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1. Full Text Non-oxime inhibitors of B-RafV600E kinase
by Ren, Li and Wenglowsky, Steve and Miknis, Greg and Rast, Bryson and Buckmelter, Alex J and Ely, Robert J and Schlachter, Stephen and Laird, Ellen R and Randolph, Nikole and Callejo, Michele and Martinson, Matthew and Galbraith, Sarah and Brandhuber, Barbara J and Vigers, Guy and Morales, Tony and Voegtli, Walter C and Lyssikatos, Joseph
Bioorganic and Medicinal Chemistry Letters, ISSN 0960-894X, 02/2011, Volume 21, Issue 4, pp. 1243 - 1247
The development of inhibitors of B-Raf serine-threonine kinase is described. Various head-groups were examined to optimize inhibitor activity and ADME... 
Furopyridine | Indazole | B-Raf
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2. Full Text RG7204 (PLX4032), a Selective BRAF(V600E) Inhibitor, Displays Potent Antitumor Activity in Preclinical Melanoma Models
by Yang, H and Higgins, B and Kolinsky, K and Packman, K and Go, Z and Iyer, R and Kolis, S and Zhao, S and Lee, R and Grippo, JF and Schostack, K and Simcox, ME and Heimbrook, D and Bollag, G and Su, F
CANCER RESEARCH, ISSN 0008-5472, 07/2010, Volume 70, Issue 13, pp. 5518 - 5527
The BRAF(V600E) mutation is common in several human cancers, especially melanoma. RG7204 (PLX4032) is a small-molecule inhibitor of BRAF(V600E) kinase activity... 
ONCOGENE | EFFICACY | ONCOLOGY | BRAF | B-RAF | MUTATIONS | TUMORS | RAF/MEK/ERK PATHWAY | KINASES
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3. Full Text Inhibition of RAF lsoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers
by Peng, SB and Henry, JR and Kaufman, MD and Lu, WP and Smith, BD and Vogeti, S and Rutkoski, TJ and Wise, S and Chun, L and Zhang, YY and Van Horn, RD and Yin, TG and Zhang, XY and Yadav, V and Chen, SH and Gong, XQ and Ma, XW and Webster, Y and Buchanan, S and Mochalkin, I and Huber, L and Kays, L and Donoho, GP and Walgren, J and McCann, D and Patel, P and Conti, I and Plowman, GD and Starling, JJ and Flynn, DL
CANCER CELL, ISSN 1535-6108, 09/2015, Volume 28, Issue 3, pp. 384 - 398
LY3009120 is a pan-RAF and RAF dimer inhibitor that inhibits all RAF isoforms and occupies both protomers in RAF dinners. Biochemical and cellular analyses... 
ACTIVATION | MELANOMA | MEK INHIBITION | ONCOLOGY | KINASE | C-RAF | IMPROVED SURVIVAL | B-RAF | MAPK PATHWAY | MEDIATES RESISTANCE | VEMURAFENIB | CELL BIOLOGY
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4. Full Text Pyrazolopyridine inhibitors of B-Raf V600E. Part 2: Structure-activity relationships
by Wenglowsky, Steve and Ahrendt, Kateri A and Buckmelter, Alex J and Feng, Bainian and Gloor, Susan L and Gradl, Stefan and Grina, Jonas and Hansen, Joshua D and Laird, Ellen R and Lunghofer, Paul and Mathieu, Simon and Moreno, David and Newhouse, Brad and Ren, Li and Risom, Tyler and Rudolph, Joachim and Seo, Jeongbeob and Sturgis, Hillary L and Voegtli, Walter C and Wen, Zhaoyang
Bioorganic and Medicinal Chemistry Letters, ISSN 0960-894X, 09/2011, Volume 21, Issue 18, pp. 5533 - 5537
Structure-activity relationships around a novel series of B-Raf inhibitors are reported. The enzymatic and cellular potencies of inhibitors derived from two... 
Pyrrolopyridine | Structure-activity relationship | B-Raf | Pyrazolopyridine
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5. Full Text Design and discovery of thioether and nicotinamide containing sorafenib analogues as multikinase inhibitors targeting B-Raf, B-RafV600E and VEGFR-2
by Sun, Shaofeng and He, Zongzhong and He, Zuopeng and Huang, Mindong and Wang, Ningning and Kong, Xiangkai and Yao, Jianwen
Bioorganic & Medicinal Chemistry, ISSN 0968-0896, 05/2018, Volume 26, Issue 9, pp. 2381 - 2391
Thioether and nicotinamide-containing sorafenib analogues with better anti-proliferative and anti-angiogenic activities than sorafenib were well designed and... 
