Evidence map›Paper›PMID 33375520›Full record

ArticlePharmaceuticals (Basel, Switzerland)2020

Expanding the Structural Diversity of DNA Methyltransferase Inhibitors.

K Eurídice Juárez-Mercado, Fernando D Prieto-Martínez, Norberto Sánchez-Cruz, Andrea Peña-Castillo, Diego Prada-Gracia, José L Medina-Franco

Open access · goldAbstract read
In one paragraph

Article in Pharmaceuticals (Basel, Switzerland), 2020. 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
1.0field-weighted citation impact, top 24% 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, 24 citations in OpenAlex.

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  9. AnArtificial intelligence in the life sciences · 2021
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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 2 institutions in 1 country.

K Eurídice Juárez-MercadoDIFACQUIM Research Group, Department of Pharmacy, School of Chemistry, National Autonomous University of Mexico, Avenida Universidad 3000, Mexico City 04510, Mexico.ORCID 0000-0002-3283-8284
Fernando D Prieto-MartínezDIFACQUIM Research Group, Department of Pharmacy, School of Chemistry, National Autonomous University of Mexico, Avenida Universidad 3000, Mexico City 04510, Mexico.ORCID 0000-0002-0054-0862
Norberto Sánchez-CruzDIFACQUIM Research Group, Department of Pharmacy, School of Chemistry, National Autonomous University of Mexico, Avenida Universidad 3000, Mexico City 04510, Mexico.ORCID 0000-0003-2707-3966
Andrea Peña-CastilloDIFACQUIM Research Group, Department of Pharmacy, School of Chemistry, National Autonomous University of Mexico, Avenida Universidad 3000, Mexico City 04510, Mexico.
Diego Prada-GraciaResearch Unit on Computational Biology and Drug Design, Children's Hospital of Mexico Federico Gomez, Mexico City 06720, Mexico.ORCID 0000-0003-3375-870X
José L Medina-FrancoDIFACQUIM Research Group, Department of Pharmacy, School of Chemistry, National Autonomous University of Mexico, Avenida Universidad 3000, Mexico City 04510, Mexico.ORCID 0000-0003-4940-1107
Universidad Nacional Autónoma de México · MXHospital Infantil de México Federico Gómez · MX

Funding

Consejo Nacional de Ciencia y Tecnología 282785
6 · The paper itself

Abstract

Inhibitors of DNA methyltransferases (DNMTs) are attractive compounds for epigenetic drug discovery. They are also chemical tools to understand the biochemistry of epigenetic processes. Herein, we report five distinct inhibitors of DNMT1 characterized in enzymatic inhibition assays that did not show activity with DNMT3B. It was concluded that the dietary component theaflavin is an inhibitor of DNMT1. Two additional novel inhibitors of DNMT1 are the approved drugs glyburide and panobinostat. The DNMT1 enzymatic inhibitory activity of panobinostat, a known pan inhibitor of histone deacetylases, agrees with experimental reports of its ability to reduce DNMT1 activity in liver cancer cell lines. Molecular docking of the active compounds with DNMT1, and re-scoring with the recently developed extended connectivity interaction features approach, led to an excellent agreement between the experimental IC

Indexed as

chemoinformaticsdietary componentenzyme inhibitionepigeneticsepi-informaticsfocused librarymultitarget epigenetic agentnatural products

Identifiers

PMID33375520
PMCPMC7824300
OpenAlexW3113720224

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.