Structures of Lung Cancer-Derived EGFR Mutants and Inhibitor Complexes: Mechanism of Activation and Insights into Differential Inhibitor Sensitivity
Yun, Cai-Hong, Boggon, Titus J., Li, Yiqun, Woo, Michele S., Greulich, Heidi, Meyerson, Matthew, Eck, Michael J.·2007·Cancer Cell
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- Epidermal growth factor receptor (EGFR) mutations in lung cancer: preclinical and clinical dataSusan E. Jorge, Susumu S. Kobayashi, Daniel Botelho Costa · 2014 · Brazilian Journal of Medical and Biological Research
- Effect of sialylation on EGFR phosphorylation and resistance to tyrosine kinase inhibitionYen, Hsin-Yung, Liu, Ying-Chih, Chen, Nai-Yu, Tsai, Chia-Feng, Wang, Yi-Ting, Chen, Yu-Ju, Hsu, Tsui-Ling, Yang, Pan-Chyr, Wong, Chi-Huey · 2015 · Proceedings of the National Academy of Sciences
- Discovery of benzimidazole derivatives as novel multi-target EGFR, VEGFR-2 and PDGFR kinase inhibitorsYunqi Li, Chunyan Tan, Chunmei Gao, Cunlong Zhang, Xudong Luan, Xiaowu Chen, Hongxia Liu, Yu Chen, Yuyang Jiang · 2011 · Bioorganic & Medicinal Chemistry
- Induced-fit docking studies of the active and inactive states of protein tyrosine kinasesHaizhen A. Zhong, Ly M. Tran, Jenna L. Stang · 2009 · Journal of Molecular Graphics and Modelling
- Targeting Conformational Plasticity of Protein KinasesMichael Tong, Markus A. Seeliger · 2014 · ACS Chemical Biology
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- Polypharmacology modelling using proteochemometrics (PCM): recent methodological developments, applications to target families, and future prospectsIsidro Cortés‐Ciriano, Qurrat Ul Ain, Vigneshwari Subramanian, Eelke Bart Lenselink, Oscar Méndez‐Lucio, Adriaan P. IJzerman, Gerd Wohlfahrt, Peteris Prūsis, Thérèse E. Malliavin, Gerard J. P. van Westen et al. · 2014 · MedChemComm
- Evaluating Caveolin Interactions: Do Proteins Interact with the Caveolin Scaffolding Domain through a Widespread Aromatic Residue-Rich Motif?Dominic P. Byrne, Caroline Dart, Daniel John Rigden · 2012 · PLoS ONE
- A Sensitive Method for Detecting EGFR Mutations in Non-small Cell Lung Cancer Samples with Few Tumor CellsMiguel Ángel Molina‐Vila, Jordi Bertrán-Alamillo, Noemı́ Reguart, Miquel Tarón, Eva Castellà, Mariona Llatjós, Carlota Costa, Clara Mayo, Anna Pradas, Cristina Queralt et al. · 2008 · Journal of Thoracic Oncology
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- A Review of the Structure–Activity Relationship of Natural and Synthetic Antimetastatic CompoundsSu Ki Liew, Sharan Malagobadan, Norhafiza Mohd Arshad, Noor Hasima Nagoor · 2020 · Biomolecules
- Targeted Therapies for Lung CancerJill E. Larsen, Tina Cascone, David E. Gerber, John Victor Heymach, John Dorrance Minna · 2011 · The Cancer Journal
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