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Transglutaminase inhibitors: a patent review

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William P Katt, Cody Aplin & Richard A Cerione. (2022) Exploring the Role of Transglutaminase in Patients with Glioblastoma: Current Perspectives. OncoTargets and Therapy 15, pages 277-290.
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Jeffrey W. Keillor & Gail V.W. Johnson. (2021) Transglutaminase 2 as a therapeutic target for neurological conditions. Expert Opinion on Therapeutic Targets 25:9, pages 721-731.
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Yi Zhang & Benjamin K. Simpson. (2020) Food-related transglutaminase obtained from fish/shellfish. Critical Reviews in Food Science and Nutrition 60:19, pages 3214-3232.
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Articles from other publishers (27)

Cong Liu, Xing Gao, Ruo‐Xi Shi, Ying‐Ying Wang, Xuan‐Cheng He, Hong‐Zhen Du, Baoyang Hu, Jianwei Jiao, Chang‐Mei Liu & Zhao‐Qian Teng. (2023) Microglial transglutaminase 2 deficiency causes impaired synaptic remodelling and cognitive deficits in mice. Cell Proliferation 56:9.
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Pratibha Sharma & Manjinder Singh. (2023) An ongoing journey of chalcone analogues as single and multi-target ligands in the field of Alzheimer's disease: A review with structural aspects. Life Sciences 320, pages 121568.
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Doa’a G. F. Al-U’datt, Carole C. Tranchant, Belal Al-Husein, Roddy Hiram, Ahmed Al-Dwairi, Mohammad AlQudah, Othman Al-shboul, Saied Jaradat, Jenan Alqbelat & Ali Almajwal. (2023) Involvement and possible role of transglutaminases 1 and 2 in mediating fibrotic signalling, collagen cross-linking and cell proliferation in neonatal rat ventricular fibroblasts. PLOS ONE 18:2, pages e0281320.
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Claudia Damaris Müller, Gloria Ruiz-Gómez, Sophie Cazzonelli, Stephanie Möller, Robert Wodtke, Reik Löser, Joanna Freyse, Jan-Niklas Dürig, Jörg Rademann, Ute Hempel, M. Teresa Pisabarro & Sarah Vogel. (2022) Sulfated glycosaminoglycans inhibit transglutaminase 2 by stabilizing its closed conformation. Scientific Reports 12:1.
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Alana M. M. Rangaswamy, Pauline Navals, Eric W. J. Gates, Sammir Shad, Sarah K. I. Watt & Jeffrey W. Keillor. (2022) Structure–activity relationships of hydrophobic alkyl acrylamides as tissue transglutaminase inhibitors. RSC Medicinal Chemistry 13:4, pages 413-428.
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Nicole M.R. McNeil, Eric W.J. Gates, Neda Firoozi, Nicholas J. Cundy, Jessica Leccese, Sarah Eisinga, Joel D.A. Tyndall, Gautam Adhikary, Richard L. Eckert & Jeffrey W. Keillor. (2022) Structure-activity relationships of N-terminal variants of peptidomimetic tissue transglutaminase inhibitors. European Journal of Medicinal Chemistry 232, pages 114172.
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Jie Zhang, HilaryGrosso Jasutkar & MMaral Mouradian. (2021) Targeting transglutaminase 2 as a potential disease modifying therapeutic strategy for synucleinopathies. Neural Regeneration Research 16:8, pages 1560.
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Regina Staffler, Ralf Pasternack, Martin Hils, Wolfgang Kaiser & Friederike M. Möller. (2020) Nucleotide binding kinetics and conformational change analysis of tissue transglutaminase with switchSENSE. Analytical Biochemistry 605, pages 113719.
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Kinga Lénárt, Attila Pap, Róbert Pórszász, Anna V. Oláh, László Fésüs & András Mádi. (2020) Transglutaminase 2 Has Metabolic and Vascular Regulatory Functions Revealed by In Vivo Activation of Alpha1-Adrenergic Receptor. International Journal of Molecular Sciences 21:11, pages 3865.
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Ruize Zhuang & Chaitan Khosla. (2020) Substrates, inhibitors, and probes of mammalian transglutaminase 2. Analytical Biochemistry 591, pages 113560.
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Ralf Pasternack, Christian Büchold, Robert Jähnig, Christiane Pelzer, Michael Sommer, Andreas Heil, Peter Florian, Götz Nowak, Uwe Gerlach & Martin Hils. (2020) Novel inhibitor ZED3197 as potential drug candidate in anticoagulation targeting coagulation FXIIIa (F13a). Journal of Thrombosis and Haemostasis 18:1, pages 191-200.
