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TBK1 inhibitors: a review of patent literature (2011 – 2014)

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Yin Sun, Haotian Tang, Xiaoyan Wang, Fang Feng, Tiantian Fan, Dongmei Zhao, Bing Xiong, Hua Xie & Tongchao Liu. (2022) Identification of 1H-pyrazolo[3,4-b]pyridine derivatives as novel and potent TBK1 inhibitors: design, synthesis, biological evaluation, and molecular docking study. Journal of Enzyme Inhibition and Medicinal Chemistry 37:1, pages 1411-1425.
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Douglas W. Thomson & Giovanna Bergamini. (2021) Recent progress in small molecule TBK1 inhibitors: a patent review (2015– 2020). Expert Opinion on Therapeutic Patents 31:9, pages 785-794.
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Iris L. A. Bodewes & Marjan A. Versnel. (2018) Interferon activation in primary Sjögren’s syndrome: recent insights and future perspective as novel treatment target. Expert Review of Clinical Immunology 14:10, pages 817-829.
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Articles from other publishers (36)

Xinchen Lu, Jinmei Jin, Ye Wu, Xiaoxia Liu, Xiaohui Liang, Jiayi Lin, Qingyan Sun, Jiangjiang Qin, Weidong Zhang & Xin Luan. (2023) Progress in RAS‐targeted therapeutic strategies: From small molecule inhibitors to proteolysis targeting chimeras. Medicinal Research Reviews.
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Lingzi Wu, Lei Zhou, Jinying An, Xianfeng Shao, Hui Zhang, Chunxi Wang, Guixia Zhao, Shuang Chen, Xuexue Cui, Xinyi Zhang, Fuhua Yang, Xiaorong Li & Xiaomin Zhang. (2023) Comprehensive profiling of extracellular vesicles in uveitis and scleritis enables biomarker discovery and mechanism exploration. Journal of Translational Medicine 21:1.
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Yanming Tian, Bin Tian, Mingshu Wang, Dongjie Cai, Anchun Cheng, Wei Zhang, Ying Wu, Qiao Yang, Xuming Ou, Di Sun, Shaqiu Zhang, Sai Mao, XinXin Zhao, Juan Huang, Qun Gao, Dekang Zhu, Renyong Jia, Shun Chen & Mafeng Liu. (2023) BX795, a kinase inhibitor, inhibit duck plague virus infection via targeting US3 kinase. Poultry Science 102:5, pages 102597.
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Xiangjie Gao, Guanxiong Lei, Bin Wang, Zhong Deng, Johannes Karges, Haihua Xiao & Donghui Tan. (2022) Encapsulation of Platinum Prodrugs into PC7A Polymeric Nanoparticles Combined with Immune Checkpoint Inhibitors for Therapeutically Enhanced Multimodal Chemotherapy and Immunotherapy by Activation of the STING Pathway. Advanced Science 10:4, pages 2205241.
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HanCheng Liu, HuiMing Li, Jie Zhang, QingLai Meng & LiHui Ma. (2022) Correlation of TBK1, AR, and other serum cancer-related biomarkers in breast cancer patients: An observational study. Medicine 101:33, pages e29996.
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Noémie Pied, Coralie F. Daussy, Zoé Denis, Jessica Ragues, Muriel Faure, Richard Iggo, Mario P. Tschan, Benoit Roger, Fabienne Rayne & Harald Wodrich. (2022) TBK1 is part of a galectin 8 dependent membrane damage recognition complex and drives autophagy upon Adenovirus endosomal escape. PLOS Pathogens 18:7, pages e1010736.
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Jiahui Ding, Anthony Maxwell, Nicholas Adzibolosu, Anna Hu, Yuan You, Aihua Liao & Gil Mor. (2022) Mechanisms of immune regulation by the placenta: Role of type I interferon and interferon‐stimulated genes signaling during pregnancy*. Immunological Reviews 308:1, pages 9-24.
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Manzar Alam, Md. Meraj Ansari, Saba Noor, Taj Mohammad, Gulam Mustafa Hasan, Syed Naqui Kazim & Md. Imtaiyaz Hassan. (2022) Therapeutic targeting of TANK-binding kinase signaling towards anticancer drug development: Challenges and opportunities. International Journal of Biological Macromolecules 207, pages 1022-1037.
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Tian-Sheng He, Jingping Huang, Tian Chen, Zhi Zhang, Kuntai Cai, Jingge Yu & Liang-Guo Xu. (2021) The Kinase MAP4K1 Inhibits Cytosolic RNA-Induced Antiviral Signaling by Promoting Proteasomal Degradation of TBK1/IKKε. Microbiology Spectrum 9:3.
