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Review

Putative allosteric MEK1 and MEK2 inhibitors

Pages 603-627 | Published online: 26 May 2008

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John I Trujillo. (2011) MEK inhibitors: a patent review 2008 – 2010. Expert Opinion on Therapeutic Patents 21:7, pages 1045-1069.
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Matthew E. Long, Ke-Qin Gong, William E. Eddy, Joseph S. Volk, Eric D. Morrell, Carmen Mikacenic, T. Eoin West, Shawn J. Skerrett, Jean Charron, W. Conrad Liles & Anne M. Manicone. (2019) MEK1 regulates pulmonary macrophage inflammatory responses and resolution of acute lung injury. JCI Insight 4:23.
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Dandan Xi, Yan Niu, Hongyue Li, Stefan M. Noha, Veronika Temml, Daniela Schuster, Chao Wang, Fengrong Xu & Ping Xu. (2019) Discovery of carbazole derivatives as novel allosteric MEK inhibitors by pharmacophore modeling and virtual screening. European Journal of Medicinal Chemistry 178, pages 802-817.
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Hongyue Li, Dandan Xi, Yan Niu, Chao Wang, Fengrong Xu, Lei Liang & Ping Xu. (2019) Design, synthesis and biological evaluation of cobalt(II)-Schiff base complexes as ATP-noncompetitive MEK1 inhibitors. Journal of Inorganic Biochemistry 195, pages 174-181.
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Ying Cheng & Hongqi Tian. (2017) Current Development Status of MEK Inhibitors. Molecules 22:10, pages 1551.
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Hongyue Li, Tongliang Zhou, Hui Liu, Fengrong Xu, Yan Niu, Chao Wang, Lei Liang & Ping Xu. (2017) Discovery of a cobalt complex with high MEK1 binding affinity. Bioorganic & Medicinal Chemistry Letters 27:10, pages 2221-2224.
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Fangxia Zou, Yifei Yang, Tianfang Ma, Jiayue Xi, Jinpei Zhou & Xiaoming Zha. (2017) Identification of novel MEK1 inhibitors by pharmacophore and docking based virtual screening. Medicinal Chemistry Research 26:4, pages 701-713.
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Jing Sun, Yan Niu, Chao Wang, Hao Zhang, Bingyu Xie, Fengrong Xu, Hongwei Jin, Yihong Peng, Lei Liang & Ping Xu. (2016) Discovery of 3-benzyl-1,3-benzoxazine-2,4-dione analogues as allosteric mitogen-activated kinase kinase (MEK) inhibitors and anti-enterovirus 71 (EV71) agents. Bioorganic & Medicinal Chemistry 24:16, pages 3472-3482.
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Ingo V. Hartung, Florian Pühler, Roland Neuhaus, Arne Scholz, Gerhard Siemeister, Jens Geisler, Roman C. Hillig, Oliver von Ahsen & Marion Hitchcock. (2015) Modular Assembly of Allosteric MEK Inhibitor Structural Elements Unravels Potency and Feedback-Modulation Handles. ChemMedChem 10:12, pages 2004-2013.
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Kirk D. Robarge, Wendy Lee, Charles Eigenbrot, Mark Ultsch, Christian Wiesmann, Robert Heald, Steve Price, Joanne Hewitt, Philip Jackson, Pascal Savy, Brenda Burton, Edna F. Choo, Jodie Pang, Jason Boggs, April Yang, Xioaye Yang & Matthew Baumgardner. (2014) Structure based design of novel 6,5 heterobicyclic mitogen-activated protein kinase kinase (MEK) inhibitors leading to the discovery of imidazo[1,5-a] pyrazine G-479. Bioorganic & Medicinal Chemistry Letters 24:19, pages 4714-4723.
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John G CummingM Raymond V Finlay, Fabrizio Giordanetto, Martin Hemmerling, Troy Lister, Hitesh Sanganee & Michael J Waring. (2014) Potential strategies for increasing drug-discovery productivity. Future Medicinal Chemistry 6:5, pages 515-527.
