New perspectives for targeting RAF kinase in human cancer

[1]  Q. Lan,et al.  CSIG-19. FHL2 INTERACTS WITH EGFRVIII TO PROMOTE GLIOBLASTOMA GROWTH , 2017 .

[2]  B. Taylor,et al.  Tumours with class 3 BRAF mutants are sensitive to the inhibition of activated RAS , 2017, Nature.

[3]  M. Barbacid,et al.  A Braf kinase-inactive mutant induces lung adenocarcinoma , 2017, Nature.

[4]  Iain A. Stewart,et al.  The Search Continues , 2017, Nature.

[5]  Joshua M. Korn,et al.  BRAF-inhibitor Associated MEK Mutations Increase RAF-Dependent and -Independent Enzymatic Activity , 2017, Molecular Cancer Research.

[6]  W. Hahn,et al.  A brain-penetrant RAF dimer antagonist for the noncanonical BRAF oncoprotein of pediatric low-grade astrocytomas , 2017, Neuro-oncology.

[7]  R. Murphy,et al.  Discrete cytosolic macromolecular BRAF complexes exhibit distinct activities and composition , 2017, The EMBO journal.

[8]  M. Herlyn,et al.  An Integrated Model of RAF Inhibitor Action Predicts Inhibitor Activity against Oncogenic BRAF Signaling. , 2016, Cancer cell.

[9]  P. Stephens,et al.  Activation Mechanism of Oncogenic Deletion Mutations in BRAF, EGFR, and HER2. , 2016, Cancer cell.

[10]  J. Sosman,et al.  Genomic and Transcriptomic Features of Response to Anti-PD-1 Therapy in Metastatic Melanoma , 2016, Cell.

[11]  Axel Hoos,et al.  Non-alcoholic steatohepatitis: emerging molecular targets and therapeutic strategies , 2016, Nature Reviews Drug Discovery.

[12]  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.

[13]  I. Waizenegger,et al.  A Novel RAF Kinase Inhibitor with DFG-Out–Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation , 2016, Molecular Cancer Therapeutics.

[14]  Susan S. Taylor,et al.  Dynamics-Driven Allostery in Protein Kinases. , 2015, Trends in biochemical sciences.

[15]  Lisa M Haley,et al.  Clinical detection and categorization of uncommon and concomitant mutations involving BRAF , 2015, BMC Cancer.

[16]  James Tsai,et al.  RAF inhibitors that evade paradoxical MAPK pathway activation , 2015, Nature.

[17]  S. Cook,et al.  MEK1 and MEK2 inhibitors and cancer therapy: the long and winding road , 2015, Nature Reviews Cancer.

[18]  P. Gibbs,et al.  Phase II Pilot Study of Vemurafenib in Patients With Metastatic BRAF-Mutated Colorectal Cancer , 2015, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

[19]  O. Abdel-Wahab,et al.  BRAF Mutants Evade ERK-Dependent Feedback by Different Mechanisms that Determine Their Sensitivity to Pharmacologic Inhibition. , 2015, Cancer cell.

[20]  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.

[21]  Kai Wang,et al.  The distribution of BRAF gene fusions in solid tumors and response to targeted therapy , 2015, International journal of cancer.

[22]  J. Blay,et al.  Vemurafenib in Multiple Nonmelanoma Cancers with BRAF V600 Mutations. , 2015, The New England journal of medicine.

[23]  J. Ji,et al.  BGB-283, a Novel RAF Kinase and EGFR Inhibitor, Displays Potent Antitumor Activity in BRAF-Mutated Colorectal Cancers , 2015, Molecular Cancer Therapeutics.

[24]  J. Larkin,et al.  Pembrolizumab versus Ipilimumab in Advanced Melanoma. , 2015, The New England journal of medicine.

[25]  Steven J. M. Jones,et al.  Genomic Classification of Cutaneous Melanoma , 2015, Cell.

[26]  P. Hipskind,et al.  Discovery of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a pan-RAF inhibitor with minimal paradoxical activation and activity against BRAF or RAS mutant tumor cells. , 2015, Journal of medicinal chemistry.

