Targeting the MAPK Pathway in KRAS-Driven Tumors.

[1]  J. Fernandez-Banet,et al.  The KRASG12C Inhibitor, MRTX849, Provides Insight Toward Therapeutic Susceptibility of KRAS Mutant Cancers in Mouse Models and Patients. , 2019, Cancer discovery.

[2]  J. Desai,et al.  The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity , 2019, Nature.

[3]  R. Rabadán,et al.  Complete Regression of Advanced Pancreatic Ductal Adenocarcinomas upon Combined Inhibition of EGFR and C-RAF. , 2019, Cancer cell.

[4]  A. Rose.  Encorafenib and binimetinib for the treatment of BRAF V600E/K-mutated melanoma. , 2019, Drugs of today.

[5]  E. Petricoin,et al.  Combination of ERK and autophagy inhibition as a treatment approach for pancreatic cancer , 2019, Nature Medicine.

[6]  P. Savoia,et al.  Targeting the ERK Signaling Pathway in Melanoma , 2019, International journal of molecular sciences.

[7]  R. Yaeger,et al.  Targeting Alterations in the RAF-MEK Pathway. , 2019, Cancer discovery.

[8]  H. Briem,et al.  Discovery of potent SOS1 inhibitors that block RAS activation via disruption of the RAS–SOS1 interaction , 2019, Proceedings of the National Academy of Sciences.

[9]  J. Yap,et al.  Protective autophagy elicited by RAF→MEK→ERK inhibition suggests a treatment strategy for RAS-driven cancers , 2019, Nature Medicine.

[10]  M. Barbacid,et al.  RAF inhibitor PLX8394 selectively disrupts BRAF-dimers and RAS-independent BRAF mutant-driven signaling , 2018, Nature Medicine.

[11]  P. Crespo,et al.  The RAS-ERK pathway: A route for couples , 2018, Science Signaling.

[12]  R. Corcoran,et al.  Therapeutic strategies to target RAS-mutant cancers , 2018, Nature Reviews Clinical Oncology.

[13]  R. Bernards,et al.  SHP2 is required for growth of KRAS-mutant non-small-cell lung cancer in vivo , 2018, Nature Medicine.

[14]  W. Birchmeier,et al.  Mutant KRAS-driven cancers depend on PTPN11/SHP2 phosphatase , 2018, Nature Medicine.

[15]  B. Taylor,et al.  Allele-Specific Mechanisms of Activation of MEK1 Mutants Determine Their Properties. , 2018, Cancer discovery.

[16]  Shanshan Gu,et al.  PROTACs: An Emerging Targeting Technique for Protein Degradation in Drug Discovery , 2018, BioEssays : news and reviews in molecular, cellular and developmental biology.

[17]  F. McCormick.  c-Raf in KRas Mutant Cancers: A Moving Target. , 2018, Cancer cell.

[18]  M. Barbacid,et al.  c-RAF Ablation Induces Regression of Advanced Kras/Trp53 Mutant Lung Adenocarcinomas by a Mechanism Independent of MAPK Signaling. , 2018, Cancer cell.

[19]  D. Morrison,et al.  Targeting the Raf kinases in human cancer: the Raf dimer dilemma , 2017, British Journal of Cancer.

[20]  Max A. Horlbeck,et al.  Combined CRISPRi/a-Based Chemical Genetic Screens Reveal that Rigosertib Is a Microtubule-Destabilizing Agent , 2017, Molecular cell.

[21]  P. Queirolo,et al.  Binimetinib for the treatment of NRAS-mutant melanoma , 2017, Expert review of anticancer therapy.

[22]  N. Blüthgen,et al.  A compendium of ERK targets , 2017, FEBS letters.

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

[24]  L. Larue,et al.  RAF proteins exert both specific and compensatory functions during tumour progression of NRAS-driven melanoma , 2017, Nature Communications.

[25]  P. Jänne,et al.  Selumetinib Plus Docetaxel Compared With Docetaxel Alone and Progression-Free Survival in Patients With KRAS-Mutant Advanced Non–Small Cell Lung Cancer: The SELECT-1 Randomized Clinical Trial , 2017, JAMA.

[26]  K. Zatloukal,et al.  A cell-autonomous tumour suppressor role of RAF1 in hepatocarcinogenesis , 2016, Nature Communications.

[27]  D. Morrison,et al.  Inhibition of Ras/Raf/MEK/ERK Pathway Signaling by a Stress-Induced Phospho-Regulatory Circuit. , 2016, Molecular cell.

[28]  Jurgen Müller,et al.  Negative feedback regulation of the ERK1/2 MAPK pathway , 2016, Cellular and Molecular Life Sciences.

[29]  K. Dutta,et al.  A Small Molecule RAS-Mimetic Disrupts RAS Association with Effector Proteins to Block Signaling , 2016, Cell.

[30]  C. Der,et al.  Targeting RAS-mutant cancers: is ERK the key? , 2015, Trends in cancer.

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

[32]  S. Anand,et al.  Kinase-independent role for CRAF-driving tumour radioresistance via CHK2 , 2015, Nature Communications.

