ArticleJournal of enzyme inhibition and medicinal chemistry2013
Evaluation of a dithiocarbamate derivative as an inhibitor of human glutaredoxin-1.
Article in Journal of enzyme inhibition and medicinal chemistry, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.
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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.
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Who cites it
13 citing papers in PubMed, 27 citations in OpenAlex.
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- Electrophiles modulate glutathione reductase activity via alkylation and upregulation of glutathione biosynthesis.Redox biology · 2019Article
- Red fluorescent redox-sensitive biosensor Grx1-roCherry.Redox biology · 2019Article
- Role of glutathione metabolism in host defense againstProceedings of the National Academy of Sciences of the United States of America · 2018Article
- Redox-Inactive Peptide Disrupting Trx1-Ask1 Interaction for Selective Activation of Stress Signaling.Biochemistry · 2018Article
- Di-2-pyridylhydrazone Dithiocarbamate Butyric Acid Ester Exerted Its Proliferative Inhibition against Gastric Cell via ROS-Mediated Apoptosis and Autophagy.Oxidative medicine and cellular longevity · 2018Article
- Article
- Glutathione Disulfide Liposomes - a Research Tool for the Study of Glutathione Disulfide Associated Functions and Dysfunctions.Biochemistry and biophysics reports · 2016Article
- Why high cholesterol levels help hematological malignancies: role of nuclear lipid microdomains.Lipids in health and disease · 2016Article
- MitoNEET Protects HL-1 Cardiomyocytes from Oxidative Stress Mediated Apoptosis in an In Vitro Model of Hypoxia and Reoxygenation.PloS one · 2016Article
- Evaluation of a dithiocarbamate derivative as a model of thiol oxidative stress in H9c2 rat cardiomyocytes.Free radical biology & medicine · 2014Article
- Monitoring intracellular redox changes in ozone-exposed airway epithelial cells.Environmental health perspectives · 2013Article
Corrections and comments
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Authors and funding
5 authors at 3 institutions in 1 country.
Funding
Abstract
contextGlutaredoxins (GRX) are involved in the regulation of thiol redox state. GRX-1 is a cytosolic enzyme responsible for the catalysis of deglutathionylation of proteins. To date, very few inhibitors of GRX-1 have been reported.
objectiveThe objective of this paper is to report 2-acetylamino-3-[4-(2-acetylamino-2-carboxyethyl-sulfanylthiocarbonylamino)phenylthiocarbamoylsulfanyl]propionic acid (2-AAPA) as an inhibitor of human GRX-1. MATERIALS AND
methodsThe mechanism of inhibition of GRX-1 was investigated using dialysis, substrate protection, and mass spectrometry.
results2-AAPA inhibits GRX-1 in a time and concentration dependent manner. The activity did not return following dialysis indicating that inhibition is irreversible. Results of substrate protection and mass spectrometry indicate that the inhibition is occurring at the active site. The compound also produced GRX inhibition in human ovarian cancer cells. DISCUSSION: 2-AAPA is an irreversible GRX-1 inhibitor with similar or greater potency compared to previously reported inhibitors.
conclusionThe inhibition of GRX-1 by 2-AAPA could be used as a tool to study thiol redox state.
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Registered trials
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