[27]  M. Therrien,et al.  Regulation of RAF protein kinases in ERK signalling , 2015, Nature Reviews Molecular Cell Biology.

[28]  J. Massagué,et al.  Therapy-induced tumour secretomes promote resistance and tumour progression , 2015, Nature.

[29]  J. Larkin,et al.  Tunable-combinatorial mechanisms of acquired resistance limit the efficacy of BRAF/MEK cotargeting but result in melanoma drug addiction. , 2015, Cancer cell.

[30]  N. Carragher,et al.  Paradox-Breaking RAF Inhibitors that Also Target SRC Are Effective in Drug-Resistant BRAF Mutant Melanoma , 2015, Cancer cell.

[31]  Emmanuel C. Alozie,et al.  Promises and Challenges , 2015 .

[32]  N. Hayward,et al.  Increased MAPK reactivation in early resistance to dabrafenib/trametinib combination therapy of BRAF-mutant metastatic melanoma , 2014, Nature Communications.

[33]  Marc Therrien,et al.  Crystal structure of a BRAF kinase domain monomer explains basis for allosteric regulation , 2014, Nature Structural &Molecular Biology.

[34]  P. Poulikakos,et al.  Targeting RAS–ERK signalling in cancer: promises and challenges , 2014, Nature Reviews Drug Discovery.

[35]  J. Utikal,et al.  Combined BRAF and MEK inhibition versus BRAF inhibition alone in melanoma. , 2014, The New England journal of medicine.

[36]  P. Ascierto,et al.  Combined vemurafenib and cobimetinib in BRAF-mutated melanoma. , 2014, The New England journal of medicine.

[37]  Ariana Peck,et al.  Structure of the BRAF-MEK complex reveals a kinase activity independent role for BRAF in MAPK signaling. , 2014, Cancer cell.

[38]  Steven J. M. Jones,et al.  Comprehensive molecular profiling of lung adenocarcinoma , 2014, Nature.

[39]  Frank McCormick,et al.  Targeting RAF kinases for cancer therapy: BRAF-mutated melanoma and beyond , 2014, Nature Reviews Cancer.

[40]  Kaitlyn Le,et al.  Inhibition of mutant BRAF splice variant signaling by next‐generation, selective RAF inhibitors , 2014, Pigment cell & melanoma research.

[41]  G. Pupo,et al.  Differential activity of MEK and ERK inhibitors in BRAF inhibitor resistant melanoma , 2014, Molecular oncology.

[42]  M. Holderfield,et al.  Mechanism and consequences of RAF kinase activation by small-molecule inhibitors , 2014, British Journal of Cancer.

[43]  Dirk Schadendorf,et al.  Safety and efficacy of vemurafenib in BRAF(V600E) and BRAF(V600K) mutation-positive melanoma (BRIM-3): extended follow-up of a phase 3, randomised, open-label study. , 2014, The Lancet. Oncology.

[44]  Tomoyasu Ishikawa,et al.  Antitumor activity of the selective pan-RAF inhibitor TAK-632 in BRAF inhibitor-resistant melanoma. , 2013, Cancer research.

[45]  Wei Xu,et al.  Concurrent MEK2 mutation and BRAF amplification confer resistance to BRAF and MEK inhibitors in melanoma. , 2013, Cell reports.

[46]  Susan S. Taylor,et al.  Allosteric Activation of Functionally Asymmetric RAF Kinase Dimers , 2013, Cell.

[47]  Tomoyasu Ishikawa,et al.  Discovery of a selective kinase inhibitor (TAK-632) targeting pan-RAF inhibition: design, synthesis, and biological evaluation of C-7-substituted 1,3-benzothiazole derivatives. , 2013, Journal of medicinal chemistry.

[48]  Kaitlyn Le,et al.  Selective RAF inhibitor impairs ERK1/2 phosphorylation and growth in mutant NRAS, vemurafenib‐resistant melanoma cells , 2013, Pigment cell & melanoma research.

