COT drives resistance to RAF inhibition through MAP kinase pathway reactivation
作者： Cory M. Johannessen , Jesse S. Boehm , So Young Kim , Sapana R. Thomas , Leslie Wardwell
DOI: 10.1038/NATURE09627
关键词: MAP kinase kinase kinase 、 Raf Kinase Inhibitor 、 MAPK/ERK pathway 、 Cancer research 、 Biology 、 Mitogen-activated protein kinase 、 Mitogen-activated protein kinase kinase 、 Proto-Oncogene Proteins B-raf 、 Kinase activity 、 Proto-Oncogene Proteins c-raf
摘要: Oncogenic mutations in the serine/threonine kinase B-RAF (also known as BRAF) are found in 50–70% of malignant melanomas 1 . Pre-clinical studies have demonstrated that the B-…
nature.com
core.ac.uk
harvard.edu
uzh.ch
researchgate.net 
sci-hub.se 参考文章(29)
Klaus P. Hoeflich, Sylvia Herter, Janet Tien, Leo Wong, Leanne Berry, Jocelyn Chan, Carol O'Brien, Zora Modrusan, Somasekar Seshagiri, Mark Lackner, Howard Stern, Edna Choo, Lesley Murray, Lori S. Friedman, Marcia Belvin, Antitumor Efficacy of the Novel RAF Inhibitor GDC-0879 Is Predicted by BRAFV600E Mutational Status and Sustained Extracellular Signal-Regulated Kinase/Mitogen-Activated Protein Kinase Pathway Suppression Cancer Research. ,vol. 69, pp. 3042- 3051 ,(2009) , 10.1158/0008-5472.CAN-08-3563
Dawn George, Michael Friedman, Hamish Allen, Maria Argiriadi, Claude Barberis, Agnieszka Bischoff, Anca Clabbers, Kevin Cusack, Richard Dixon, Shannon Fix-Stenzel, Thomas Gordon, Bernd Janssen, Yong Jia, Maria Moskey, Christopher Quinn, Jose-Andres Salmeron, Neil Wishart, Kevin Woller, Zhengtian Yu, Discovery of thieno[2,3-c]pyridines as potent COT inhibitors Bioorganic & Medicinal Chemistry Letters. ,vol. 18, pp. 4952- 4955 ,(2008) , 10.1016/J.BMCL.2008.08.037
Esther Edlundh-Rose, Suzanne Egyha??zi, Katarina Omholt, Eva Mansson-Brahme, Anton Platz, Johan Hansson, Joakim Lundeberg, NRAS and BRAF mutations in melanoma tumours in relation to clinical characteristics: a study based on mutation screening by pyrosequencing Melanoma Research. ,vol. 16, pp. 471- 478 ,(2006) , 10.1097/01.CMR.0000232300.22032.86
J. A. Engelman, K. Zejnullahu, T. Mitsudomi, Y. Song, C. Hyland, J. O. Park, N. Lindeman, C.-M. Gale, X. Zhao, J. Christensen, T. Kosaka, A. J. Holmes, A. M. Rogers, F. Cappuzzo, T. Mok, C. Lee, B. E. Johnson, L. C. Cantley, P. A. Janne, MET Amplification Leads to Gefitinib Resistance in Lung Cancer by Activating ERBB3 Signaling Science. ,vol. 316, pp. 1039- 1043 ,(2007) , 10.1126/SCIENCE.1141478
Mercedes E Gorre, Mansoor Mohammed, Katharine Ellwood, Nicholas Hsu, Ron Paquette, P Nagesh Rao, Charles L Sawyers, Clinical Resistance to STI-571 Cancer Therapy Caused by BCR-ABL Gene Mutation or Amplification Science. ,vol. 293, pp. 876- 880 ,(2001) , 10.1126/SCIENCE.1062538
Poulikos I. Poulikakos, Chao Zhang, Gideon Bollag, Kevan M. Shokat, Neal Rosen, RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF Nature. ,vol. 464, pp. 427- 430 ,(2010) , 10.1038/NATURE08902
Ante S Lundberg, Scott H Randell, Sheila A Stewart, Brian Elenbaas, Kimberly A Hartwell, Mary W Brooks, Mark D Fleming, John C Olsen, Scott W Miller, Robert A Weinberg, William C Hahn, Immortalization and transformation of primary human airway epithelial cells by gene transfer. Oncogene. ,vol. 21, pp. 4577- 4586 ,(2002) , 10.1038/SJ.ONC.1205550
U. McDermott, S. V. Sharma, L. Dowell, P. Greninger, C. Montagut, J. Lamb, H. Archibald, R. Raudales, A. Tam, D. Lee, S. M. Rothenberg, J. G. Supko, R. Sordella, L. E. Ulkus, A. J. Iafrate, S. Maheswaran, C. N. Njauw, H. Tsao, L. Drew, J. H. Hanke, X.-J. Ma, M. G. Erlander, N. S. Gray, D. A. Haber, J. Settleman, Identification of genotype-correlated sensitivity to selective kinase inhibitors by using high-throughput tumor cell line profiling Proceedings of the National Academy of Sciences of the United States of America. ,vol. 104, pp. 19936- 19941 ,(2007) , 10.1073/PNAS.0707498104
C. M. Emery, K. G. Vijayendran, M. C. Zipser, A. M. Sawyer, L. Niu, J. J. Kim, C. Hatton, R. Chopra, P. A. Oberholzer, M. B. Karpova, L. E. MacConaill, J. Zhang, N. S. Gray, W. R. Sellers, R. Dummer, L. A. Garraway, MEK1 mutations confer resistance to MEK and B-RAF inhibition Proceedings of the National Academy of Sciences of the United States of America. ,vol. 106, pp. 20411- 20416 ,(2009) , 10.1073/PNAS.0905833106
Georgia Hatzivassiliou, Kyung Song, Ivana Yen, Barbara J. Brandhuber, Daniel J. Anderson, Ryan Alvarado, Mary J. C. Ludlam, David Stokoe, Susan L. Gloor, Guy Vigers, Tony Morales, Ignacio Aliagas, Bonnie Liu, Steve Sideris, Klaus P. Hoeflich, Bijay S. Jaiswal, Somasekar Seshagiri, Hartmut Koeppen, Marcia Belvin, Lori S. Friedman, Shiva Malek, RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth Nature. ,vol. 464, pp. 431- 435 ,(2010) , 10.1038/NATURE08833