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Nature, ISSN 0028-0836, 12/2010, Volume 468, Issue 7326, pp. 973 - 977
Journal Article
Nature, ISSN 0028-0836, 12/2011, Volume 480, Issue 7377, pp. 387 - 390
Journal Article
Nature, ISSN 0028-0836, 09/2010, Volume 467, Issue 7315, pp. 596 - 599
B-RAF is the most frequently mutated protein kinase in human cancers. The finding that oncogenic mutations in BRAF are common in melanoma, followed by the... 
ACTIVATION | PATHWAY | MULTIDISCIPLINARY SCIENCES | MUTATION | KERATOACANTHOMAS | SENSITIVITY | SENESCENCE | SORAFENIB | HUMAN CANCER | PROGRESSION | BRAF(V600E) | Humans | Extracellular Signal-Regulated MAP Kinases - antagonists & inhibitors | Macaca fascicularis | Melanoma - enzymology | Substrate Specificity | Positron-Emission Tomography | Extracellular Signal-Regulated MAP Kinases - metabolism | Indoles - administration & dosage | Neoplasm Metastasis | Melanoma - genetics | Phosphorylation - drug effects | Mutant Proteins - antagonists & inhibitors | Proto-Oncogene Proteins B-raf - metabolism | Proto-Oncogene Proteins B-raf - chemistry | Sulfonamides - chemistry | Mutant Proteins - genetics | Models, Molecular | Rats | Mutant Proteins - metabolism | Melanoma - pathology | Mutation - genetics | Proto-Oncogene Proteins B-raf - antagonists & inhibitors | Xenograft Model Antitumor Assays | Animals | Indoles - adverse effects | MAP Kinase Signaling System - drug effects | Sulfonamides - therapeutic use | Proto-Oncogene Proteins B-raf - genetics | Melanoma - drug therapy | Mutant Proteins - chemistry | Alleles | Dogs | Sulfonamides - adverse effects | Indoles - therapeutic use | Indoles - chemistry | Sulfonamides - administration & dosage | Control | Gene mutations | Melanoma | Development and progression | Genetic aspects | Research | Health aspects | Protein kinases | Cancer | Proteins | Mutation | Kinases | Rodents | Index Medicus | targeted therapy | melanoma | BRAF | PLX4032 | biomarker | oncogene
Journal Article
Journal of the American Chemical Society, ISSN 0002-7863, 12/2013, Volume 135, Issue 51, pp. 19319 - 19329
Journal Article
Cell, ISSN 0092-8674, 04/2016, Volume 165, Issue 3, pp. 643 - 655
Oncogenic activation of genes via point mutations occurs in 20%–30% of human cancers. The development of effective RAS inhibitors has been challenging,... 
rigosertib | RAS-binding domain | PI3K | MAPK | RAS | RAF | POINT MUTATIONS | BLADDER-CARCINOMA ONCOGENE | MUTANT | SELECTIVE INHIBITOR | ACTIVATION | PHOSPHORYLATION | BIOCHEMISTRY & MOLECULAR BIOLOGY | IN-VIVO | KINASE | BINDING | TRANSFORMING PROPERTIES | CELL BIOLOGY | Glycine - analogs & derivatives | Phosphorylation | Humans | Molecular Sequence Data | ras Proteins - metabolism | Crystallography, X-Ray | Proto-Oncogene Proteins - chemistry | Sulfones - pharmacology | MAP Kinase Signaling System | Cell Cycle Proteins - chemistry | Pancreatic Neoplasms - drug therapy | Glycine - chemistry | Sulfones - chemistry | Nuclear Magnetic Resonance, Biomolecular | Dimerization | Glycine - administration & dosage | Protein-Serine-Threonine Kinases - metabolism | Proto-Oncogene Proteins B-raf - metabolism | Proto-Oncogene Proteins B-raf - chemistry | Proto-Oncogene Proteins - metabolism | Amino Acid Sequence | RNA-Binding Proteins - chemistry | Cell Cycle Proteins - metabolism | Models, Molecular | Sequence Alignment | Animals | Glycine - pharmacology | Signal Transduction - drug effects | Mice, Nude | Mice | Protein-Serine-Threonine Kinases - chemistry | Cell Transformation, Neoplastic - drug effects | RNA-Binding Proteins - metabolism | Sulfones - administration & dosage | Proteins | Medical colleges | Gene mutations | Protein binding | Jewish schools | Phosphotransferases | Index Medicus
Journal Article
CANCER DISCOVERY, ISSN 2159-8274, 04/2018, Volume 8, Issue 4, pp. 385 - 385
KSR-MEK complexes allosterically activate BRAF, which then phosphorylates a second MEK molecule. 
