Evidence map›Paper›PMID 31218726›Full record

ReviewMedicinal research reviews2020

Epigenetic polypharmacology: A new frontier for epi-drug discovery.

Daniela Tomaselli, Alessia Lucidi, Dante Rotili, Antonello Mai

Abstract readReview
In one paragraph

Review in Medicinal research reviews, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 58 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
58citing papers in PubMed, 1 pooled it
–field-weighted citation impact
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

58 citing papers in PubMed, 1 synthesis or guideline pooled it.

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  20. Novel dual inhibitor targeting CDC25 and HDAC for treating triple-negative breast cancer.Apoptosis : an international journal on programmed cell death · 2024
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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

4 authors.

Daniela TomaselliDepartment of Chemistry and Technologies of Drugs, "Sapienza" University of Rome, Rome, Italy.
Alessia LucidiDepartment of Chemistry and Technologies of Drugs, "Sapienza" University of Rome, Rome, Italy.
Dante RotiliDepartment of Chemistry and Technologies of Drugs, "Sapienza" University of Rome, Rome, Italy.
Antonello MaiDepartment of Chemistry and Technologies of Drugs, "Sapienza" University of Rome, Rome, Italy.ORCID 0000-0001-9176-2382

Funding

Histone Lysine deMethylation: Structures, Inhibitions and MechanismsR01GM114306 · NIGMS · UNIVERSITY OF TX MD ANDERSON CAN CTR · PI CHENG, XIAODONG · 2015 to 2018
$1.2M
NIGMS NIH HHS R01 GM114306
6 · The paper itself

Abstract

Recently, despite the great success achieved by the so-called "magic bullets" in the treatment of different diseases through a marked and specific interaction with the target of interest, the pharmacological research is moving toward the development of "molecular network active compounds," embracing the related polypharmacology approach. This strategy was born to overcome the main limitations of the single target therapy leading to a superior therapeutic effect, a decrease of adverse reactions, and a reduction of potential mechanism(s) of drug resistance caused by robustness and redundancy of biological pathways. It has become clear that multifactorial diseases such as cancer, neurological, and inflammatory disorders, may require more complex therapeutic approaches hitting a certain biological system as a whole. Concerning epigenetics, the goal of the multi-epi-target approach consists in the development of small molecules able to simultaneously and (often) reversibly bind different specific epi-targets. To date, two dual histone deacetylase/kinase inhibitors (CUDC-101 and CUDC-907) are in an advanced stage of clinical trials. In the last years, the growing interest in polypharmacology encouraged the publication of high-quality reviews on combination therapy and hybrid molecules. Hence, to update the state-of-the-art of these therapeutic approaches avoiding redundancy, herein we focused only on multiple medication therapies and multitargeting compounds exploiting epigenetic plus nonepigenetic drugs reported in the literature in 2018. In addition, all the multi-epi-target inhibitors known in literature so far, hitting two or more epigenetic targets, have been included.

Indexed as

Drug DiscoveryEpigenesis, GeneticPolypharmacologyAnimalsClinical Trials as TopicHumansLigandsNeoplasmsLigandscancerepigeneticshybrid molecules designpolypharmacology

Identifiers

PMID31218726
PMCPMC6917854

What OpenQuestion holds

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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.