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NATURE, ISSN 0028-0836, 12/2010, Volume 468, Issue 7326, pp. 973 - U377
Activating B-RAF(V600E) (also known as BRAF) kinase mutations occur in similar to 7% of human malignancies and similar to 60% of melanomas(1). Early clinical... 
CELLS | MEK | PLX4032 | PATHWAY | MULTIDISCIPLINARY SCIENCES | KINASE | SENSITIVITY | BRAF | MUTATIONS | CRAF | CANCER
Journal Article
Annals of Pharmacotherapy, ISSN 1060-0280, 11/2011, Volume 45, Issue 11, pp. 1399 - 1405
Journal Article
Tetrahedron Letters, ISSN 0040-4039, 08/2012, Volume 53, Issue 32, pp. 4161 - 4165
Microwave-assisted total syntheses of the highly selective BRAF inhibitors PLX4720 and PLX4032 are reported. In addition to the synthesis of the title... 
BRAF | MAOS | PLX4032 | PLX4720 | Melanoma
Journal Article
Journal of Endocrinological Investigation, ISSN 0391-4097, 12/2013, Volume 36, Issue 11, pp. 1099 - 1104
Journal Article
The New England Journal of Medicine, ISSN 0028-4793, 02/2012, Volume 366, Issue 8, pp. 707 - 714
Journal Article
The New England Journal of Medicine, ISSN 0028-4793, 01/2012, Volume 366, Issue 3, pp. 207 - 215
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
Nature Reviews Clinical Oncology, ISSN 1759-4774, 07/2011, Volume 8, Issue 7, pp. 426 - 433
Journal Article
Journal Article
Cancer Research, ISSN 0008-5472, 04/2011, Volume 71, Issue 7, pp. 2750 - 2760
This study addresses the role of PTEN loss in intrinsic resistance to the BRAF inhibitor PLX4720. Immunohistochemical staining of a tissue array covering all... 
METASTATIC MELANOMA | APOPTOSIS | PROTEIN | ONCOLOGY | PHOSPHORYLATION | CUTANEOUS MELANOMA | RAF KINASE | CANCER | MEDIATES RESISTANCE | LINES | ERK | RNA, Small Interfering - genetics | Up-Regulation | Humans | Drug Resistance, Neoplasm | Phosphatidylinositol 3-Kinases - metabolism | Phosphatidylinositol 3-Kinases - antagonists & inhibitors | Proto-Oncogene Proteins - biosynthesis | Bcl-2-Like Protein 11 | Melanoma - genetics | Apoptosis Regulatory Proteins - genetics | Indoles - pharmacology | Proto-Oncogene Proteins c-akt - metabolism | Proto-Oncogene Proteins B-raf - metabolism | Apoptosis Regulatory Proteins - biosynthesis | Melanoma - metabolism | Proto-Oncogene Proteins - antagonists & inhibitors | PTEN Phosphohydrolase - deficiency | Membrane Proteins - genetics | PTEN Phosphohydrolase - biosynthesis | Proto-Oncogene Proteins - genetics | Melanoma - pathology | Sulfonamides - pharmacology | Proto-Oncogene Proteins B-raf - antagonists & inhibitors | Membrane Proteins - biosynthesis | Membrane Proteins - antagonists & inhibitors | Proto-Oncogene Proteins B-raf - genetics | Melanoma - drug therapy | Apoptosis Regulatory Proteins - antagonists & inhibitors | Cell Line, Tumor | Protein Kinase Inhibitors - pharmacology | Apoptosis - physiology | Mutation | RNA, Small Interfering - administration & dosage | Index Medicus | PTEN | melanoma | BRAF | PLX4032 | therapy | resistance
Journal Article
Pigment Cell & Melanoma Research, ISSN 1755-1471, 05/2014, Volume 27, Issue 3, pp. 495 - 501
The BRAF V600E mutation, which approaches 50% in human melanomas, constitutively activates pERK and contributes to disease progression. The BRAF V600E... 
Cells | Melanoma | Vemurafenib | PLX4032 | cell culture | melanoma | Murine BRafV600E | pERK | B6 syngeneic mouse model
Journal Article
by Wang, J and Chen, JJ and Miller, DD and Li, W
MOLECULAR CANCER THERAPEUTICS, ISSN 1535-7163, 01/2014, Volume 13, Issue 1, pp. 16 - 26
Acquired clinical resistance to vemurafenib, a selective BRAF(V600E) inhibitor, arises frequently after short-term chemotherapy. Because inhibitions of targets... 
BRAF INHIBITION | METASTATIC MELANOMA | ANTIPROLIFERATIVE ACTIVITY | THERAPY | PLX4032 | ONCOLOGY | ANTICANCER AGENTS | POLYMERIZATION | MUTATIONS | ANTITUMOR-ACTIVITY | CANCER
Journal Article
British Journal of Cancer, ISSN 0007-0920, 10/2014, Volume 111, Issue 8, pp. 1625 - 1633
  Melanoma, the most lethal form of skin cancer, is responsible for over 80% of all skin cancer deaths and is highly metastatic, readily spreading to the lymph... 
Molecular Diagnostics | PLX4032 | MMP-1 | vemurafenib | cytokines | tumour microenvironment | chemokines | carcinoma-like associated fibroblasts | stromal fibroblasts
Journal Article