Nicotinamide | B-Raf | Kinase inhibitor | VEGFR-2 | Antitumor
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6. Full Text BRAFE600 in benign and malignant human tumours
by Michaloglou, C and Vredeveld, L.C.W and Mooi, W.J and Peeper, D.S
Oncogene, ISSN 0950-9232, 02/2008, Volume 27, Issue 7, pp. 877 - 895
  Of the RAF family of protein kinases, BRAF is the only member to be frequently activated by mutation in cancer. A single amino acid substitution (V600E)... 
Senescence | BRAF/B-RAF | Naevus/nevus | Melanoma | Cancer | Thyroid | Oncology | Genetics | Mutation | Kinases | Cell cycle | Tumors
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7. Full Text Antitumor Efficacy of the Novel RAF Inhibitor GDC-0879 Is Predicted by BRAF(V600E) Mutational Status and Sustained Extracellular Signal-Regulated Kinase/Mitogen-Activated Protein Kinase Pathway Suppression
by Hoeflich, KP and Herter, S and Tien, J and Wong, L and Berry, L and Chan, J and O'Brien, C and Modrusan, Z and Seshagiri, S and Lackner, M and Stern, H and Choo, E and Murray, L and Friedman, LS and Belvin, M
CANCER RESEARCH, ISSN 0008-5472, 04/2009, Volume 69, Issue 7, pp. 3042 - 3051
Oncogenic activation of the BRAF serine/threonine kinase has been associated with initiation and maintenance of melanoma tumors. As such, development of... 
BRAF GENE | POTENT | MELANOMA | MECHANISM | ONCOLOGY | PHOSPHORYLATION | BENIGN | PATTERNS | B-RAF | TUMORS | HUMAN CANCER
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8. Full Text Dabrafenib and trametinib versus dabrafenib and placebo for Val600 BRAF-mutant melanoma: a multicentre, double-blind, phase 3 randomised controlled trial
by Long, Georgina V, MD and Stroyakovskiy, Daniil, MD and Gogas, Helen, MD and Levchenko, Evgeny, MD and de Braud, Filippo, MD and Larkin, James, FRCP and Garbe, Claus, Prof and Jouary, Thomas, MD and Hauschild, Axel, Prof and Grob, Jean-Jacques, Prof and Chiarion-Sileni, Vanna, MD and Lebbe, Celeste, Prof and Mandalà, Mario, MD and Millward, Michael, Prof and Arance, Ana, MD and Bondarenko, Igor, Prof and Haanen, John B A G, Prof and Hansson, Johan, Prof and Utikal, Jochen, Prof and Ferraresi, Virginia, MD and Kovalenko, Nadezhda, Prof and Mohr, Peter, MD and Probachai, Volodymr, MD and Schadendorf, Dirk, Prof and Nathan, Paul, MD and Robert, Caroline, MD and Ribas, Antoni, Prof and DeMarini, Douglas J, PhD and Irani, Jhangir G, MA and Swann, Suzanne, PhD and Legos, Jeffrey J, PhD and Jin, Fan, MD and Mookerjee, Bijoyesh, MD and Flaherty, Keith, MD
Lancet, The, ISSN 0140-6736, 2015, Volume 386, Issue 9992, pp. 444 - 451
Summary Background Previously, a study of ours showed that the combination of dabrafenib and trametinib improves progression-free survival compared with... 
