozikowa@uic.edu.
University of Illinois Chicago · US

Funding

Optimization of HDAC6 Inhibitors in the Treatment of CMTR01NS079183 · NINDS · UNIVERSITY OF ILLINOIS AT CHICAGO · PI KOZIKOWSKI, ALAN P., VAN DEN BOSCH, LUDO · 2013 to 2017
$1.9M
NINDS NIH HHS NS079183NINDS NIH HHS R01 NS079183
6 · The paper itself

Abstract

Hydroxamate-based histone deacetylase inhibitors (HDACIs) have been approved as therapeutic agents by the US Food and Drug Administration for use in oncology applications. While the potential utility of such HDACIs in other areas of medicinal chemistry is tremendous, there are significant concerns that "pan-HDAC inhibitors" may be too broadly acting and/or toxic for clinical use beyond oncology. In addition to the isozyme selectivity challenge, the potential mutagenicity of hydroxamate-containing HDAC inhibitors represents a major hindrance in their application to other therapeutic areas. Herein we report on the mutagenicity of known hydroxamates, discuss the mechanisms responsible for their genotoxicity, and review some of the current alternatives to hydroxamates. We conclude that the hydroxamate group, while providing high-potency HDACIs, is not necessarily the best zinc-binding group for HDACI drug discovery.

Indexed as

Drug DiscoveryHistone Deacetylase InhibitorsHistone DeacetylasesHumansHydroxamic AcidsMolecular StructureHistone Deacetylase InhibitorsHistone DeacetylasesHydroxamic Acidshistone deacetylase inhibitorshydroxamateLossen rearrangementmutagenicity

Identifiers

PMID26603496
PMCPMC4765907
OpenAlexW2179490146

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.