Evidence map›Paper›PMID 26118420›Full record

ArticleJournal of enzyme inhibition and medicinal chemistry2016

Resveratrol-salicylate derivatives as selective DNMT3 inhibitors and anticancer agents.

Fahad S Aldawsari, Rodrigo Aguayo-Ortiz, Kanishk Kapilashrami, Jakyung Yoo, Minkui Luo, José L Medina-Franco, Carlos A Velázquez-Martínez

Open access · greenAbstract read
In one paragraph

Article in Journal of enzyme inhibition and medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.

0numbers the graph read from it
0cells of the map it votes in
18citing papers in PubMed
2.5field-weighted citation impact, top 11% 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

18 citing papers in PubMed, 57 citations in OpenAlex.

  1. Review
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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

7 authors at 4 institutions in 4 countries.

Fahad S Aldawsaria Faculty of Pharmacy and Pharmaceutical Sciences , University of Alberta , Edmonton, Alberta , Canada .
Rodrigo Aguayo-Ortizb Departamento de Farmacia, Facultad de Química , Universidad Nacional Autónoma de México , México City , Mexico .
Kanishk Kapilashramic Molecular Pharmacology and Chemistry Program, Memorial Sloan-Kettering Cancer Center , New York , NY , USA , and.
Jakyung Yood Life Science Research Institute, Daewoong Pharmaceutical Co., Ltd. , Pogok-Eup , Republic of Korea.
Minkui Luoc Molecular Pharmacology and Chemistry Program, Memorial Sloan-Kettering Cancer Center , New York , NY , USA , and.
José L Medina-Francob Departamento de Farmacia, Facultad de Química , Universidad Nacional Autónoma de México , México City , Mexico .
Carlos A Velázquez-Martíneza Faculty of Pharmacy and Pharmaceutical Sciences , University of Alberta , Edmonton, Alberta , Canada .
Memorial Sloan Kettering Cancer Center · USUniversidad Nacional Autónoma de México · MXUniversity of Alberta · CADaewoong Pharmaceutical (South Korea) · KR

Funding

X-RAY CRYSTALLOGRAPHYP30CA008748 · NCI · SLOAN-KETTERING INSTITUTE FOR CANCER RES · PI Nicholas D Socci · 1985 to 2026
$347.4M
Profile substrates and inhibitors of protein lysine methyltransferaseR01GM096056 · NIGMS · SLOAN-KETTERING INST CAN RESEARCH · PI LUO, MINKUI · 2011 to 2018
$3.2M
Enzyme-engineering Approaches to Dissect Protein Methylation ProfilesDP2OD007335 · OD · SLOAN-KETTERING INST CAN RESEARCH · PI LUO, MINKUI · 2010 to 2010
$2.9M
NCI NIH HHS P30 CA008748NIGMS NIH HHS R01 GM096056NIH HHS DP2 OD007335
6 · The paper itself

Abstract

Resveratrol is a natural polyphenol with plethora of biological activities. Resveratrol has previously shown to decrease DNA-methyltransferase (DNMT) enzymes expression and to reactivate silenced tumor suppressor genes. Currently, it seems that no resveratrol analogs have been developed as DNMT inhibitors. Recently, we reported the synthesis of resveratrol-salicylate derivatives and by examining the chemical structure of these analogs, we proposed that these compounds could exhibit DNMT inhibition especially that they resembled NSC 14778, a compound we previously identified as a DNMT inhibitor by virtual screening. Indeed, using in vitro DNMT inhibition assay, some of the resveratrol-salicylate analogs we screened in this work that showed selective inhibition against DNMT3 enzymes which were greater than resveratrol. A molecular docking study revealed key binding interactions with DNMT3A and DNMT3B enzymes. In addition, the most active analog, 10 showed considerable cytotoxicity against three human cancer cells; HT-29, HepG2 and SK-BR-3, which was greater than resveratrol. Further studies are needed to understand the anticancer mechanisms of these derivatives.

Indexed as

Antineoplastic AgentsCell Line, TumorCell SurvivalDNA (Cytosine-5-)-MethyltransferasesDNA Methyltransferase 3BEnzyme ActivationHep G2 CellsHT29 CellsHumansInhibitory Concentration 50Models, MolecularMolecular StructureProtein BindingResveratrolSalicylatesStilbenesAntineoplastic AgentsDNA (Cytosine-5-)-MethyltransferasesDNA Methyltransferase 3BResveratrolSalicylatesStilbenesAspirinchemopreventionDNMTdockingresveratrol

Identifiers

PMID26118420
PMCPMC4828318
OpenAlexW1831077942

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.