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Ludvig M. Sollid & Knut E.A. Lundin. 2020. The Autoimmune Diseases. The Autoimmune Diseases 849 869 .
Laszlo Lorand & Siiri E. Iismaa. (2018) Transglutaminase diseases: from biochemistry to the bedside. The FASEB Journal 33:1, pages 3-12.
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William P. Katt, Nicolas J. Blobel, Svetlana Komarova, Marc A. Antonyak, Ichiro Nakano & Richard A. Cerione. (2018) A small molecule regulator of tissue transglutaminase conformation inhibits the malignant phenotype of cancer cells. Oncotarget 9:76, pages 34379-34397.
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Brad A. Palanski & Chaitan Khosla. (2018) Cystamine and Disulfiram Inhibit Human Transglutaminase 2 via an Oxidative Mechanism. Biochemistry 57:24, pages 3359-3363.
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Robert Wodtke, Christoph Hauser, Gloria Ruiz-Gómez, Elisabeth Jäckel, David Bauer, Martin Lohse, Alan Wong, Johanna Pufe, Friedrich-Alexander Ludwig, Steffen Fischer, Sandra Hauser, Dieter Greif, M. Teresa Pisabarro, Jens Pietzsch, Markus Pietsch & Reik Löser. (2018) N ε -Acryloyllysine Piperazides as Irreversible Inhibitors of Transglutaminase 2: Synthesis, Structure–Activity Relationships, and Pharmacokinetic Profiling . Journal of Medicinal Chemistry 61:10, pages 4528-4560.
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Elizabeth Reyna-Beltrán, María Iranzo, Karla Grisel Calderón-González, Ricardo Mondragón-Flores, María Luisa Labra-Barrios, Salvador Mormeneo & Juan Pedro Luna-Arias. (2018) The Candida albicans ENO1 gene encodes a transglutaminase involved in growth, cell division, morphogenesis, and osmotic protection. Journal of Biological Chemistry 293:12, pages 4304-4323.
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Marsha C. Lampi & Cynthia A. Reinhart-King. (2018) Targeting extracellular matrix stiffness to attenuate disease: From molecular mechanisms to clinical trials. Science Translational Medicine 10:422.
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Lei Zhang, Wenbing Rao, Solange Muhayimana, Xianfei Zhang, Jiuyong Xu, Ciying Xiao & Qingchun Huang. (2018) Purification and biochemical characterization of a novel transglutaminase from Mythimna separata larvae (Noctuidae, Lepidoptera). Journal of Biotechnology 265, pages 1-7.
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Will W. Minuth. (2017) Concepts for a therapeutic prolongation of nephrogenesis in preterm and low-birth-weight babies must correspond to structural-functional properties in the nephrogenic zone. Molecular and Cellular Pediatrics 4:1.
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Abdullah Akbar, Nicole M. R. McNeil, Marie R. Albert, Viviane Ta, Gautam Adhikary, Karine Bourgeois, Richard L. Eckert & Jeffrey W. Keillor. (2017) Structure–Activity Relationships of Potent, Targeted Covalent Inhibitors That Abolish Both the Transamidation and GTP Binding Activities of Human Tissue Transglutaminase. Journal of Medicinal Chemistry 60:18, pages 7910-7927.
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Zsuzsa Szondy, Ilma Korponay-Szabó, Robert Király, Zsolt Sarang & Gregory J. Tsay. (2017) Transglutaminase 2 in human diseases. BioMedicine 7:3, pages 15.
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E. Teran-Hinojosa, H. Sobral, C. Sánchez-Pérez, A. Pérez-García, N. Alemán-García & J. Hernández-Ruiz. (2017) Differentiation of fibrotic liver tissue using laser-induced breakdown spectroscopy. Biomedical Optics Express 8:8, pages 3816.
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Chaitan Khosla. (2017) Celiac Disease: Lessons for and from Chemical Biology. ACS Chemical Biology 12:6, pages 1455-1459.
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Minsoo Song, Hayoung Hwang, Chun Young Im & Soo-Youl Kim. (2016) Recent Progress in the Development of Transglutaminase 2 (TGase2) Inhibitors. Journal of Medicinal Chemistry 60:2, pages 554-567.
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Aaron Lerner, Rustam Aminov & Torsten Matthias. (2017) Transglutaminases in Dysbiosis As Potential Environmental Drivers of Autoimmunity. Frontiers in Microbiology 8.
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Nicola Gaetano Gatta, Rosaria Romano, Elenamaria Fioretti & Vittorio Gentile. (2017) Transglutaminase inhibition: possible therapeutic mechanisms to protect cells from death in neurological disorders. AIMS Molecular Science 4:4, pages 399-414.
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