[49]  M. Therrien,et al.  Inhibitors that stabilize a closed RAF kinase domain conformation induce dimerization , 2013, Nature chemical biology.

[50]  F. McCormick,et al.  RAF inhibitors activate the MAPK pathway by relieving inhibitory autophosphorylation. , 2013, Cancer cell.

[51]  G. Pupo,et al.  Antiproliferative Effects of Continued Mitogen-Activated Protein Kinase Pathway Inhibition following Acquired Resistance to BRAF and/or MEK Inhibition in Melanoma , 2013, Molecular Cancer Therapeutics.

[52]  A. Viale,et al.  Relief of Feedback Inhibition of Her3 Transcription by Raf and Mek Inhibitors Attenuates Their Antitumor Effects in Braf -mutant Thyroid Carcinomas Human Oncology and Pathogenesis Program, Pathology, And , 2022 .

[53]  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.

[54]  S. O'toole,et al.  BRAF inhibitor activity in V600R metastatic melanoma. , 2013, European journal of cancer.

[55]  D. Morrison,et al.  Effects of Raf dimerization and its inhibition on normal and disease-associated Raf signaling. , 2013, Molecular cell.

[56]  G. Madonna,et al.  Effect of dabrafenib on melanoma cell lines harbouring the BRAFV600D/R mutations , 2013, BMC Cancer.

[57]  S. Chandarlapaty,et al.  Relief of profound feedback inhibition of mitogenic signaling by RAF inhibitors attenuates their activity in BRAFV600E melanomas. , 2012, Cancer cell.

[58]  Junfeng Xia,et al.  BRAF(L597) mutations in melanoma are associated with sensitivity to MEK inhibitors. , 2012, Cancer discovery.

[59]  A. Hauschild,et al.  Dabrafenib in BRAF-mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trial , 2012, The Lancet.

[60]  Jane Fridlyand,et al.  Widespread potential for growth-factor-driven resistance to anticancer kinase inhibitors , 2012, Nature.

[61]  T. Golub,et al.  Tumour micro-environment elicits innate resistance to RAF inhibitors through HGF secretion , 2012, Nature.

[62]  David C. Smith,et al.  Safety, activity, and immune correlates of anti-PD-1 antibody in cancer. , 2012, The New England journal of medicine.

[63]  W. Sellers,et al.  Modulation of activation-loop phosphorylation by JAK inhibitors is binding mode dependent. , 2012, Cancer discovery.

[64]  A. von Deimling,et al.  Distinct requirement for an intact dimer interface in wild‐type, V600E and kinase‐dead B‐Raf signalling , 2012, The EMBO journal.

[65]  M. Brown,et al.  Dabrafenib in patients with melanoma, untreated brain metastases, and other solid tumours: a phase 1 dose-escalation trial , 2012, The Lancet.

[66]  Mari Mino-Kenudson,et al.  EGFR-mediated re-activation of MAPK signaling contributes to insensitivity of BRAF mutant colorectal cancers to RAF inhibition with vemurafenib. , 2012, Cancer discovery.

[67]  Raffaella Faraoni,et al.  CEP-32496: A Novel Orally Active BRAFV600E Inhibitor with Selective Cellular and In Vivo Antitumor Activity , 2012, Molecular Cancer Therapeutics.

[68]  R. Bernards,et al.  Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR , 2012, Nature.

[69]  K. Flaherty,et al.  RAS mutations in cutaneous squamous-cell carcinomas in patients treated with BRAF inhibitors. , 2012, The New England journal of medicine.

[70]  S. Nelson,et al.  Melanoma whole exome sequencing identifies V600EB-RAF amplification-mediated acquired B-RAF inhibitor resistance , 2012, Nature Communications.

[71]  Tom Misteli,et al.  RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E) , 2011, Nature.

[72]  C. Der,et al.  Inhibition of Ras for cancer treatment: the search continues. , 2011, Future medicinal chemistry.

[73]  Nikhil Wagle,et al.  Dissecting therapeutic resistance to RAF inhibition in melanoma by tumor genomic profiling. , 2011, Journal of clinical oncology : official journal of the American Society of Clinical Oncology.