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Yves Pacheco, Dominique Valeyre, Thomas El Jammal, Maxime Vallee, Fabien Chevalier, Jérôme Lamartine, Dominique Sigaudo-Roussel, Bernard Verrier, Dominique Israel-Biet, Nathalie Freymond, Vincent Cottin & Alain Calender. (2021) Autophagy and Mitophagy-Related Pathways at the Crossroads of Genetic Pathways Involved in Familial Sarcoidosis and Host-Pathogen Interactions Induced by Coronaviruses. Cells 10:8, pages 1995.
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Manzar Alam, Gulam Mustafa Hasan & Md. Imtaiyaz Hassan. (2021) A review on the role of TANK-binding kinase 1 signaling in cancer. International Journal of Biological Macromolecules 183, pages 2364-2375.
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Lina Herhaus. (2021) TBK1 (TANK-binding kinase 1)-mediated regulation of autophagy in health and disease. Matrix Biology 100-101, pages 84-98.
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Jiamin Zheng, Jun Wu, Xiao Ding, Hong C. Shen & Ge Zou. (2021) Small molecule approaches to treat autoimmune and inflammatory diseases (Part I): Kinase inhibitors. Bioorganic & Medicinal Chemistry Letters 38, pages 127862.
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Zere Mukhamejanova, Yichen Tong, Qi Xiang, Fang Xu & Jiyan Pang. (2021) Recent Advances in the Design and Development of Anticancer Molecules based on PROTAC Technology. Current Medicinal Chemistry 28:7, pages 1304-1327.
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Chunyong Ding, Zilan Song, Ancheng Shen, Tingting Chen & Ao Zhang. (2020) Small molecules targeting the innate immune cGAS‒STING‒TBK1 signaling pathway. Acta Pharmaceutica Sinica B 10:12, pages 2272-2298.
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Eleftherios Kostaras, Teresa Kaserer, Glorianne Lazaro, Sara Farrah Heuss, Aasia Hussain, Pedro Casado, Angela Hayes, Cihangir Yandim, Nicolaos Palaskas, Yi Yu, Brian Schwartz, Florence Raynaud, Yuen-Li Chung, Pedro R. Cutillas & Igor Vivanco. (2020) A systematic molecular and pharmacologic evaluation of AKT inhibitors reveals new insight into their biological activity. British Journal of Cancer 123:4, pages 542-555.
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Hao Zhang, Suleman Abid, Jong Chan Ahn, Ramya Mathiyalagan, Yu-Jin Kim, Deok-Chun Yang & Yingping Wang. (2020) Characteristics of Panax ginseng Cultivars in Korea and China. Molecules 25:11, pages 2635.
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Aja Aravamudhan, Andrew J. Haak, Kyoung Moo Choi, Jeffrey A. Meridew, Nunzia Caporarello, Dakota L. Jones, Qi Tan, Giovanni Ligresti & Daniel J. Tschumperlin. (2020) TBK1 regulates YAP/TAZ and fibrogenic fibroblast activation. American Journal of Physiology-Lung Cellular and Molecular Physiology 318:5, pages L852-L863.
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Tao Yu, Zhibin Wang, Wang Jie, Xiuxiu Fu, Bing Li, Hong Xu, Yan Liu, Min Li, Eunji Kim, Yanyan Yang & Jae Youl Cho. (2020) The kinase inhibitor BX795 suppresses the inflammatory response via multiple kinases. Biochemical Pharmacology 174, pages 113797.
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Yang Wang, Xueyang Jiang, Feng Feng, Wenyuan Liu & Haopeng Sun. (2020) Degradation of proteins by PROTACs and other strategies. Acta Pharmaceutica Sinica B 10:2, pages 207-238.
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Julien Lefranc, Volker Klaus Schulze, Roman Christian Hillig, Hans Briem, Florian Prinz, Anne Mengel, Tobias Heinrich, Jozsef Balint, Srinivasan RengachariHorst Irlbacher, Detlef Stöckigt, Ulf Bömer, Benjamin Bader, Stefan Nikolaus Gradl, Carl Friedrich Nising, Franz von Nussbaum, Dominik Mumberg, Daniel Panne & Antje Margret Wengner. (2019) Discovery of BAY-985, a Highly Selective TBK1/IKKε Inhibitor. Journal of Medicinal Chemistry 63:2, pages 601-612.
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Seung Jun Lee, Amal Gharbi, Jueng Soo You, Hee Dong Han, Tae Heung Kang, Seong Hwi Hong, Won Sun Park, In Duk Jung & Yeong-Min Park. (2019) Drug repositioning of TANK-binding kinase 1 inhibitor CYT387 as an alternative for the treatment of Gram-negative bacterial sepsis. International Immunopharmacology 73, pages 482-490.
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Douglas W. Thomson, Daniel Poeckel, Nico Zinn, Christina Rau, Katrin Strohmer, Anne J. Wagner, Alan P. Graves, Jessica Perrin, Marcus Bantscheff, Birgit Duempelfeld, Viera Kasparcova, Joshi M. Ramanjulu, G. Scott Pesiridis, Marcel Muelbaier & Giovanna Bergamini. (2019) Discovery of GSK8612, a Highly Selective and Potent TBK1 Inhibitor. ACS Medicinal Chemistry Letters 10:5, pages 780-785.
