Dissecting RAF Inhibitor Resistance by Structure-based Modeling Reveals Ways to Overcome Oncogenic RAS Signaling.
作者： Oleksii S. Rukhlenko , Fahimeh Khorsand , Aleksandar Krstic , Jan Rozanc , Leonidas G. Alexopoulos
DOI: 10.1016/J.CELS.2018.06.002
关键词: Cell culture 、 Cell biology 、 Neuroblastoma RAS viral oncogene homolog 、 HRAS 、 Mutant 、 Cell growth 、 MAPK/ERK pathway 、 Chemistry 、 Cell 、 Inhibitor resistance
摘要: Clinically used RAF inhibitors are ineffective in RAS mutant tumors because they enhance homo-and heterodimerization of RAF kinases, leading to paradoxical activation of ERK …
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Rachel E. Lamson, Satoe Takahashi, Matthew J. Winters, Peter M. Pryciak, Dual Role for Membrane Localization in Yeast MAP Kinase Cascade Activation and Its Contribution to Signaling Fidelity Current Biology. ,vol. 16, pp. 618- 623 ,(2006) , 10.1016/J.CUB.2006.02.060
K. Arora, C. L. Brooks, Large-scale allosteric conformational transitions of adenylate kinase appear to involve a population-shift mechanism. Proceedings of the National Academy of Sciences of the United States of America. ,vol. 104, pp. 18496- 18501 ,(2007) , 10.1073/PNAS.0706443104
Doriano Fabbro, 25 years of small molecular weight kinase inhibitors: potentials and limitations. Molecular Pharmacology. ,vol. 87, pp. 766- 775 ,(2015) , 10.1124/MOL.114.095489
Malha Sahmi, Martin Lefrançois, Frank Sicheri, Marc Therrien, Thanashan Rajakulendran, A dimerization-dependent mechanism drives RAF catalytic activation Nature. ,vol. 461, pp. 542- 545 ,(2009) , 10.1038/NATURE08314
Matthew Holderfield, Marian M. Deuker, Frank McCormick, Martin McMahon, Targeting RAF kinases for cancer therapy: BRAF-mutated melanoma and beyond Nature Reviews Cancer. ,vol. 14, pp. 455- 467 ,(2014) , 10.1038/NRC3760
Adam C. Bastidas, Michael S. Deal, Jon M. Steichen, Malik M. Keshwani, Yurong Guo, Susan S. Taylor, Role of N-Terminal Myristylation in the Structure and Regulation of cAMP-Dependent Protein Kinase Journal of Molecular Biology. ,vol. 422, pp. 215- 229 ,(2012) , 10.1016/J.JMB.2012.05.021
Md Atiqur Rahman, Ali Salajegheh, Robert Anthony Smith, AK-Y Lam, None, BRAF inhibitors: From the laboratory to clinical trials Critical Reviews in Oncology Hematology. ,vol. 90, pp. 220- 232 ,(2014) , 10.1016/J.CRITREVONC.2013.12.008
Lufen Chang, Michael Karin, Mammalian MAP kinase signalling cascades Nature. ,vol. 410, pp. 37- 40 ,(2001) , 10.1038/35065000
Walter KOLCH, Meaningful relationships: the regulation of the Ras/Raf/MEK/ERK pathway by protein interactions. Biochemical Journal. ,vol. 351, pp. 289- 305 ,(2000) , 10.1042/BJ3510289
D. Matallanas, M. Birtwistle, D. Romano, A. Zebisch, J. Rauch, A. von Kriegsheim, W. Kolch, Raf Family Kinases: Old Dogs Have Learned New Tricks Genes & Cancer. ,vol. 2, pp. 232- 260 ,(2011) , 10.1177/1947601911407323