[74]  W. Kolch,et al.  Raf family kinases: old dogs have learned new tricks. , 2011, Genes & cancer.

[75]  N. Rosen,et al.  Mutant BRAF melanomas--dependence and resistance. , 2011, Cancer cell.

[76]  S. Nelson,et al.  Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation , 2010, Nature.

[77]  Damien Kee,et al.  Acquired resistance to BRAF inhibitors mediated by a RAF kinase switch in melanoma can be overcome by cotargeting MEK and IGF-1R/PI3K. , 2010, Cancer cell.

[78]  Justin Chapman,et al.  Characterization of PF-4708671, a novel and highly specific inhibitor of p70 ribosomal S6 kinase (S6K1). , 2010, The Biochemical journal.

[79]  W. Hahn,et al.  Recurrent BRAF mutations in Langerhans cell histiocytosis. , 2010, Blood.

[80]  Kam Y. J. Zhang,et al.  Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma , 2010, Nature.

[81]  K. Flaherty,et al.  Inhibition of mutated, activated BRAF in metastatic melanoma. , 2010, The New England journal of medicine.

[82]  D. Schadendorf,et al.  Improved survival with ipilimumab in patients with metastatic melanoma. , 2010, The New England journal of medicine.

[83]  B. Taylor,et al.  The RAF inhibitor PLX4032 inhibits ERK signaling and tumor cell proliferation in a V600E BRAF-selective manner , 2010, Proceedings of the National Academy of Sciences.

[84]  Francesca Demichelis,et al.  Rearrangements of the RAF kinase pathway in prostate cancer, gastric cancer and melanoma , 2010, Nature Medicine.

[85]  M. Belvin,et al.  RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth , 2010, Nature.

[86]  Chao Zhang,et al.  RAF inhibitors transactivate RAF dimers and ERK signaling in cells with wild-type BRAF , 2010, Nature.

[87]  Michael Krauthammer,et al.  PLX4032, a selective BRAFV600E kinase inhibitor, activates the ERK pathway and enhances cell migration and proliferation of BRAFWT melanoma cells , 2010, Pigment cell & melanoma research.

[88]  J. Reis-Filho,et al.  Kinase-Dead BRAF and Oncogenic RAS Cooperate to Drive Tumor Progression through CRAF , 2010, Cell.

[89]  Marc Therrien,et al.  A dimerization-dependent mechanism drives RAF catalytic activation , 2009, Nature.

[90]  Chao Zhang,et al.  Inhibitor Hijacking of Akt Activation , 2009, Nature chemical biology.

[91]  P. Parker,et al.  PKC maturation is promoted by nucleotide pocket occupation independently of intrinsic kinase activity , 2009, Nature Structural &Molecular Biology.

[92]  M. Belvin,et al.  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. , 2009, Cancer research.

[93]  David T. W. Jones,et al.  Tandem duplication producing a novel oncogenic BRAF fusion gene defines the majority of pilocytic astrocytomas. , 2008, Cancer research.

[94]  Dieter Häussinger,et al.  Sorafenib in advanced hepatocellular carcinoma. , 2008, The New England journal of medicine.

[95]  J. Hamm,et al.  A Phase 1 dose-escalation trial of glufosfamide in combination with gemcitabine in solid tumors including pancreatic adenocarcinoma , 2008, Cancer Chemotherapy and Pharmacology.

[96]  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.

[97]  C. Der,et al.  Targeting the Raf-MEK-ERK mitogen-activated protein kinase cascade for the treatment of cancer , 2007, Oncogene.

[98]  O. Rath,et al.  MAP kinase signalling pathways in cancer , 2007, Oncogene.

[99]  Apurva A Desai,et al.  Sorafenib in advanced clear-cell renal-cell carcinoma. , 2007, The New England journal of medicine.

[100]  Hieu T. Do,et al.  Demonstration of a genetic therapeutic index for tumors expressing oncogenic BRAF by the kinase inhibitor SB-590885. , 2006, Cancer research.