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Jianguo Qi & Gang Zhang. (2019) Proteolysis-targeting chimeras for targeting protein for degradation. Future Medicinal Chemistry 11:7, pages 723-741.
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Ja-Young Kwon, Paulomi Aldo, Yuan You, Jiahui Ding, Karen Racicot, Xiaoyan Dong, John Murphy, Guy Glukshtad, Michelle Silasi, Jian Peng, Li Wen, Vikki M. Abrahams, Roberto Romero & Gil Mor. (2018) Relevance of placental type I interferon beta regulation for pregnancy success. Cellular & Molecular Immunology 15:12, pages 1010-1026.
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Hailing Yang, Weiqun Mao, Cristian Rodriguez-Aguayo, Lingegowda S. Mangala, Geoffrey Bartholomeusz, Lakesla R. Iles, Nicholas B. Jennings, Ahmed Ashour Ahmed, Anil K. Sood, Gabriel Lopez-Berestein, Zhen Lu & Robert C. BastJr.Jr.. (2018) Paclitaxel Sensitivity of Ovarian Cancer Can be Enhanced by Knocking Down Pairs of Kinases that Regulate MAP4 Phosphorylation and Microtubule Stability. Clinical Cancer Research 24:20, pages 5072-5084.
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Iris L.A. Bodewes, Erika Huijser, Cornelia G. van Helden-Meeuwsen, Liselotte Tas, Ruth Huizinga, Virgil A.S.H. Dalm, P. Martin van Hagen, Noortje Groot, Sylvia Kamphuis, Paul L.A. van Daele & Marjan A. Versnel. (2018) TBK1: A key regulator and potential treatment target for interferon positive Sjögren's syndrome, systemic lupus erythematosus and systemic sclerosis. Journal of Autoimmunity 91, pages 97-102.
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Andrew P. Crew, Kanak Raina, Hanqing Dong, Yimin Qian, Jing Wang, Dominico Vigil, Yevgeniy V. Serebrenik, Brian D. Hamman, Alicia Morgan, Caterina Ferraro, Kam Siu, Taavi K. Neklesa, James D. Winkler, Kevin G. Coleman & Craig M. Crews. (2017) Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1. Journal of Medicinal Chemistry 61:2, pages 583-598.
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Claudio Bussi, Javier M. Peralta Ramos, Daniela S. Arroyo, Jose I. Gallea, Paolo Ronchi, Androniki Kolovou, Ji M. Wang, Oliver Florey, Maria S. Celej, Yannick Schwab, Nicholas T. Ktistakis & Pablo Iribarren. (2018) Alpha-synuclein fibrils recruit TBK1 and OPTN to lysosomal damage sites and induce autophagy in microglial cells. Journal of Cell Science.
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Federica Begalli, Jason Bennett, Daria Capece, Daniela Verzella, Daniel D’Andrea, Laura Tornatore & Guido Franzoso. (2017) Unlocking the NF-κB Conundrum: Embracing Complexity to Achieve Specificity. Biomedicines 5:3, pages 50.
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Tao Yu, Yanyan Yang, Yi-Seong Kwak, Gwan Gyu Song, Mi-Yeon Kim, Man Hee Rhee & Jae Youl Cho. (2017) Ginsenoside Rc from Panax ginseng exerts anti-inflammatory activity by targeting TANK-binding kinase 1/interferon regulatory factor-3 and p38/ATF-2. Journal of Ginseng Research 41:2, pages 127-133.
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Jae Sik Yu, Jun Ho Kim, Seulah Lee, Kiwon Jung, Ki Hyun Kim & Jae Youl Cho. (2017) Src/Syk-Targeted Anti-Inflammatory Actions of Triterpenoidal Saponins from Gac ( Momordica cochinchinensis ) Seeds . The American Journal of Chinese Medicine 45:03, pages 459-473.
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J.K. Durand & A.S. Baldwin. 2017. Chromatin Proteins and Transcription Factors as Therapeutic Targets. Chromatin Proteins and Transcription Factors as Therapeutic Targets 77 115 .
Eline Wauters, Kristel Sleegers, Marc Cruts & Christine Van Broeckhoven. 2017. Disease-Modifying Targets in Neurodegenerative Disorders. Disease-Modifying Targets in Neurodegenerative Disorders 199 249 .
Zoe O. Gage, Andri Vasou, David W. Gray, Richard E. Randall & Catherine S. Adamson. (2016) Identification of Novel Inhibitors of the Type I Interferon Induction Pathway Using Cell-Based High-Throughput Screening. SLAS Discovery 21:9, pages 978-988.
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Maroof Hasan & Nan Yan. (2016) Therapeutic potential of targeting TBK1 in autoimmune diseases and interferonopathies. Pharmacological Research 111, pages 336-342.
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