Evidence map›Paper›PMID 37116763›Full record

ArticleBioorganic & medicinal chemistry letters2023

Optimization of 3-aminotetrahydrothiophene 1,1-dioxides with improved potency and efficacy as non-electrophilic antioxidant response element (ARE) activators.

Jeyun Jo, Jisu Kim, Lara Ibrahim, Manoj Kumar, Jonathan Iaconelli, Cong So Tran, Hyung Ryong Moon, Yunjin Jung, R Luke Wiseman, Luke L Lairson and 3 more

Open access · greenAbstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2023. 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
0.5field-weighted citation impact, top 34% 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

2 citing papers in PubMed, 3 citations in OpenAlex.

  1. Article
  2. HPPE Activates NRF2 Signaling by Liberating Heavy Metal Stores.Chembiochem : a European journal of chemical biology · 2025
    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

13 authors at 3 institutions in 2 countries.

Jeyun JoCollege of Pharmacy, Pusan National University, Busan 46241, Republic of Korea.
Jisu KimCollege of Pharmacy, Pusan National University, Busan 46241, Republic of Korea.
Lara IbrahimDepartment of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, United States; Department of Molecular Medicine, The Scripps Research Institute, La Jolla, CA 92037, United States.
Manoj KumarCalifornia Institute for Biomedical Research, La Jolla, CA 92037, United States.
Jonathan IaconelliDepartment of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, United States.
Cong So TranCollege of Pharmacy, Pusan National University, Busan 46241, Republic of Korea.
Hyung Ryong MoonCollege of Pharmacy, Pusan National University, Busan 46241, Republic of Korea; Research Institute for Drug Development, Pusan National University, Busan 46241, Republic of Korea.
Yunjin JungCollege of Pharmacy, Pusan National University, Busan 46241, Republic of Korea; Research Institute for Drug Development, Pusan National University, Busan 46241, Republic of Korea.
R Luke WisemanDepartment of Molecular Medicine, The Scripps Research Institute, La Jolla, CA 92037, United States.
Luke L LairsonDepartment of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, United States.
Arnab K ChatterjeeDepartment of Molecular Medicine, The Scripps Research Institute, La Jolla, CA 92037, United States.
Michael J BollongDepartment of Chemistry, The Scripps Research Institute, La Jolla, CA 92037, United States. Electronic address: mbollong@scripps.edu.
Hwayoung YunCollege of Pharmacy, Pusan National University, Busan 46241, Republic of Korea; Research Institute for Drug Development, Pusan National University, Busan 46241, Republic of Korea. Electronic address: hyun@pusan.ac.kr.
Pusan National University · KRScripps Research Institute · USCalifornia Institute for Biomedical Research · US

Funding

Discovering small molecules activators of stress responsive signalingR01AG046495 · NIA · SCRIPPS RESEARCH INSTITUTE, THE · PI JEFFERY W KELLY, Rockland Luke Wiseman · 2013 to 2026
$6.0M
Discovering Small Molecule Activators of Stress-Responsive SignalingRF1AG046495 · NIA · SCRIPPS RESEARCH INSTITUTE, THE · PI KELLY, JEFFERY W, WISEMAN, ROCKLAND LUKE · 2023 to 2025
$2.8M
Methods and approaches to expand the pharmacological toolsetR35GM146865 · NIGMS · SCRIPPS RESEARCH INSTITUTE, THE · PI Michael J Bollong · 2022 to 2026
$2.3M
NIA NIH HHS R01 AG046495NIA NIH HHS RF1 AG046495NIGMS NIH HHS R35 GM146865
6 · The paper itself

Abstract

Activating NRF2-driven transcription with non-electrophilic small molecules represents an attractive strategy to therapeutically target disease states associated with oxidative stress and inflammation. In this study, we describe a campaign to optimize the potency and efficacy of a previously identified bis-sulfone based non-electrophilic ARE activator 2. This work identifies the efficacious analog 17, a compound with a non-cytotoxic profile in IMR32 cells, as well as ARE activators 18 and 22, analogs with improved cellular potency. In silico drug-likeness prediction suggested the optimized bis-sulfones 17, 18, and 22 will likely be of pharmacological utility.

Indexed as

Antioxidant Response ElementsAntioxidantsNF-E2-Related Factor 2Oxidative StressAntioxidantsNF-E2-Related Factor 2ARE activatorDrug-likenessNon-electrophilicNRF2PGK1 inhibitor

Identifiers

PMID37116763
PMCPMC10241094
OpenAlexW4367043463

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.