[33]  S. Meloche,et al.  Functional Redundancy of ERK1 and ERK2 MAP Kinases during Development. , 2015, Cell reports.

[34]  G. Kéri,et al.  Small Molecule Inhibition of ERK Dimerization Prevents Tumorigenesis by RAS-ERK Pathway Oncogenes. , 2015, Cancer cell.

[35]  Enrico Desideri,et al.  Alike but Different: RAF Paralogs and Their Signaling Outputs , 2015, Cell.

[36]  D. Planchard,et al.  A randomized phase II study of the MEK1/MEK2 inhibitor trametinib (GSK1120212) compared with docetaxel in KRAS-mutant advanced non-small-cell lung cancer (NSCLC)†. , 2015, Annals of oncology : official journal of the European Society for Medical Oncology.

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

[38]  L. Shultz,et al.  MEK Guards Proteome Stability and Inhibits Tumor-Suppressive Amyloidogenesis via HSF1 , 2015, Cell.

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

[40]  R. Bernards,et al.  Loss of p53 induces cell proliferation via Ras-independent activation of the Raf/Mek/Erk signaling pathway , 2014, Proceedings of the National Academy of Sciences.

[41]  Joon-Oh Park,et al.  A randomised, double-blind, placebo-controlled trial of trametinib, an oral MEK inhibitor, in combination with gemcitabine for patients with untreated metastatic adenocarcinoma of the pancreas. , 2014, European journal of cancer.

[42]  F. Kern,et al.  Essential, non-redundant roles of B-Raf and Raf-1 in Ras-driven skin tumorigenesis , 2013, Oncogene.

[43]  M. Baccarini,et al.  MEK1 Is Required for PTEN Membrane Recruitment, AKT Regulation, and the Maintenance of Peripheral Tolerance , 2013, Molecular cell.

[44]  R. Rad,et al.  Selective requirement of PI3K/PDK1 signaling for Kras oncogene-driven pancreatic cell plasticity and cancer. , 2013, Cancer cell.

[45]  Jens T Siveke,et al.  EGF receptor is required for KRAS-induced pancreatic tumorigenesis. , 2012, Cancer cell.

[46]  M. Barbacid,et al.  EGF receptor signaling is essential for k-ras oncogene-driven pancreatic ductal adenocarcinoma. , 2012, Cancer cell.

[47]  K. Flaherty,et al.  Safety, pharmacokinetic, pharmacodynamic, and efficacy data for the oral MEK inhibitor trametinib: a phase 1 dose-escalation trial. , 2012, The Lancet. Oncology.

[48]  Kyoung-Han Kim,et al.  Increased BRAF Heterodimerization Is the Common Pathogenic Mechanism for Noonan Syndrome-Associated RAF1 Mutants , 2012, Molecular and Cellular Biology.

[49]  T. Ciuleanu,et al.  A phase II open-label randomized study to assess the efficacy and safety of selumetinib (AZD6244 [ARRY-142886]) versus capecitabine in patients with advanced or metastatic pancreatic cancer who have failed first-line gemcitabine therapy , 2012, Investigational New Drugs.

[50]  R. Roskoski.  MEK1/2 dual-specificity protein kinases: structure and regulation. , 2012, Biochemical and biophysical research communications.

[51]  D. Tuveson,et al.  C-Raf is required for the initiation of lung cancer by K-Ras(G12D). , 2011, Cancer discovery.

[52]  Edward S. Kim,et al.  The BATTLE trial: personalizing therapy for lung cancer. , 2011, Cancer discovery.

[53]  M. Barbacid,et al.  c-Raf, but not B-Raf, is essential for development of K-Ras oncogene-driven non-small cell lung carcinoma. , 2011, Cancer cell.

[54]  R. Roskoski,et al.  RAF protein-serine/threonine kinases: structure and regulation. , 2010, Biochemical and biophysical research communications.

[55]  Boris N. Kholodenko,et al.  Signalling ballet in space and time , 2010, Nature Reviews Molecular Cell Biology.

[56]  Eric B Haura,et al.  A Phase II Study of PD-0325901, an Oral MEK Inhibitor, in Previously Treated Patients with Advanced Non–Small Cell Lung Cancer , 2010, Clinical Cancer Research.

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

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

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

[60]  M. Baccarini,et al.  Raf-1 addiction in Ras-induced skin carcinogenesis. , 2009, Cancer cell.

[61]  R. Perez-soler,et al.  Skin toxicities associated with epidermal growth factor receptor inhibitors , 2009, Targeted Oncology.

[62]  P. Khavari,et al.  Selective role for Mek1 but not Mek2 in the induction of epidermal neoplasia. , 2009, Cancer research.

[63]  O. Carugo,et al.  A Mek1–Mek2 heterodimer determines the strength and duration of the Erk signal , 2009, Nature Structural &Molecular Biology.

[64]  J. Hussain,et al.  CRAF autophosphorylation of serine 621 is required to prevent its proteasome-mediated degradation. , 2008, Molecular cell.

