Evidence map›Paper›PMID 22549716›Full record

ReviewMedicinal research reviews2012

Small molecule modulators of Keap1-Nrf2-ARE pathway as potential preventive and therapeutic agents.

Sadagopan Magesh, Yu Chen, Longqin Hu

Open access · greenAbstract readReview
In one paragraph

Review in Medicinal research reviews, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 336 papers, 1 of them a synthesis that pooled it.

0numbers the graph read from it
0cells of the map it votes in
336citing papers in PubMed, 1 pooled it
16.9field-weighted citation impact, top 1% 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

336 citing papers in PubMed, 1 synthesis or guideline pooled it, 749 citations in OpenAlex.

  1. Pooled it
  2. Review
  3. Article
  4. International journal of molecular sciences · 2026
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  18. Drynachromoside A fromRedox report : communications in free radical research · 2025
    Article
  19. Flavonoids fromRedox report : communications in free radical research · 2025
    Article
  20. Article

276 more citing papers are in PubMed but not listed here.

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 2 institutions in 1 country.

Sadagopan MageshDepartment of Medicinal Chemistry, Ernest Mario School of Pharmacy, Rutgers, The State University of New Jersey, 160 Frelinghuysen Road, Piscataway, NJ 08854, USA.
Yu Chen
Longqin Hu
Rutgers, The State University of New Jersey · USCancer Institute of Florida · US

Funding

Homogenous HTS Assays to Screen for Inhibitors of Keap1-Nrf2 InteractionR01CA133791 · NCI · RUTGERS, THE STATE UNIV OF N.J. · PI HU, LONGQIN · 2008 to 2010
$876k
Novel Keap1-Nrf2 Inhibitors as Chemopreventive AgentsR03CA125868 · NCI · RUTGERS, THE STATE UNIV OF N.J. · PI HU, LONGQIN · 2007 to 2008
$155k
HTS fluorescence polarization assay for inhibitors of Keap1-Nrf2 interactionR03MH093197 · NIMH · RUTGERS, THE STATE UNIV OF N.J. · PI HU, LONGQIN · 2011 to 2012
$85k
NCI NIH HHS CA125868NCI NIH HHS CA133791NCI NIH HHS R01 CA133791NCI NIH HHS R03 CA125868NIMH NIH HHS MH093197NIMH NIH HHS R03 MH093197
6 · The paper itself

Abstract

Kelch-like ECH-associated protein 1 (Keap1)-nuclear factor erythroid 2-related factor 2 (Nrf2)-antioxidant response elements (ARE) pathway represents one of the most important cellular defense mechanisms against oxidative stress and xenobiotic damage. Activation of Nrf2 signaling induces the transcriptional regulation of ARE-dependent expression of various detoxifying and antioxidant defense enzymes and proteins. Keap1-Nrf2-ARE signaling has become an attractive target for the prevention and treatment of oxidative stress-related diseases and conditions including cancer, neurodegenerative, cardiovascular, metabolic, and inflammatory diseases. Over the last few decades, numerous Nrf2 inducers have been developed and some of them are currently undergoing clinical trials. Recently, overactivation of Nrf2 has been implicated in cancer progression as well as in drug resistance to cancer chemotherapy. Thus, Nrf2 inhibitors could potentially be used to improve the effectiveness of cancer therapy. Herein, we review the signaling mechanism of Keap1-Nrf2-ARE pathway, its disease relevance, and currently known classes of small molecule modulators. We also discuss several aspects of Keap1-Nrf2 interaction, Nrf2-based peptide inhibitor design, and the screening assays currently used for the discovery of direct inhibitors of Keap1-Nrf2 interaction.

Indexed as

Signal TransductionAnimalsAnti-Inflammatory AgentsAntineoplastic AgentsAntioxidantsHumansHypoglycemic AgentsIntracellular Signaling Peptides and ProteinsNeuroprotective AgentsNF-E2-Related Factor 2Oxidative StressResponse ElementsAnti-Inflammatory AgentsAntineoplastic AgentsAntioxidantsHypoglycemic AgentsIntracellular Signaling Peptides and ProteinsNeuroprotective AgentsNF-E2-Related Factor 2

Identifiers

PMID22549716
PMCPMC3393814
OpenAlexW1767659454

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.