ONCOLOGY | Proto-Oncogene Proteins B-raf - chemistry
Journal Article
Journal of Medicinal Chemistry, ISSN 0022-2623, 10/2009, Volume 52, Issue 20, pp. 6189 - 6192
Journal Article
Nature, ISSN 0028-0836, 03/2010, Volume 464, Issue 7287, pp. 427 - 430
Tumours with mutant BRAF are dependent on the RAF–MEK–ERK signalling pathway for their growth. We found that ATP-competitive RAF inhibitors inhibit ERK... 
SELECTIVE INHIBITOR | ACTIVATION | MELANOMA | MECHANISM | MULTIDISCIPLINARY SCIENCES | SENSITIVITY | HETERODIMERIZATION | KINASE INHIBITOR | B-RAF | CRAF | ONCOGENIC BRAF | Neoplasms - metabolism | ras Proteins - genetics | Phosphorylation | raf Kinases - antagonists & inhibitors | Humans | Protein Multimerization | Transcriptional Activation - drug effects | ras Proteins - metabolism | Extracellular Signal-Regulated MAP Kinases - metabolism | raf Kinases - metabolism | Mitogen-Activated Protein Kinase Kinases - metabolism | Neoplasms - genetics | Adenosine Triphosphate - metabolism | Indoles - pharmacology | raf Kinases - genetics | Proto-Oncogene Proteins B-raf - metabolism | Proto-Oncogene Proteins B-raf - chemistry | Cell Line | raf Kinases - chemistry | Catalytic Domain | Neoplasms - enzymology | Enzyme Activation - drug effects | Sulfonamides - pharmacology | Neoplasms - drug therapy | Proto-Oncogene Proteins B-raf - antagonists & inhibitors | Animals | MAP Kinase Signaling System - drug effects | Models, Biological | Protein Kinase Inhibitors - therapeutic use | Proto-Oncogene Proteins B-raf - genetics | Cell Line, Tumor | Protein Binding | Mice | Protein Kinase Inhibitors - pharmacology | Protein Kinase Inhibitors - metabolism | Care and treatment | Enzyme inhibitors | Gene mutations | Cellular signal transduction | Genetic aspects | Research | Health aspects | Cancer | Proteins | Competition | Drugs | Mutation | Kinases | Tumors | Index Medicus
Journal Article
Nature, ISSN 0028-0836, 03/2010, Volume 464, Issue 7287, pp. 431 - 435
Activating mutations in KRAS and BRAF are found in more than 30% of all human tumours and 40% of melanoma, respectively, thus targeting this pathway could have... 
