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Calpain inhibitors: a survey of compounds reported in the patent and scientific literature

Pages 601-636 | Published online: 24 Mar 2011

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Isaac O. Donkor. (2020) An update on the therapeutic potential of calpain inhibitors: a patent review. Expert Opinion on Therapeutic Patents 30:9, pages 659-675.
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Levente Endre Dókus, Mo’ath Yousef & Zoltán Bánóczi. (2020) Modulators of calpain activity: inhibitors and activators as potential drugs. Expert Opinion on Drug Discovery 15:4, pages 471-486.
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Désirée White-Schenk, Riyi Shi & James F Leary. (2015) Nanomedicine strategies for treatment of secondary spinal cord injury. International Journal of Nanomedicine 10, pages 923-938.
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Isaac O Donkor. (2015) An updated patent review of calpain inhibitors (2012 – 2014). Expert Opinion on Therapeutic Patents 25:1, pages 17-31.
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Michel Baudry, Maggie M Chou & Xiaoning Bi. (2013) Targeting calpain in synaptic plasticity. Expert Opinion on Therapeutic Targets 17:5, pages 579-592.
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Articles from other publishers (62)

Michel Baudry, Yun Lyna Luo & Xiaoning Bi. (2023) Calpain-2 Inhibitors as Therapy for Traumatic Brain Injury. Neurotherapeutics 20:6, pages 1592-1602.
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Ruiyang Zhao, Xiufei Teng & Yanchao Yang. (2023) Calpain as a Therapeutic Target for Hypoxic-Ischemic Encephalopathy. Molecular Neurobiology.
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Jennifer T. Vu, Elena Wang, Jolan Wu, Young Joo Sun, Gabriel Velez, Alexander G. Bassuk, Soo Hyeon Lee & Vinit B. Mahajan. (2022) Calpains as mechanistic drivers and therapeutic targets for ocular disease. Trends in Molecular Medicine 28:8, pages 644-661.
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Heena Khan, Nikhil Garg, Thakur Gurjeet Singh, Amarjot Kaur & Komal Thapa. (2022) Calpain Inhibitors as Potential Therapeutic Modulators in Neurodegenerative Diseases. Neurochemical Research 47:5, pages 1125-1149.
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Yanyan Cao, Kai Liu, Ying Xiong, Chunyue Zhao & Lei Liu. (2021) Increased expression of fragmented tRNA promoted neuronal necrosis. Cell Death & Disease 12:9.
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Ammar Jastaniah, Irina N. Gaisina, Rachel C. Knopp & Gregory R. J. Thatcher. (2020) Synthesis of α‐Ketoamide‐Based Stereoselective Calpain‐1 Inhibitors as Neuroprotective Agents. ChemMedChem 15:23, pages 2280-2285.
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Ravinder Kaur & Neera Raghav. (2020) Some thiocarbamoyl based novel anticathepsin agents. Bioorganic Chemistry 104, pages 104174.
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Xianliang Zeng, Ping Chen, Li Zhao & Sizeng Chen. (2020) Acylated and unacylated ghrelin relieve cancer cachexia in mice through multiple mechanisms. Chinese Journal of Physiology 63:5, pages 195.
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Ana M. Matos, Francisco R. Pinto, Patrícia Barros, Margarida D. Amaral, Rainer Pepperkok & Paulo Matos. (2019) Inhibition of calpain 1 restores plasma membrane stability to pharmacologically rescued Phe508del-CFTR variant. Journal of Biological Chemistry 294:36, pages 13396-13410.
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The Minh Vo, Saket Jain, Rebecca Burchett, Elizabeth A. Monckton & Roseline Godbout. (2019) A positive feedback loop involving nuclear factor IB and calpain 1 suppresses glioblastoma cell migration. Journal of Biological Chemistry 294:34, pages 12638-12654.
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Bianca Sparatore, Marco Pedrazzi, Anna Garuti, Alice Franchi, Monica Averna, Alberto Ballestrero & Roberta De Tullio. (2019) A new human calpastatin skipped of the inhibitory region protects calpain-1 from inactivation and degradation. Biochimica et Biophysica Acta (BBA) - Molecular Cell Research 1866:8, pages 1260-1271.
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Rhiannon Roberts & Maurice Hallett. (2019) Neutrophil Cell Shape Change: Mechanism and Signalling during Cell Spreading and Phagocytosis. International Journal of Molecular Sciences 20:6, pages 1383.
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Christian-Scott E. McCartney & Peter L. Davies. 2019. Calpain. Calpain 39 55 .
