Targeting the Raf kinases in human cancer: the Raf dimer dilemma
暂无分享,去创建一个
[1] M. Therrien,et al. RAF inhibitors promote RAS-RAF interaction by allosterically disrupting RAF autoinhibition , 2017, Nature Communications.
[2] W. Hahn,et al. A brain-penetrant RAF dimer antagonist for the noncanonical BRAF oncoprotein of pediatric low-grade astrocytomas , 2017, Neuro-oncology.
[3] Xiu-juan Yuan,et al. LY3009120, a panRAF inhibitor, has significant anti-tumor activity in BRAF and KRAS mutant preclinical models of colorectal cancer , 2016, Oncotarget.
[4] D. Morrison,et al. Inhibition of Ras/Raf/MEK/ERK Pathway Signaling by a Stress-Induced Phospho-Regulatory Circuit. , 2016, Molecular cell.
[5] G. Bollag,et al. Preclinical efficacy of a RAF inhibitor that evades paradoxical MAPK pathway activation in protein kinase BRAF-mutant lung cancer , 2016, Proceedings of the National Academy of Sciences.
[6] M. Herlyn,et al. An Integrated Model of RAF Inhibitor Action Predicts Inhibitor Activity against Oncogenic BRAF Signaling. , 2016, Cancer cell.
[7] M. Herlyn,et al. Corrections: An Integrated Model of RAF Inhibitor Action Predicts Inhibitor Activity against Oncogenic BRAF Signaling (Cancer Cell (2016) 30(3) (501–503) (S1535610816302847) (10.1016/j.ccell.2016.06.024)) , 2016 .
[8] K. Shokat,et al. Direct small-molecule inhibitors of KRAS: from structural insights to mechanism-based design , 2016, Nature Reviews Drug Discovery.
[9] P. Stephens,et al. Activation Mechanism of Oncogenic Deletion Mutations in BRAF, EGFR, and HER2. , 2016, Cancer cell.
[10] Vivek Subbiah,et al. Genomically Driven Tumors and Actionability across Histologies: BRAF-Mutant Cancers as a Paradigm , 2016, Molecular Cancer Therapeutics.
[11] Shih-Hsun Chen,et al. Oncogenic BRAF Deletions That Function as Homodimers and Are Sensitive to Inhibition by RAF Dimer Inhibitor LY3009120. , 2016, Cancer discovery.
[12] Neal Rosen,et al. Allele-specific inhibitors inactivate mutant KRAS G12C by a trapping mechanism , 2016, Science.
[13] James Tsai,et al. RAF inhibitors that evade paradoxical MAPK pathway activation , 2015, Nature.
[14] Susan S. Taylor,et al. Integration of signaling in the kinome: Architecture and regulation of the αC Helix. , 2015, Biochimica et biophysica acta.
[15] O. Abdel-Wahab,et al. BRAF Mutants Evade ERK-Dependent Feedback by Different Mechanisms that Determine Their Sensitivity to Pharmacologic Inhibition. , 2015, Cancer cell.
[16] Xiwen Ma,et al. Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers. , 2015, Cancer cell.
[17] M. Therrien,et al. Regulation of RAF protein kinases in ERK signalling , 2015, Nature Reviews Molecular Cell Biology.
[18] N. Carragher,et al. Paradox-Breaking RAF Inhibitors that Also Target SRC Are Effective in Drug-Resistant BRAF Mutant Melanoma , 2015, Cancer cell.
[19] Ariana Peck,et al. Structure of the BRAF-MEK complex reveals a kinase activity independent role for BRAF in MAPK signaling. , 2014, Cancer cell.
[20] N. Rosen,et al. Tumor adaptation and resistance to RAF inhibitors , 2013, Nature Medicine.
[21] D. Morrison,et al. The importance of Raf dimerization in cell signaling , 2013, Small GTPases.
[22] V. Sondak,et al. Paradoxical oncogenesis—the long-term effects of BRAF inhibition in melanoma , 2013, Nature Reviews Clinical Oncology.
[23] M. Therrien,et al. Inhibitors that stabilize a closed RAF kinase domain conformation induce dimerization , 2013, Nature chemical biology.
[24] R. Marais,et al. Deja Vu: EGF receptors drive resistance to BRAF inhibitors. , 2013, Cancer discovery.
[25] A. Resnick,et al. Paradoxical activation and RAF inhibitor resistance of BRAF protein kinase fusions characterizing pediatric astrocytomas , 2013, Proceedings of the National Academy of Sciences.
[26] D. Morrison,et al. Effects of Raf dimerization and its inhibition on normal and disease-associated Raf signaling. , 2013, Molecular cell.
[27] N. Rosen,et al. Induction of cutaneous squamous cell carcinomas by RAF inhibitors: cause for concern? , 2012, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.
[28] K. Flaherty,et al. RAS mutations in cutaneous squamous-cell carcinomas in patients treated with BRAF inhibitors. , 2012, The New England journal of medicine.
[29] Tom Misteli,et al. RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E) , 2011, Nature.
[30] E. Reddy,et al. Discovery of a clinical stage multi-kinase inhibitor sodium (E)-2-{2-methoxy-5-[(2',4',6'-trimethoxystyrylsulfonyl)methyl]phenylamino}acetate (ON 01910.Na): synthesis, structure-activity relationship, and biological activity. , 2011, Journal of medicinal chemistry.
[31] D. Morrison,et al. RAF Inhibitor-Induced KSR1/B-RAF Binding and Its Effects on ERK Cascade Signaling , 2011, Current Biology.
[32] U. Rapp,et al. Single Substitution within the RKTR Motif Impairs Kinase Activity but Promotes Dimerization of RAF Kinase* , 2011, The Journal of Biological Chemistry.
[33] Kam Y. J. Zhang,et al. Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma , 2010, Nature.
[34] M. Belvin,et al. RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth , 2010, Nature.
[35] Chao Zhang,et al. RAF inhibitors transactivate RAF dimers and ERK signaling in cells with wild-type BRAF , 2010, Nature.
[36] J. Reis-Filho,et al. Kinase-Dead BRAF and Oncogenic RAS Cooperate to Drive Tumor Progression through CRAF , 2010, Cell.
[37] Kam Y. J. Zhang,et al. Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity , 2008, Proceedings of the National Academy of Sciences.
[38] Ming Zhou,et al. Regulation of Raf-1 by direct feedback phosphorylation. , 2005, Molecular cell.
[39] U. Rapp,et al. Active Ras induces heterodimerization of cRaf and BRaf. , 2001, Cancer research.
[40] M. Herlyn,et al. An Integrated Model of RAF Inhibitor Action Predicts Inhibitor Activity against Oncogenic BRAF Signaling. , 2016, Cancer cell.
[41] A. McCullough. RAS Mutations in Cutaneous Squamous-Cell Carcinomas in Patients Treated with BRAF Inhibitors , 2013 .