SELECTIVE INHIBITOR | POTENT | EFFICACY | PHOSPHORYLATION | MULTIDISCIPLINARY SCIENCES | IN-VIVO | C-RAF | HETERODIMERIZATION | B-RAF | PROTEIN-KINASE KINASE | CANCER | Neoplasms - metabolism | ras Proteins - genetics | Proto-Oncogene Proteins p21(ras) | Diphenylamine - pharmacology | raf Kinases - antagonists & inhibitors | Humans | Protein Multimerization | ras Proteins - metabolism | Protein Transport - drug effects | Extracellular Signal-Regulated MAP Kinases - metabolism | raf Kinases - metabolism | Diphenylamine - analogs & derivatives | Mitogen-Activated Protein Kinase Kinases - metabolism | Adenosine Triphosphate - metabolism | Indoles - pharmacology | Benzamides - pharmacology | Cell Membrane - metabolism | raf Kinases - genetics | Cell Membrane - drug effects | Proto-Oncogene Proteins B-raf - metabolism | Proto-Oncogene Proteins B-raf - chemistry | Pyrazoles - pharmacology | Protein Structure, Tertiary | Proto-Oncogene Proteins - metabolism | Cell Line | Indenes - pharmacology | raf Kinases - chemistry | Proto-Oncogene Proteins c-raf - genetics | Mitogen-Activated Protein Kinase Kinases - antagonists & inhibitors | Neoplasms - enzymology | Proto-Oncogene Proteins - genetics | Enzyme Activation - drug effects | Sulfonamides - pharmacology | Proto-Oncogene Proteins c-raf - metabolism | Neoplasms - drug therapy | Proto-Oncogene Proteins B-raf - antagonists & inhibitors | Xenograft Model Antitumor Assays | Animals | MAP Kinase Signaling System - drug effects | Protein Kinase Inhibitors - therapeutic use | Proto-Oncogene Proteins B-raf - genetics | Proto-Oncogene Proteins c-raf - deficiency | Cell Proliferation - drug effects | Mice | Protein Kinase Inhibitors - pharmacology | Neoplasms - pathology | Ras genes | Growth | Physiological aspects | Cellular signal transduction | Genetic aspects | Research | Mitogen-activated protein kinases | Competition | Clinical trials | Enzymes | Kinases | Index Medicus | Proteins | Cellular | Inhibitors | Pathways | Tumours | Signalling | Dimerization
Journal Article
Nature, ISSN 0028-0836, 12/2010, Volume 468, Issue 7326, pp. 968 - 972
Oncogenic mutations in the serine/threonine kinase B-RAF (also known as BRAF) are found in 50-70% of malignant melanomas. Pre-clinical studies have... 
TRANSFORMATION | CELLS | TUMOR PROGRESSION | GENE | SIGNALING PATHWAY | MULTIDISCIPLINARY SCIENCES | BRAF | B-RAF | KAPPA-B | MUTATIONS | CANCER | Allosteric Regulation | Humans | Gene Expression Regulation, Neoplastic | Melanoma - enzymology | Gene Expression Profiling | MAP Kinase Signaling System | Mitogen-Activated Protein Kinase Kinases - metabolism | Melanoma - genetics | Indoles - pharmacology | Proto-Oncogene Proteins B-raf - metabolism | Proto-Oncogene Proteins B-raf - chemistry | Melanoma - metabolism | Proto-Oncogene Proteins - metabolism | Gene Library | Proto-Oncogene Proteins c-raf - genetics | MAP Kinase Kinase Kinases - genetics | Mitogen-Activated Protein Kinase Kinases - antagonists & inhibitors | Proto-Oncogene Proteins - genetics | Clinical Trials as Topic | MAP Kinase Kinase Kinases - metabolism | Enzyme Activation - drug effects | Open Reading Frames - genetics | Sulfonamides - pharmacology | Proto-Oncogene Proteins c-raf - metabolism | Proto-Oncogene Proteins B-raf - antagonists & inhibitors | Drug Resistance, Neoplasm - genetics | Sulfonamides - therapeutic use | Protein Kinase Inhibitors - therapeutic use | Proto-Oncogene Proteins B-raf - genetics | Melanoma - drug therapy | Cell Line, Tumor | Indoles - therapeutic use | Protein Kinase Inhibitors - pharmacology | Drug Resistance, Neoplasm - drug effects | Mitogen-Activated Protein Kinases - metabolism | Protein research | Research | Properties | Protein kinases | Cancer cells | Cell lines | Biochemistry | Mutation | Kinases | Genes | Cancer | Index Medicus
Journal Article