Evidence map›Paper›PMID 35866162›Full record

ArticleRSC chemical biology2022

Monitoring GAPDH activity and inhibition with cysteine-reactive chemical probes.

Sarah E Canarelli, Brooke M Swalm, Eric T Larson, Michael J Morrison, Eranthie Weerapana

Open access · goldAbstract read
In one paragraph

Article in RSC chemical biology, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
0.3field-weighted citation impact, top 45% 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

4 citing papers in PubMed, 5 citations in OpenAlex.

  1. Review
  2. Article
  3. Article
  4. Review
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 at 1 institution in 1 country.

Sarah E CanarelliDepartment of Chemistry, Boston College Chestnut Hill Massachusetts 02467 USA eranthie@bc.edu.
Brooke M SwalmRheos Medicines, Inc Cambridge Massachusetts 02142 USA elarson@rheosrx.com mmorrison57@gmail.com.
Eric T LarsonRheos Medicines, Inc Cambridge Massachusetts 02142 USA elarson@rheosrx.com mmorrison57@gmail.com.ORCID https://orcid.org/0000-0002-2862-4291
Michael J MorrisonRheos Medicines, Inc Cambridge Massachusetts 02142 USA elarson@rheosrx.com mmorrison57@gmail.com.ORCID https://orcid.org/0000-0002-8948-1773
Eranthie WeerapanaDepartment of Chemistry, Boston College Chestnut Hill Massachusetts 02467 USA eranthie@bc.edu.ORCID https://orcid.org/0000-0002-0835-8301
Boston College · US

Funding

Developing chemical-proteomic tools to investigate cysteine oxidationR35GM134964 · NIGMS · BOSTON COLLEGE · PI WEERAPANA, ERANTHIE · 2020 to 2024
$3.1M
NIGMS NIH HHS R35 GM134964
6 · The paper itself

Abstract

Glyceraldehyde 3-phosphate dehydrogenase (GAPDH) is a central enzyme in glycolysis that regulates the Warburg effect in cancer cells. In addition to its role in metabolism, GAPDH is also implicated in diverse cellular processes, including transcription and apoptosis. Dysregulated GAPDH activity is associated with a variety of pathologies, and GAPDH inhibitors have demonstrated therapeutic potential as anticancer and immunomodulatory agents. Given the critical role of GAPDH in pathophysiology, it is important to have access to tools that enable rapid monitoring of GAPDH activity and inhibition within a complex biological system. Here, we report an electrophilic peptide-based probe, SEC1, which covalently modifies the active-site cysteine, C152, of GAPDH to directly report on GAPDH activity within a proteome. We demonstrate the utility of SEC1 to assess changes in GAPDH activity in response to oncogenic transformation, reactive oxygen species (ROS) and small-molecule GAPDH inhibitors, including Koningic acid (KA). We then further evaluated KA, to determine the detailed mechanism of inhibition. Our mechanistic studies confirm that KA is a highly effective irreversible inhibitor of GAPDH, which acts through a NAD

Identifiers

PMID35866162
PMCPMC9257626
OpenAlexW4285269377

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC
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.