ArticleActa crystallographica. Section D, Biological crystallography2011
Isothiazolidinone (IZD) as a phosphoryl mimetic in inhibitors of the Yersinia pestis protein tyrosine phosphatase YopH.
Article in Acta crystallographica. Section D, Biological crystallography, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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Who cites it
11 citing papers in PubMed.
- Allostery in Protein Tyrosine Phosphatases is Enabled by Divergent Dynamics.Journal of chemical information and modeling · 2024Article
- Citric Acid Controls the Activity of YopH Bacterial Tyrosine Phosphatase.Drug design, development and therapy · 2024Article
- Aurintricarboxylic acid structure modifications lead to reduction of inhibitory properties against virulence factor YopH and higher cytotoxicity.World journal of microbiology & biotechnology · 2016Article
- Chicoric acid binds to two sites and decreases the activity of the YopH bacterial virulence factor.Oncotarget · 2016Article
- Exploring Oxidovanadium(IV) Complexes as YopH Inhibitors: Mechanism of Action and Modeling Studies.ACS medicinal chemistry letters · 2015Article
- Redox process is crucial for inhibitory properties of aurintricarboxylic acid against activity of YopH: virulence factor of Yersinia pestis.Oncotarget · 2015Article
- Structure of human dual-specificity phosphatase 7, a potential cancer drug target.Acta crystallographica. Section F, Structural biology communications · 2015Article
- Structural analysis of human dual-specificity phosphatase 22 complexed with a phosphotyrosine-like substrate.Acta crystallographica. Section F, Structural biology communications · 2015Article
- Biomolecular Interactions of small-molecule inhibitors affecting the YopH protein tyrosine phosphatase.Chemical biology & drug design · 2013Article
- Inhibitors of the Yersinia protein tyrosine phosphatase through high throughput and virtual screening approaches.Bioorganic & medicinal chemistry letters · 2013Article
- Structure of the Trypanosoma cruzi protein tyrosine phosphatase TcPTP1, a potential therapeutic target for Chagas' disease.Molecular and biochemical parasitology · 2013Article
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Authors and funding
6 authors.
Funding
Abstract
Isothiazolidinone (IZD) heterocycles can act as effective components of protein tyrosine phosphatase (PTP) inhibitors by simultaneously replicating the binding interactions of both a phosphoryl group and a highly conserved water molecule, as exemplified by the structures of several PTP1B-inhibitor complexes. In the first unambiguous demonstration of IZD interactions with a PTP other than PTP1B, it is shown by X-ray crystallography that the IZD motif binds within the catalytic site of the Yersinia pestis PTP YopH by similarly displacing a highly conserved water molecule. It is also shown that IZD-based bidentate ligands can inhibit YopH in a nonpromiscuous fashion at low micromolar concentrations. Hence, the IZD moiety may represent a useful starting point for the development of YopH inhibitors.
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