[101]  W. Kolch,et al.  Regulation and Role of Raf-1/B-Raf Heterodimerization , 2006, Molecular and Cellular Biology.

[102]  Todd R. Golub,et al.  BRAF mutation predicts sensitivity to MEK inhibition , 2006, Nature.

[103]  D. Barford,et al.  Wild-type and mutant B-RAF activate C-RAF through distinct mechanisms involving heterodimerization. , 2005, Molecular cell.

[104]  Richard Marais,et al.  The RAF proteins take centre stage , 2004, Nature Reviews Molecular Cell Biology.

[105]  P. C. Chin,et al.  The c‐Raf inhibitor GW5074 provides neuroprotection in vitro and in an animal model of neurodegeneration through a MEK‐ERK and Akt‐independent mechanism , 2004, Journal of neurochemistry.

[106]  D. Barford,et al.  Mechanism of Activation of the RAF-ERK Signaling Pathway by Oncogenic Mutations of B-RAF , 2004, Cell.

[107]  J. McCubrey,et al.  Differential effects of kinase cascade inhibitors on neoplastic and cytokine-mediated cell proliferation , 2003, Leukemia.

[108]  Yuri E Nikiforov,et al.  High prevalence of BRAF mutations in thyroid cancer: genetic evidence for constitutive activation of the RET/PTC-RAS-BRAF signaling pathway in papillary thyroid carcinoma. , 2003, Cancer research.

[109]  K. Kinzler,et al.  Tumorigenesis: RAF/RAS oncogenes and mismatch-repair status , 2002, Nature.

[110]  A. Nicholson,et al.  Mutations of the BRAF gene in human cancer , 2002, Nature.

[111]  G. Bollag,et al.  Discovery of a novel Raf kinase inhibitor. , 2001, Endocrine-related cancer.

[112]  U. Rapp,et al.  Active Ras induces heterodimerization of cRaf and BRaf. , 2001, Cancer research.

[113]  Philip R. Cohen,et al.  Paradoxical activation of Raf by a novel Raf inhibitor. , 1999, Chemistry & biology.

[114]  R. Stephens,et al.  Autoregulation of the Raf-1 serine/threonine kinase. , 1998, Proceedings of the National Academy of Sciences of the United States of America.

[115]  P. Warne,et al.  Direct interaction of Ras and the amino-terminal region of Raf-1 in vitro , 1993, Nature.

[116]  Jonathan A. Cooper,et al.  Mammalian Ras interacts directly with the serine/threonine kinase raf , 1993, Cell.

[117]  M. Weber,et al.  Complexes of Ras.GTP with Raf-1 and mitogen-activated protein kinase kinase. , 1993, Science.

[118]  M. Mandalà,et al.  Immunotolerance as a Mechanism of Resistance to Targeted Therapies in Melanoma. , 2018, Handbook of experimental pharmacology.

[119]  Antoni Ribas,et al.  Acquired resistance and clonal evolution in melanoma during BRAF inhibitor therapy. , 2014, Cancer discovery.

[120]  T. Eberlein,et al.  Improved Survival with Vemurafenib in Melanoma with BRAF V600E Mutation , 2012 .

[121]  A. Tefferi,et al.  BRAF mutations in hairy-cell leukemia. , 2011, The New England journal of medicine.

[122]  M. Gordon,et al.  RG7204 (PLX4032), a Selective BRAFV600E Inhibitor, Displays Potent Antitumor Activity in Preclinical Melanoma Models , 2010 .

[123]  N. Gray,et al.  Targeting cancer with small molecule kinase inhibitors , 2009, Nature Reviews Cancer.

[124]  Amy Young,et al.  Ras signaling and therapies. , 2009, Advances in cancer research.

[125]  C. Hancock The long and winding road , 2005, Nature Reviews Drug Discovery.

[126]  X. F. Zhang,et al.  Ras activation of the Raf kinase: tyrosine kinase recruitment of the MAP kinase cascade. , 2001, Recent progress in hormone research.