Evidence map›Paper›PMID 39762580›Full record

ArticleCommunications chemistry2025

Modulation of Nrf2 expression by targeting i-motif DNA.

E F Warner, D Guneri, M A O'Connell, C J MacDonald, Z A E Waller

Abstract read
In one paragraph

Article in Communications chemistry, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing papers in PubMed
–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

2 citing papers in PubMed.

  1. Article
  2. 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.

E F WarnerSchool of Chemistry, Pharmacy and Pharmacology, University of East Anglia, Norwich, Norfolk, UK.
D GuneriUCL School of Pharmacy, London, UK.ORCID http://orcid.org/0000-0003-0858-1746
M A O'ConnellSchool of Chemistry, Pharmacy and Pharmacology, University of East Anglia, Norwich, Norfolk, UK.
C J MacDonaldSchool of Chemistry, Pharmacy and Pharmacology, University of East Anglia, Norwich, Norfolk, UK.
Z A E WallerUCL School of Pharmacy, London, UK. z.waller@ucl.ac.uk.ORCID http://orcid.org/0000-0001-8538-0484

Funding

RCUK | Biotechnology and Biological Sciences Research Council (BBSRC) BB/W001616/1Wellcome TrustWellcome Trust (Wellcome) 204515/Z/16/Z
6 · The paper itself

Abstract

Nuclear factor (erythroid-derived 2)-like 2 (Nrf2) is a key regulator of cell detoxification, which maintains homoeostasis in healthy cells and promotes chemoresistance in cancer cells. Controlling the expression of this transcription factor is therefore of great interest. There are many compounds that have been shown to induce Nrf2 expression, but ligands that can inhibit Nrf2 are scant. Herein we characterise an i-motif-forming sequence downstream of the Nrf2 promoter, which we hypothesised may regulate the expression of the gene. The Nrf2 i-motif was found to be stable at near-physiological conditions. We identified small molecule ligands that interact with this i-motif structure and one significantly upregulated Nrf2 mRNA expression, and one ligand reduced Nrf2 mRNA expression in human cancer cells. This is the first example of controlling the promoter of Nrf2 by targeting DNA structures and offers an alternative mode of action for the development of compounds to improve the chemotherapeutic responsiveness of existing treatments for cancer.

Identifiers

PMID39762580
PMCPMC11704350

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Registered trials

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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.