ArticleChemistry & biology2008
Identification of chemical inhibitors to human tissue transglutaminase by screening existing drug libraries.
Article in Chemistry & biology, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 27 papers.
What it found
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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.
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Who cites it
27 citing papers in PubMed, 67 citations in OpenAlex.
- Inhibition of TGM2 enhances cisplatin sensitivity in MSH2-deficient bladder cancer.Cell death discovery · 2026Article
- Deletion of Tgm2 suppresses BMP-mediated hepatocyte-to-cholangiocyte metaplasia in ductular reaction.Cell proliferation · 2024Article
- Transglutaminase 2-mediated histone monoaminylation and its role in cancer.Bioscience reports · 2024Review
- A guide to selecting high-performing antibodies for Protein-glutamine gamma-glutamyltransferase 2 (TGM2) for use in western blot, immunoprecipitation and immunofluorescence.F1000Research · 2024Article
- Transglutaminase 2 in diabetes mellitus: Unraveling its multifaceted role and therapeutic implications for vascular complications.Theranostics · 2024Review
- Transglutaminase 2 is associated with adverse colorectal cancer survival and represents a therapeutic target.Cancer gene therapy · 2023Article
- Epigenetic meets metabolism: novel vulnerabilities to fight cancer.Cell communication and signaling : CCS · 2023Review
- Effects of α-Synuclein Monomers Administration in the Gigantocellular Reticular Nucleus on Neurotransmission in Mouse Model.Neurochemical research · 2019Article
- The diamond anniversary of tissue transglutaminase: a protein of many talents.Drug discovery today · 2018Review
- Screening a small molecule library to identify inhibitors of NF-κB inducing kinase and pro-labor genes in human placenta.Scientific reports · 2018Article
- Transglutaminase 2 in human diseases.BioMedicine · 2017Article
- Strategies towards in vivo imaging of active transglutaminase type 2 using positron emission tomography.Amino acids · 2017Review
- Small molecules reveal an alternative mechanism of Bax activation.The Biochemical journal · 2016Article
- NNC 55-0396, a T-type Ca2+ channel inhibitor, inhibits angiogenesis via suppression of hypoxia-inducible factor-1α signal transduction.Journal of molecular medicine (Berlin, Germany) · 2015Article
- Transglutaminase 2 inhibitor abrogates renal cell carcinoma in xenograft models.Journal of cancer research and clinical oncology · 2014Article
- Transglutaminse 2 and EGGL, the protein cross-link formed by transglutaminse 2, as therapeutic targets for disabilities of old age.Rejuvenation research · 2013Review
- TGM2 inhibition attenuates ID1 expression in CD44-high glioma-initiating cells.Neuro-oncology · 2013Article
- Ethacrynic Acid Inhibits Sphingosylphosphorylcholine-Induced Keratin 8 Phosphorylation and Reorganization via Transglutaminase-2 Inhibition.Biomolecules & therapeutics · 2013Article
- Anti-cancer effect of a quinoxaline derivative GK13 as a transglutaminase 2 inhibitor.Journal of cancer research and clinical oncology · 2013Article
- Role of transglutaminase 2 in celiac disease pathogenesis.Seminars in immunopathology · 2012Review
Corrections and comments
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Authors and funding
9 authors at 3 institutions in 1 country.
Funding
Abstract
Human tissue transglutaminase (TGM2) is a calcium-dependent crosslinking enzyme involved in the posttranslational modification of intra- and extracellular proteins and implicated in several neurodegenerative diseases. To find specific inhibitors to TGM2, two structurally diverse chemical libraries (LOPAC and Prestwick) were screened. We found that ZM39923, a Janus kinase inhibitor, and its metabolite ZM449829 were the most potent inhibitors with IC(50) of 10 and 5 nM, respectively. In addition, two other inhibitors, including tyrphostin 47 and vitamin K(3), were found to have an IC(50) in the micromolar range. These agents used in part a thiol-dependent mechanism to inhibit TGM2, consistent with the activation of TGM2 by reduction of an intramolecular disulfide bond. These inhibitors were tested in a polyglutamine-expressing Drosophila model of neurodegeneration and found to improve survival. The TGM2 inhibitors we discovered may serve as valuable lead compounds for the development of orally active TGM2 inhibitors to treat human diseases.
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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.