Evidence map›Paper›PMID 30637990›Full record

ArticleChemical biology & drug design2019

Bisubstrate inhibitors to target histone acetyltransferase 1.

Liza Ngo, Tyler Brown, Yujun G Zheng

Open access · greenAbstract read
In one paragraph

Article in Chemical biology & drug design, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.

0numbers the graph read from it
0cells of the map it votes in
12citing papers in PubMed
1.3field-weighted citation impact, top 21% 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

12 citing papers in PubMed, 26 citations in OpenAlex.

  1. Article
  2. Article
  3. Article
  4. Review
  5. Review
  6. Article
  7. Review
  8. Review
  9. Recent insights intoEpigenetics · 2021
    Review
  10. Targeting a critical step in fungal hexosamine biosynthesis.The Journal of biological chemistry · 2020
    Article
  11. Review
  12. 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

3 authors at 1 institution in 1 country.

Liza NgoDepartment of Pharmaceutical and Biomedical Sciences, College of Pharmacy, University of Georgia, Athens, Georgia.
Tyler BrownDepartment of Pharmaceutical and Biomedical Sciences, College of Pharmacy, University of Georgia, Athens, Georgia.
Yujun G ZhengDepartment of Pharmaceutical and Biomedical Sciences, College of Pharmacy, University of Georgia, Athens, Georgia.ORCID 0000-0001-7116-3067
University of Georgia · US

Funding

Mechanism and Inhibition of Protein Arginine MethylationR01GM126154 · NIGMS · UNIVERSITY OF GEORGIA · PI ZHENG, Y. GEORGE · 2018 to 2021
$1.2M
NIGMS NIH HHS R01 GM126154
6 · The paper itself

Abstract

Developing selective enzyme inhibitors allows for the expansion of molecular toolboxes to investigate functions and activities of target enzymes. The histone acetyltransferase 1 (HAT1) is among the first histone acetyltransferase (HAT) enzymes that were discovered in the mid-1990s; however, it remains one of the poorly studied enzymes in comparison with the other HATs. Although HAT1 has been linked to various disease states, no inhibitors have been reported to target HAT1. Here, we designed a set of peptide-CoA conjugates as bisubstrate inhibitors of HAT1 with submicromolar potency. In particular, the bisubstrate inhibitor H4K12CoA exhibited a low K

Indexed as

Amino Acid SequenceBinding, CompetitiveEnzyme InhibitorsHistone AcetyltransferasesHumansInhibitory Concentration 50KineticsRecombinant ProteinsSubstrate SpecificityEnzyme InhibitorsHistone Acetyltransferaseshistone acetyltransferase type B complexRecombinant Proteinsbisubstrate inhibitorchemical probesepigeneticsHATHAT1histone acetyltransferase

Identifiers

PMID30637990
PMCPMC6533141
OpenAlexW2910701220

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.