ArticleChemistry & biology2011
Dihydroisoxazole analogs for labeling and visualization of catalytically active transglutaminase 2.
Article in Chemistry & biology, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 26 citations in OpenAlex.
- Upcoming Treatments in Celiac Disease: From Luminal Enzymes to Oral Immune Tolerance.United European gastroenterology journal · 2026Review
- Article
- Covalent Inhibition by a Natural Product-Inspired Latent Electrophile.Journal of the American Chemical Society · 2023Article
- Application of a Fluorescence Anisotropy-Based Assay to Quantify Transglutaminase 2 Activity in Cell Lysates.International journal of molecular sciences · 2022Article
- Substrates, inhibitors, and probes of mammalian transglutaminase 2.Analytical biochemistry · 2020Review
- Article
- Tissue transglutaminase in astrocytes is enhanced by inflammatory mediators and is involved in the formation of fibronectin fibril-like structures.Journal of neuroinflammation · 2017Article
- An unprecedented dual antagonist and agonist of human Transglutaminase 2.Bioorganic & medicinal chemistry letters · 2015Article
- Discovery of potent and specific dihydroisoxazole inhibitors of human transglutaminase 2.Journal of medicinal chemistry · 2014Article
- Elevated transglutaminase 2 activity is associated with hypoxia-induced experimental pulmonary hypertension in mice.ACS chemical biology · 2014Article
- Detection of transglutaminase activity using click chemistry.Amino acids · 2012Article
- Cellular functions of tissue transglutaminase.International review of cell and molecular biology · 2012Review
- Activation and inhibition of transglutaminase 2 in mice.PloS one · 2012Article
- A unique role for heat shock protein 70 and its binding partner tissue transglutaminase in cancer cell migration.The Journal of biological chemistry · 2011Article
Corrections and comments
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Authors and funding
2 authors at 1 institution in 1 country.
Funding
Abstract
We report the synthesis and preliminary characterization of "clickable" inhibitors of human transglutaminase 2 (TG2). These inhibitors possess the 3-halo-4,5-dihydroisoxazole warhead along with bioorthogonal groups such as azide or alkyne moieties that enable subsequent covalent modification with fluorophores. Their mechanism for inhibition of TG2 is based on halide displacement, resulting in the formation of a stable imino thioether. Inhibition assays against recombinant human TG2 revealed that some of the clickable inhibitors prepared in this study have comparable specificity as benchmark dihydroisoxazole inhibitors reported earlier. At low micromolar concentrations they completely inhibited transiently activated TG2 in a WI-38 fibroblast scratch assay and could subsequently be used to visualize the active enzyme in situ. The potential use of these inhibitors to probe the role of TG2 in celiac sprue as well as other diseases is discussed.
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Registered trials
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.