Internal Medicine | COBIMETINIB | MEDICINE, GENERAL & INTERNAL | MUTATIONS | MEK INHIBITION | CLINICAL-TRIALS | VEMURAFENIB | Double-Blind Method | Humans | Middle Aged | Oximes - administration & dosage | Imidazoles - administration & dosage | Male | Treatment Outcome | Young Adult | Disease-Free Survival | Pyridones - administration & dosage | Proto-Oncogene Proteins B-raf - genetics | Melanoma - drug therapy | Aged, 80 and over | Adult | Female | Aged | Pyrimidinones - administration & dosage | Drug Therapy, Combination | Clinical trials | Medical colleges | Melanoma | Studies | Survival analysis | Chemotherapy | Mutation | Metastasis
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9. Full Text Combined nivolumab and ipilimumab versus ipilimumab alone in patients with advanced melanoma: 2-year overall survival outcomes in a multicentre, randomised, controlled, phase 2 trial
by Hodi, F Stephen, Dr and Chesney, Jason, Prof and Pavlick, Anna C, MD and Robert, Caroline, Prof and Grossmann, Kenneth F, MD and McDermott, David F, MD and Linette, Gerald P, MD and Meyer, Nicolas, Prof and Giguere, Jeffrey K, MD and Agarwala, Sanjiv S, Prof and Shaheen, Montaser, MD and Ernstoff, Marc S, Prof and Minor, David R, MD and Salama, April K, MD and Taylor, Matthew H, MD and Ott, Patrick A, MD and Horak, Christine, PhD and Gagnier, Paul, MD and Jiang, Joel, PhD and Wolchok, Jedd D, Prof and Postow, Michael A, MD
Lancet Oncology, The, ISSN 1470-2045, 2016, Volume 17, Issue 11, pp. 1558 - 1568
Summary Background Results from phase 2 and 3 trials in patients with advanced melanoma have shown significant improvements in the proportion of patients... 
Hematology, Oncology and Palliative Medicine | PEMBROLIZUMAB | ONCOLOGY | PLUS IPILIMUMAB | CHEMOTHERAPY | Double-Blind Method | Humans | Ipilimumab | Antibodies, Monoclonal - adverse effects | Antibodies, Monoclonal - therapeutic use | Antibodies, Monoclonal - administration & dosage | Antineoplastic Combined Chemotherapy Protocols - therapeutic use | Melanoma - genetics | Proto-Oncogene Proteins B-raf - genetics | Melanoma - drug therapy | Nivolumab | Mutation | Melanoma - mortality | Viral antibodies | Medical colleges | Care and treatment | Patient outcomes | Melanoma | Antibodies | Clinical trials | Analysis
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10. Full Text Nivolumab and Ipilimumab versus Ipilimumab in Untreated Melanoma
by Postow, Michael A and Chesney, Jason and Pavlick, Anna C and Robert, Caroline and Grossmann, Kenneth and McDermott, David and Linette, Gerald P and Meyer, Nicolas and Giguere, Jeffrey K and Agarwala, Sanjiv S and Shaheen, Montaser and Ernstoff, Marc S and Minor, David and Salama, April K and Taylor, Matthew and Ott, Patrick A and Rollin, Linda M and Horak, Christine and Gagnier, Paul and Wolchok, Jedd D and Hodi, F. Stephen
The New England Journal of Medicine, ISSN 0028-4793, 05/2015, Volume 372, Issue 21, pp. 2006 - 2017
The combination of a CTLA-4 blocker and a PD-1 blocker produced responses in more than 60% of previously untreated patients with BRAF wild-type advanced... 
DABRAFENIB | SURVIVAL | RESPONSES | MEDICINE, GENERAL & INTERNAL | MEK INHIBITION | SAFETY | ANTI-PD-1 | PD-1 | ASSOCIATION | COMBINED BRAF | VEMURAFENIB | Double-Blind Method | Humans | Ipilimumab | Middle Aged | Antibodies, Monoclonal - adverse effects | Antineoplastic Combined Chemotherapy Protocols - adverse effects | Antibodies, Monoclonal - therapeutic use | Male | Antineoplastic Agents - therapeutic use | Disease-Free Survival | Tumor Burden - drug effects | Antineoplastic Agents - adverse effects | Antineoplastic Combined Chemotherapy Protocols - therapeutic use | Melanoma - genetics | Proto-Oncogene Proteins B-raf - genetics | Melanoma - drug therapy | Nivolumab | Aged, 80 and over | Adult | Female | Aged | Immunomodulation | Medical treatment | Body weight | Melanoma | Lymphocytes T | Metastasis | Cancer therapies | Patients | Immune system | Tumors | Metastases | Index Medicus | Abridged Index Medicus
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11. Full Text BRAF(V600E): Implications for Carcinogenesis and Molecular Therapy
by Cantwell-Dorris, ER and O'Leary, JJ and Sheils, OM
MOLECULAR CANCER THERAPEUTICS, ISSN 1535-7163, 03/2011, Volume 10, Issue 3, pp. 385 - 394
The mitogen-activated protein kinase (MAPK)/extracellular signal-regulated kinase (ERK) pathway is frequently mutated in human cancer. This pathway consists of... 
