Vemurafenib: the first drug approved for BRAF-mutant cancer.

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Published in Nat Rev Drug Discov on October 12, 2012

Authors

Gideon Bollag1, James Tsai, Jiazhong Zhang, Chao Zhang, Prabha Ibrahim, Keith Nolop, Peter Hirth

Author Affiliations

1: Plexxikon, 91 Bolivar Drive, Berkeley, California 94710, USA. gbollag@plexxikon.com

Associated clinical trials:

A Study of Vemurafenib (RO5185426) in Comparison With Dacarbazine in Previously Untreated Patients With Metastatic Melanoma (BRIM 3) | NCT01006980

Ph I Ipilimumab Vemurafenib Combo in Patients With v-Raf Murine Sarcoma Viral Oncogene Homolog B1 (BRAF) | NCT01400451

A Study of Vemurafenib in Previously Treated Patients With Metastatic Melanoma | NCT00949702

Safety Study of PLX4032 in Patients With Solid Tumors | NCT00405587

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Suppression of p53-dependent senescence by the JNK signal transduction pathway. Proc Natl Acad Sci U S A (2007) 1.67

The crystal structures of human steroidogenic factor-1 and liver receptor homologue-1. Proc Natl Acad Sci U S A (2005) 1.67

TFIIH and P-TEFb coordinate transcription with capping enzyme recruitment at specific genes in fission yeast. Mol Cell (2009) 1.66

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A glutamine switch mechanism for nucleotide selectivity by phosphodiesterases. Mol Cell (2004) 1.64

Global mapping of the protein structure space and application in structure-based inference of protein function. Proc Natl Acad Sci U S A (2005) 1.59

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Trends in in-hospital deaths among hospitalizations with pulmonary embolism. Arch Intern Med (2012) 1.53

Chemical genetic inhibition of Mps1 in stable human cell lines reveals novel aspects of Mps1 function in mitosis. PLoS One (2010) 1.50

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Pharmacodynamic characterization of the efficacy signals due to selective BRAF inhibition with PLX4032 in malignant melanoma. Neoplasia (2010) 1.48

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Protein kinase C epsilon regulates gamma-aminobutyrate type A receptor sensitivity to ethanol and benzodiazepines through phosphorylation of gamma2 subunits. J Biol Chem (2007) 1.43

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Human Ago2 is required for efficient microRNA 122 regulation of hepatitis C virus RNA accumulation and translation. J Virol (2010) 1.42

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The effect of poloxamer 188 on nanoparticle morphology, size, cancer cell uptake, and cytotoxicity. Nanomedicine (2009) 1.32

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Dynamic phosphoregulation of the cortical actin cytoskeleton and endocytic machinery revealed by real-time chemical genetic analysis. J Cell Biol (2003) 1.27

Internal fixation of distal tibiofibular syndesmotic injuries: a systematic review with meta-analysis. Int Orthop (2013) 1.23

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Switching Cdk2 on or off with small molecules to reveal requirements in human cell proliferation. Mol Cell (2011) 1.21

Optimizing small molecule inhibitors of calcium-dependent protein kinase 1 to prevent infection by Toxoplasma gondii. J Med Chem (2013) 1.19

Tissue-specific PKA inhibition using a chemical genetic approach and its application to studies on sperm capacitation. Proc Natl Acad Sci U S A (2008) 1.18

Structural characterization of autoinhibited c-Met kinase produced by coexpression in bacteria with phosphatase. Proc Natl Acad Sci U S A (2006) 1.18

Inhibition of ZAP-70 kinase activity via an analog-sensitive allele blocks T cell receptor and CD28 superagonist signaling. J Biol Chem (2008) 1.15