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Erika Martinelli, Teresa Troiani, Elena D'Aiuto, Floriana Morgillo, Donata Vitagliano, Anna Capasso, Sarah Costantino, Loreta Pia Ciuffreda, Francesco Merolla, Loredana Vecchione, Veerle De Vriendt, Sabine Tejpar, Anna Nappi, Vincenzo Sforza, Giulia Martini, Liberato Berrino, Raffaele De Palma & Fortunato Ciardiello. (2013) Antitumor activity of pimasertib, a selective MEK 1/2 inhibitor, in combination with PI3K/mTOR inhibitors or with multi-targeted kinase inhibitors in pimasertib-resistant human lung and colorectal cancer cells. International Journal of Cancer 133:9, pages 2089-2101.
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Chao Wang, Hao Zhang, Fengrong Xu, Yan Niu, Yun Wu, Xin Wang, Yihong Peng, Jing Sun, Lei Liang & Ping Xu. (2013) Substituted 3-Benzylcoumarins as Allosteric MEK1 Inhibitors: Design, Synthesis and Biological Evaluation as Antiviral Agents. Molecules 18:5, pages 6057-6091.
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Ingo V. Hartung, Marion Hitchcock, Florian Pühler, Roland Neuhaus, Arne Scholz, Stefanie Hammer, Kirstin Petersen, Gerhard Siemeister, Dominic Brittain & Roman C. Hillig. (2013) Optimization of allosteric MEK inhibitors. Part 1: Venturing into underexplored SAR territories. Bioorganic & Medicinal Chemistry Letters 23:8, pages 2384-2390.
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Anette Weyergang, Pål K. Selbo & Kristian Berg. (2013) Sustained EKR inhibition by EGFR targeting therapies is a predictive factor for synergistic cytotoxicity with PDT as neoadjuvant therapy. Biochimica et Biophysica Acta (BBA) - General Subjects 1830:3, pages 2659-2670.
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Robert A. HealdPhilip JacksonPascal SavyMark JonesEmanuela GanciaBrenda BurtonRichard NewmanJason Boggs, Emily Chan, Jocelyn Chan, Edna Choo, Mark Merchant, Patrick Rudewicz, Mark Ultsch, Christian Wiesmann, Qin Yue, Marcia Belvin & Steve Price. (2012) Discovery of Novel Allosteric Mitogen-Activated Protein Kinase Kinase (MEK) 1,2 Inhibitors Possessing Bidentate Ser212 Interactions. Journal of Medicinal Chemistry 55:10, pages 4594-4604.
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Juyong Yoon, Kyoung-Hwa Koo & Kang-Yell Choi. (2011) MEK1/2 Inhibitors AS703026 and AZD6244 May Be Potential Therapies for KRAS Mutated Colorectal Cancer That Is Resistant to EGFR Monoclonal Antibody Therapy . Cancer Research 71:2, pages 445-453.
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Satoru Tamura, Yuuhi Hattori, Masafumi Kaneko, Nobuhiro Shimizu, Susumu Tanimura, Michiaki Kohno & Nobutoshi Murakami. (2010) Peumusolide A, unprecedented NES non-antagonistic inhibitor for nuclear export of MEK. Tetrahedron Letters 51:13, pages 1678-1681.
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Richard Morphy. (2009) Selectively Nonselective Kinase Inhibition: Striking the Right Balance. Journal of Medicinal Chemistry 53:4, pages 1413-1437.
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Klaus P. Hoeflich, Carol O'Brien, Zachary Boyd, Guy Cavet, Steve Guerrero, Kenneth Jung, Tom Januario, Heidi Savage, Elizabeth Punnoose, Tom Truong, Wei Zhou, Leanne Berry, Lesley Murray, Lukas Amler, Marcia Belvin, Lori S. Friedman & Mark R. Lackner. (2009) In vivo Antitumor Activity of MEK and Phosphatidylinositol 3-Kinase Inhibitors in Basal-Like Breast Cancer Models . Clinical Cancer Research 15:14, pages 4649-4664.
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