Sara Gutiérrez, María Morón, Mercedes Griera, David Sucunza, Laura Calleros, Andrea García-Jérez, Claire Coderch, Francisco J. Hermoso, Carolina Burgos, Manuel Rodríguez-Puyol, Beatriz de Pascual-Teresa, María L. Diez-Marques, Antonio Jimenez, Miguel Toro-Londoño, Diego Rodríguez-Puyol & Juan J. Vaquero. (2018) Discovery of potent calpain inhibitors based on the azolo-imidazolidenone scaffold. European Journal of Medicinal Chemistry 157, pages 946-959.
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Andreas Kling, Katja Jantos, Helmut Mack, Wilfried Hornberger, Gisela Backfisch, Yanbin Lao, Marjoleen Nijsen, Beatrice Rendenbach-Mueller & Achim Moeller. (2018) Mitigating the Metabolic Liability of Carbonyl Reduction: Novel Calpain Inhibitors with P1′ Extension. ACS Medicinal Chemistry Letters 9:3, pages 221-226.
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Yubin WangYan LiuDulce LopezMoses LeeSujay DayalAlexander HurtadoXiaoning BiMichel Baudry. (2018) Protection against TBI-Induced Neuronal Death with Post-Treatment with a Selective Calpain-2 Inhibitor in Mice. Journal of Neurotrauma 35:1, pages 105-117.
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Yubin Wang, Xiaoning Bi & Michel Baudry. 2018. Acute Neuronal Injury. Acute Neuronal Injury 19 35 .
Xianliang Zeng, Sizeng Chen, Yang Yang & Zhao Ke. (2017) Acylated and unacylated ghrelin inhibit atrophy in myotubes co-cultured with colon carcinoma cells. Oncotarget 8:42, pages 72872-72885.
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Andreas Kling, Katja Jantos, Helmut Mack, Wilfried Hornberger, Karla Drescher, Volker Nimmrich, Ana Relo, Karsten Wicke, Charles W. Hutchins, Yanbin Lao, Kennan Marsh & Achim Moeller. (2017) Discovery of Novel and Highly Selective Inhibitors of Calpain for the Treatment of Alzheimer’s Disease: 2-(3-Phenyl-1 H -pyrazol-1-yl)-nicotinamides . Journal of Medicinal Chemistry 60:16, pages 7123-7138.
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Jonasz J. Weber, Matthias Golla, Giambattista Guaitoli, Pimthanya Wanichawan, Stefanie N. Hayer, Stefan Hauser, Ann-Christin Krahl, Maike Nagel, Sebastian Samer, Eleonora Aronica, Cathrine R. Carlson, Ludger Schöls, Olaf Riess, Christian J. Gloeckner, Huu P. Nguyen & Jeannette Hübener-Schmid. (2017) A combinatorial approach to identify calpain cleavage sites in the Machado-Joseph disease protein ataxin-3. Brain 140:5, pages 1280-1299.
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Xing-Yu Lin & Si-Zeng Chen. (2017) Calpain inhibitors ameliorate muscle wasting in a cachectic mouse model bearing CT26 colorectal adenocarcinoma. Oncology Reports 37:3, pages 1601-1610.
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Katarzyna Starska, Ewa Forma, Paweł Jóźwiak, Iwona Lewy-Trenda, Marian Danilewicz, Olga Stasikowska-Kanicka, Michał Skóra, Katarzyna Kolary, Jakub Miazga, Anna Krześlak & Magdalena Bryś. (2016) Gene/protein expression of CAPN1/2-CAST system members is associated with ERK1/2 kinases activity as well as progression and clinical outcome in human laryngeal cancer. Tumor Biology 37:10, pages 13185-13203.
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Kyung Hye Baek, Han Vit Yu, Eosu Kim, Younghwa Na & Youngjoo Kwon. (2016) Calcium influx-mediated translocation of m -calpain induces Ku80 cleavage and enhances the Ku80-related DNA repair pathway . Oncotarget 7:21, pages 30831-30844.
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Marton Siklos, Manel BenAissa & Gregory R.J. Thatcher. (2015) Cysteine proteases as therapeutic targets: does selectivity matter? A systematic review of calpain and cathepsin inhibitors. Acta Pharmaceutica Sinica B 5:6, pages 506-519.
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Liang Lu, Michael J. Meehan, Shuo Gu, Zhilong Chen, Weipeng Zhang, Gen Zhang, Lingli Liu, Xuhui Huang, Pieter C. Dorrestein, Ying Xu, Bradley S. Moore & Pei-Yuan Qian. (2015) Mechanism of Action of Thalassospiramides, A New Class of Calpain Inhibitors. Scientific Reports 5:1.
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S. E. Adams, E. J. Robinson, D. J. Miller, P. J. Rizkallah, M. B. Hallett & R. K. Allemann. (2015) Conformationally restricted calpain inhibitors. Chemical Science 6:12, pages 6865-6871.
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Andrew F. Teich, Russell E. Nicholls, Daniela Puzzo, Jole Fiorito, Rosa Purgatorio, Mauro Fa’ & Ottavio Arancio. (2015) Synaptic Therapy in Alzheimer’s Disease: A CREB-centric Approach. Neurotherapeutics 12:1, pages 29-41.
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Zhengli Wu, Xiaochun Chen, Fang Liu, Wei Chen, Ping Wu, Adam J. Wieschhaus, Athar H. Chishti, Paul A. Roche, Wei-Min Chen & Tong-Jun Lin. (2014) Calpain-1 Contributes to IgE-Mediated Mast Cell Activation. The Journal of Immunology 192:11, pages 5130-5139.
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