CPG ISLAND METHYLATION | SERRATED ADENOMAS | ONCOLOGY | BRAF MUTATION | MELANOCORTIN-1 RECEPTOR | NECROSIS-FACTOR-ALPHA | B-RAF | MC1R VARIANTS | RET/PTC REARRANGEMENTS | AZD6244 ARRY-142886 | DEPENDENT ACTIVATION
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12. Full Text Dabrafenib in BRAF -mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trial
by Hauschild, Axel, Prof and Grob, Jean-Jacques, Prof and Demidov, Lev V, Prof and Jouary, Thomas, MD and Gutzmer, Ralf, MD and Millward, Michael, MD and Rutkowski, Piotr, PhD and Blank, Christian U, PhD and Miller, Wilson H, PhD and Kaempgen, Eckhart, PhD and Martín-Algarra, Salvador, PhD and Karaszewska, Boguslawa, MD and Mauch, Cornelia, Prof and Chiarion-Sileni, Vanna, MD and Martin, Anne-Marie, PhD and Swann, Suzanne, PhD and Haney, Patricia, BSN and Mirakhur, Beloo, PhD and Guckert, Mary E, MSN and Goodman, Vicki, MD and Chapman, Paul B, MD
Lancet, The, ISSN 0140-6736, 2012, Volume 380, Issue 9839, pp. 358 - 365
Summary Background Dabrafenib, an inhibitor of mutated BRAF, has clinical activity with a manageable safety profile in studies of phase 1 and 2 in patients... 
Internal Medicine | SURVIVAL | MEDICINE, GENERAL & INTERNAL | INHIBITION | SOLID TUMORS | RESISTANCE | CANCER | VEMURAFENIB | Dacarbazine - therapeutic use | Humans | Middle Aged | Oximes - therapeutic use | Male | Treatment Outcome | Antineoplastic Agents, Alkylating - therapeutic use | Young Adult | Disease-Free Survival | Melanoma - genetics | Melanoma - drug therapy | Aged, 80 and over | Adult | Female | Aged | Imidazoles - therapeutic use | Mutation | Proto-Oncogene Proteins B-raf | Antimitotic agents | Usage | Patient outcomes | Melanoma | Research | Antineoplastic agents | Drug therapy | Meetings | Human immunodeficiency virus--HIV | Committees | Clinical trials | Acute coronary syndromes | Drug dosages
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13. Full Text A Landscape of Driver Mutations in Melanoma
by Hodis, Eran and Watson, Ian R and Kryukov, Gregory V and Arold, Stefan T and Imielinski, Marcin and Theurillat, Jean-Philippe and Nickerson, Elizabeth and Auclair, Daniel and Li, Liren and Place, Chelsea and DiCara, Daniel and Ramos, Alex H and Lawrence, Michael S and Cibulskis, Kristian and Sivachenko, Andrey and Voet, Douglas and Saksena, Gordon and Stransky, Nicolas and Onofrio, Robert C and Winckler, Wendy and Ardlie, Kristin and Wagle, Nikhil and Wargo, Jennifer and Chong, Kelly and Morton, Donald L and Stemke-Hale, Katherine and Chen, Guo and Noble, Michael and Meyerson, Matthew and Ladbury, John E and Davies, Michael A and Gershenwald, Jeffrey E and Wagner, Stephan N and Hoon, Dave S.B and Schadendorf, Dirk and Lander, Eric S and Gabriel, Stacey B and Getz, Gad and Garraway, Levi A and Chin, Lynda
Cell, ISSN 0092-8674, 07/2012, Volume 150, Issue 2, pp. 251 - 263
Despite recent insights into melanoma genetics, systematic surveys for driver mutations are challenged by an abundance of passenger mutations caused by... 
CATALOG | RAS | BIOCHEMISTRY & MOLECULAR BIOLOGY | SOMATIC MUTATIONS | HUMAN CANCER | GENOME | DISCOVERY | PROTEIN COMPLEX | AURORA | CELL BIOLOGY | Amino Acid Sequence | Genome-Wide Association Study | Humans | Cells, Cultured | Models, Molecular | Molecular Sequence Data | Melanocytes - metabolism | Exome | Sequence Alignment | Ultraviolet Rays | Mutagenesis | Melanoma - genetics | Proto-Oncogene Proteins B-raf - genetics | rac1 GTP-Binding Protein - genetics | Medical colleges | Gene mutations | Genes | Melanoma | Genetic research | Genetic aspects | Tumor proteins
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