Evidence map›Paper›PMID 30613344›Full record

ArticleACS medicinal chemistry letters2018

Molecular Basis for the Selective Inhibition of Histone Deacetylase 6 by a Mercaptoacetamide Inhibitor.

Nicholas J Porter, Sida Shen, Cyril Barinka, Alan P Kozikowski, David W Christianson

Open access · greenAbstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.

0numbers the graph read from it
0cells of the map it votes in
13citing papers in PubMed
1.6field-weighted citation impact, top 16% 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

13 citing papers in PubMed, 30 citations in OpenAlex.

  1. Review
  2. Article
  3. Review
  4. Article
  5. Design, Synthesis and Antitumor Activity of 1International journal of molecular sciences · 2023
    Article
  6. Review
  7. Binding of inhibitors to active-site mutants of CD1, the enigmatic catalytic domain of histone deacetylase 6.Acta crystallographica. Section F, Structural biology communications · 2020
    Article
  8. Review
  9. Review
  10. Article
  11. Article
  12. Review
  13. 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

5 authors at 3 institutions in 2 countries.

Nicholas J PorterRoy and Diana Vagelos Laboratories, Department of Chemistry, University of Pennsylvania, Philadelphia, Pennsylvania 19104-6323, United States.
Sida ShenDepartment of Medicinal Chemistry and Pharmacognosy, Drug Discovery Program, University of Illinois at Chicago, Chicago, Illinois 60612, United States.
Cyril BarinkaLaboratory of Structural Biology, Institute of Biotechnology of the Czech Academy of Sciences, Prumyslova 595, 252 50 Vestec, Czech Republic.
Alan P KozikowskiStarWise Therapeutics LLC, 505 South Rosa Road, Madison, Wisconsin 53719, United States.
David W ChristiansonRoy and Diana Vagelos Laboratories, Department of Chemistry, University of Pennsylvania, Philadelphia, Pennsylvania 19104-6323, United States.
University of Pennsylvania · USCzech Academy of Sciences · CZUniversity of Illinois Chicago · US

Funding

Overall EvaluationP41GM103403 · NIGMS · CORNELL UNIVERSITY · PI EALICK, STEVEN E · 2012 to 2017
$14.3M
Structure and Function of MetalloenzymesR01GM049758 · NIGMS · UNIVERSITY OF PENNSYLVANIA · PI CHRISTIANSON, DAVID W · 1994 to 2025
$7.6M
NIGMS NIH HHS P41 GM103403NIGMS NIH HHS R01 GM049758
6 · The paper itself

Abstract

Mercaptoacetamide histone deacetylase inhibitors are neuroprotective agents that do not exhibit the genotoxicity associated with more commonly used hydroxamate inhibitors. Here, we present the crystal structure of a selective mercaptoacetamide complexed with the C-terminal catalytic domain of HDAC6. When compared with the structure of a mercaptoacetamide bound to the class I isozyme HDAC8, different interactions are observed with the conserved tandem histidine pair in the active site. These differences likely contribute to the selectivity for inhibition of HDAC6, an important target for cancer chemotherapy and the treatment of neurodegenerative disease.

Identifiers

PMID30613344
PMCPMC6295862
OpenAlexW2900916306

What OpenQuestion holds

Textmetadata
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.