Evidence map›Paper›PMID 33062173›Full record

ArticleACS medicinal chemistry letters2020

Gibberellin JRA-003: A Selective Inhibitor of Nuclear Translocation of IKKα.

James R Annand, Andrew R Henderson, Kyle S Cole, Aaron J Maurais, Jorge Becerra, Yejun Liu, Eranthie Weerapana, Angela N Koehler, Anna K Mapp, Corinna S Schindler

Open access · greenAbstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
0.3field-weighted citation impact, top 50% 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

5 citing papers in PubMed, 10 citations in OpenAlex.

  1. Stereoselective Synthesis and Antimicrobial Studies ofPharmaceuticals (Basel, Switzerland) · 2025
    Article
  2. Gibberellic Acid (GAChemistry & biodiversity · 2025
    Review
  3. Article
  4. Concise Synthesis of (-)-GAJournal of the American Chemical Society · 2023
    Article
  5. 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

10 authors at 3 institutions in 1 country.

James R AnnandDepartment of Chemistry, Willard-Henry-Dow Laboratory, University of Michigan, 930 North University Avenue, Ann Arbor, Michigan 48109, United States.
Andrew R HendersonProgram in Chemical Biology, University of Michigan, 210 Washtenaw Avenue, Ann Arbor, Michigan 48109, United States.
Kyle S ColeDepartment of Chemistry, Merkert Center, Boston College, 2609 Beacon Street., Chestnut Hill, Massachusetts 02467, United States.
Aaron J MauraisDepartment of Chemistry, Merkert Center, Boston College, 2609 Beacon Street., Chestnut Hill, Massachusetts 02467, United States.
Jorge BecerraProgram in Chemical Biology, University of Michigan, 210 Washtenaw Avenue, Ann Arbor, Michigan 48109, United States.
Yejun LiuProgram in Chemical Biology, University of Michigan, 210 Washtenaw Avenue, Ann Arbor, Michigan 48109, United States.
Eranthie WeerapanaDepartment of Chemistry, Merkert Center, Boston College, 2609 Beacon Street., Chestnut Hill, Massachusetts 02467, United States.
Angela N KoehlerDavid H. Koch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, 500 Main Street, Cambridge, Massachusetts 02139, United States.
Anna K MappDepartment of Chemistry, Willard-Henry-Dow Laboratory, University of Michigan, 930 North University Avenue, Ann Arbor, Michigan 48109, United States.
Corinna S SchindlerDepartment of Chemistry, Willard-Henry-Dow Laboratory, University of Michigan, 930 North University Avenue, Ann Arbor, Michigan 48109, United States.
Washtenaw Community College · USBoston College · USMassachusetts Institute of Technology · US

Funding

Probing transcriptional activation at the molecular level - Equipment SupplementR35GM136356 · NIGMS · UNIVERSITY OF MICHIGAN AT ANN ARBOR · PI ANNA K. MAPP · 2020 to 2026
$3.3M
Developing chemical-proteomic tools to investigate cysteine oxidationR35GM134964 · NIGMS · BOSTON COLLEGE · PI WEERAPANA, ERANTHIE · 2020 to 2024
$3.1M
Investigating cysteine PTMs in living cellsR01GM117004 · NIGMS · BOSTON COLLEGE · PI WEERAPANA, ERANTHIE · 2016 to 2019
$1.2M
NIGMS NIH HHS R01 GM117004NIGMS NIH HHS R35 GM134964NIGMS NIH HHS R35 GM136356
6 · The paper itself

Abstract

The small molecule gibberellin JRA-003 was identified as an inhibitor of the NF-kB (nuclear kappa-light-chain-enhancer of activated B cells) pathway. Here we find that JRA-003 binds to and significantly inhibits the nuclear translocation of pathway-activating kinases IKKα (IκB kinase alpha) and IKKβ (IκB kinase beta). Analogs of JRA-003 were synthesized and NF-κB-inhibiting gibberellins were found to be cytotoxic in cancer-derived cell lines (HS 578T, HCC 1599, RC-K8, Sud-HL4, CA 46, and NCIH 4466). Not only was JRA-003 identified as the most potent synthetic gibberellin against cancer-derived cell lines, it displayed no cytotoxicity in cells derived from noncancerous sources (HEK 293T, HS 578BST, HS 888Lu, HS 895Sk, HUVEC). This selectivity suggests a promising approach for the development of new therapeutics.

Identifiers

PMID33062173
PMCPMC7549252
OpenAlexW3028078672

What OpenQuestion holds

Textmetadata
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.