[65]  M. Carless,et al.  A small molecule disruptor of Rb/Raf-1 interaction inhibits cell proliferation, angiogenesis, and growth of human tumor xenografts in nude mice. , 2008, Cancer research.

[66]  P. Khavari,et al.  Mek1/2 MAPK kinases are essential for Mammalian development, homeostasis, and Raf-induced hyperplasia. , 2007, Developmental cell.

[67]  S. Wilhelm,et al.  Discovery and development of sorafenib: a multikinase inhibitor for treating cancer , 2006, Nature Reviews Drug Discovery.

[68]  J. Charron,et al.  Requirement for Map2k1 (Mek1) in extra-embryonic ectoderm during placentogenesis , 2006, Development.

[69]  M. Baccarini,et al.  Essential role of B-Raf in ERK activation during extraembryonic development , 2006, Proceedings of the National Academy of Sciences of the United States of America.

[70]  M. Baccarini,et al.  Raf-1 sets the threshold of Fas sensitivity by modulating Rok-α signaling , 2005, The Journal of cell biology.

[71]  G. Landreth,et al.  ERK1-Deficient Mice Show Normal T Cell Effector Function and Are Highly Susceptible to Experimental Autoimmune Encephalomyelitis1 , 2005, The Journal of Immunology.

[72]  J. Small,et al.  Raf-1 regulates Rho signaling and cell migration , 2005, The Journal of cell biology.

[73]  Walter Kolch,et al.  Role of the Kinase MST2 in Suppression of Apoptosis by the Proto-Oncogene Product Raf-1 , 2004, Science.

[74]  Naoya Nakai,et al.  Essential role for ERK2 mitogen‐activated protein kinase in placental development , 2003, Genes to cells : devoted to molecular & cellular mechanisms.

[75]  S. Meloche,et al.  An essential function of the mitogen‐activated protein kinase Erk2 in mouse trophoblast development , 2003, EMBO reports.

[76]  M. Tremblay,et al.  Mek2 Is Dispensable for Mouse Growth and Development , 2003, Molecular and Cellular Biology.

[77]  M. Barbacid,et al.  RAS oncogenes: the first 30 years , 2003, Nature Reviews Cancer.

[78]  Jing Chen,et al.  Raf-1 promotes cell survival by antagonizing apoptosis signal-regulating kinase 1 through a MEK–ERK independent mechanism , 2001, Proceedings of the National Academy of Sciences of the United States of America.

[79]  E. Wagner,et al.  Embryonic lethality and fetal liver apoptosis in mice lacking the c‐raf‐1 gene , 2001, The EMBO journal.

[80]  C. Pritchard,et al.  MEK kinase activity is not necessary for Raf‐1 function , 2001, The EMBO journal.

[81]  K. Kaibuchi,et al.  Regulation and functions of Rho-associated kinase. , 2000, Experimental cell research.

[82]  T. Wirth,et al.  Raf induces NF-kappaB by membrane shuttle kinase MEKK1, a signaling pathway critical for transformation. , 2000, Proceedings of the National Academy of Sciences of the United States of America.

[83]  U. Rapp,et al.  Overlapping and specific functions of Braf and Craf-1 proto-oncogenes during mouse embryogenesis , 2000, Mechanisms of Development.

[84]  J. Charron,et al.  Embryonic death of Mek1-deficient mice reveals a role for this kinase in angiogenesis in the labyrinthine region of the placenta , 1999, Current Biology.

[85]  S. Chellappan,et al.  Raf-1 Physically Interacts with Rb and Regulates Its Function: a Link between Mitogenic Signaling and Cell Cycle Regulation , 1998, Molecular and Cellular Biology.

[86]  D. Clawson,et al.  Oncogenes, growth factors and phorbol esters regulate Raf-1 through common mechanisms , 1998, Oncogene.

[87]  U. Rapp,et al.  Endothelial apoptosis in Braf-deficient mice , 1997, Nature Genetics.

[88]  John Calvin Reed,et al.  Bcl-2 Targets the Protein Kinase Raf-1 to Mitochondria , 1996, Cell.

[89]  C. Pritchard,et al.  Post-natal lethality and neurological and gastrointestinal defects in mice with targeted disruption of the A-Raf protein kinase gene , 1996, Current Biology.

[90]  J. Sedivy,et al.  Raf-1 protein kinase activates the NF-kappa B transcription factor by dissociating the cytoplasmic NF-kappa B-I kappa B complex. , 1993, Proceedings of the National Academy of Sciences of the United States of America.

[91]  D. Morrison,et al.  Ras-Mediated Activation of the Raf Family Kinases. , 2019, Cold Spring Harbor perspectives in medicine.

[92]  M. Berger,et al.  Abstract B015: An approach to suppress the evolution of resistance in BRAFV600E-mutant cancer , 2018 .

[93]  S. Anand,et al.  A MEK-independent role for CRAF in mitosis and tumor progression , 2011, Nature Medicine.

[94]  W. Kolch,et al.  Tumor and Stem Cell Biology Heterogeneous Nuclear Ribonucleoprotein H Blocks Mst2-mediated Apoptosis in Cancer Cells by Regulating A-raf Transcription , 2022 .