ArticleJournal of enzyme inhibition and medicinal chemistry2017
A new nitrobenzoxadiazole-based GSTP1-1 inhibitor with a previously unheard of mechanism of action and high stability.
Article in Journal of enzyme inhibition and medicinal chemistry, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed.
- Review
- Overexpression of Glutathione S-Transferases in Human Diseases: Drug Targets and Therapeutic Implications.Antioxidants (Basel, Switzerland) · 2023Review
- Inhibition Analysis and High-Resolution Crystal Structure ofBiomolecules · 2023Article
- Monocarbonyl Curcumin Analogues as Potent Inhibitors against Human Glutathione Transferase P1-1.Antioxidants (Basel, Switzerland) · 2022Article
- Automated approach for the evaluation of glutathione-S-transferase P1-1 inhibition by organometallic anticancer compounds.Journal of enzyme inhibition and medicinal chemistry · 2022Article
- Glutathione-Biomolecules · 2022Article
- The Nitrobenzoxadiazole Derivative NBDHEX Behaves asPharmaceuticals (Basel, Switzerland) · 2022Article
- Anti-influenza A virus activity and structure-activity relationship of a series of nitrobenzoxadiazole derivatives.Journal of enzyme inhibition and medicinal chemistry · 2021Article
- Synthesis and characterisation of a new benzamide-containing nitrobenzoxadiazole as a GSTP1-1 inhibitor endowed with high stability to metabolic hydrolysis.Journal of enzyme inhibition and medicinal chemistry · 2019Article
- Glutathione Transferases: Potential Targets to Overcome Chemoresistance in Solid Tumors.International journal of molecular sciences · 2018Review
- 6-(7-nitro-2,1,3-benzoxadiazol-4-ylthio) hexanol: a promising new anticancer compound.Bioscience reports · 2018Review
- GlutathioneDrug design, development and therapy · 2018Review
Corrections and comments
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Authors and funding
11 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
contextThe nitrobezoxadiazole derivative NBDHEX is a potent inhibitor of glutathione transferase P1-1 (GSTP1-1) endowed with outstanding anticancer activity in different tumor models.
objectiveTo characterize by in vitro biochemical and in silico studies the NBDHEX analogues named MC2752 and MC2753. MATERIALS AND
methodsSynthesis of MC2752 and MC2753, biochemical assays and in silico docking and normal-mode analyses.
resultsThe presence of a hydrophobic moiety in the side chain of MC2753 confers unique features to this molecule. Unlike its parent drug NBDHEX, MC2753 does not require GSH to trigger the dissociation of the complex between GSTP1-1 and TRAF2, and displays high stability towards the nucleophilic attack of the tripeptide under physiological conditions. DISCUSSION AND
conclusionMC2753 may represent a lead compound for the development of novel GSTP1-1 inhibitors not affected in their anticancer action by fluctuations of cellular GSH levels, and characterized by an increased half-life in vivo.
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