Targeting oncogenic BRAF in human cancer.

PubWeight™: 0.86‹?›

🔗 View Article (PMC 3508196)

Published in Curr Top Microbiol Immunol on January 01, 2012

Authors

Christine A Pratilas1, Feng Xing, David B Solit

Author Affiliations

1: Memorial Sloan-Kettering Cancer Center, New York, NY 10065, USA.

Associated clinical trials:

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

Articles cited by this

Mutations of the BRAF gene in human cancer. Nature (2002) 65.42

Inhibition of mutated, activated BRAF in metastatic melanoma. N Engl J Med (2010) 36.57

BAY 43-9006 exhibits broad spectrum oral antitumor activity and targets the RAF/MEK/ERK pathway and receptor tyrosine kinases involved in tumor progression and angiogenesis. Cancer Res (2004) 21.36

Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAF. Cell (2004) 19.51

Melanomas acquire resistance to B-RAF(V600E) inhibition by RTK or N-RAS upregulation. Nature (2010) 18.69

Kinase-dead BRAF and oncogenic RAS cooperate to drive tumor progression through CRAF. Cell (2010) 17.48

Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity. Proc Natl Acad Sci U S A (2008) 17.41

RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF. Nature (2010) 17.31

BRAF mutation predicts sensitivity to MEK inhibition. Nature (2005) 17.14

BRAFE600-associated senescence-like cell cycle arrest of human naevi. Nature (2005) 16.87

Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma. Nature (2010) 16.12

RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth. Nature (2010) 15.63

Integrative genomic analyses identify MITF as a lineage survival oncogene amplified in malignant melanoma. Nature (2005) 15.28

COT drives resistance to RAF inhibition through MAP kinase pathway reactivation. Nature (2010) 14.62

PD 098059 is a specific inhibitor of the activation of mitogen-activated protein kinase kinase in vitro and in vivo. J Biol Chem (1995) 14.14

Acquired resistance to BRAF inhibitors mediated by a RAF kinase switch in melanoma can be overcome by cotargeting MEK and IGF-1R/PI3K. Cancer Cell (2010) 12.50

Inhibition of mTORC1 leads to MAPK pathway activation through a PI3K-dependent feedback loop in human cancer. J Clin Invest (2008) 10.74

High frequency of BRAF mutations in nevi. Nat Genet (2002) 9.95

RAS oncogenes: the first 30 years. Nat Rev Cancer (2003) 8.61

BRAF and RAS mutations in human lung cancer and melanoma. Cancer Res (2002) 8.55

Blockade of the MAP kinase pathway suppresses growth of colon tumors in vivo. Nat Med (1999) 7.97

Braf(V600E) cooperates with Pten loss to induce metastatic melanoma. Nat Genet (2009) 7.81

Oncogenic BRAF induces senescence and apoptosis through pathways mediated by the secreted protein IGFBP7. Cell (2008) 6.84

(V600E)BRAF is associated with disabled feedback inhibition of RAF-MEK signaling and elevated transcriptional output of the pathway. Proc Natl Acad Sci U S A (2009) 6.78

Multicenter phase II study of the oral MEK inhibitor, CI-1040, in patients with advanced non-small-cell lung, breast, colon, and pancreatic cancer. J Clin Oncol (2004) 6.61

The RAF inhibitor PLX4032 inhibits ERK signaling and tumor cell proliferation in a V600E BRAF-selective manner. Proc Natl Acad Sci U S A (2010) 6.54

Results of a phase III, randomized, placebo-controlled study of sorafenib in combination with carboplatin and paclitaxel as second-line treatment in patients with unresectable stage III or stage IV melanoma. J Clin Oncol (2009) 6.44

Complexes of Ras.GTP with Raf-1 and mitogen-activated protein kinase kinase. Science (1993) 6.07

Targeting the mitogen-activated protein kinase cascade to treat cancer. Nat Rev Cancer (2004) 6.07

Elevated CRAF as a potential mechanism of acquired resistance to BRAF inhibition in melanoma. Cancer Res (2008) 6.05

Regulation of Raf-1 by direct feedback phosphorylation. Mol Cell (2005) 5.88

Phosphorylation and regulation of Raf by Akt (protein kinase B). Science (1999) 5.61

Transforming genes of human bladder and lung carcinoma cell lines are homologous to the ras genes of Harvey and Kirsten sarcoma viruses. Proc Natl Acad Sci U S A (1982) 5.39

Tumorigenic transformation of mammalian cells induced by a normal human gene homologous to the oncogene of Harvey murine sarcoma virus. Nature (1982) 5.08

A new mouse model to explore the initiation, progression, and therapy of BRAFV600E-induced lung tumors. Genes Dev (2007) 5.07

Sorafenib in advanced melanoma: a Phase II randomised discontinuation trial analysis. Br J Cancer (2006) 4.93

V599EB-RAF is an oncogene in melanocytes. Cancer Res (2004) 4.49

Structures of human MAP kinase kinase 1 (MEK1) and MEK2 describe novel noncompetitive kinase inhibition. Nat Struct Mol Biol (2004) 4.40

Suppression of BRAF(V599E) in human melanoma abrogates transformation. Cancer Res (2003) 4.28

BRAF mutations are sufficient to promote nevi formation and cooperate with p53 in the genesis of melanoma. Curr Biol (2005) 3.68

Modulation of signalling by Sprouty: a developing story. Nat Rev Mol Cell Biol (2004) 3.46

GSK1120212 (JTP-74057) is an inhibitor of MEK activity and activation with favorable pharmacokinetic properties for sustained in vivo pathway inhibition. Clin Cancer Res (2011) 3.36

Sprouty1 and Sprouty2 provide a control mechanism for the Ras/MAPK signalling pathway. Nat Cell Biol (2002) 3.35

The complexity of Raf-1 regulation. Curr Opin Cell Biol (1997) 3.25

Cellular senescence in naevi and immortalisation in melanoma: a role for p16? Br J Cancer (2006) 3.23

Three human transforming genes are related to the viral ras oncogenes. Proc Natl Acad Sci U S A (1983) 3.06

Oncogenic BRAF is required for tumor growth and maintenance in melanoma models. Cancer Res (2006) 2.84

Mammalian Sprouty4 suppresses Ras-independent ERK activation by binding to Raf1. Nat Cell Biol (2003) 2.71

Analysis of BRAF and N-RAS mutations in metastatic melanoma tissues. Cancer Res (2003) 2.62

Unlocking the code of 14-3-3. J Cell Sci (2004) 2.58

KSR modulates signal propagation within the MAPK cascade. Genes Dev (1996) 2.46

Phase I and pharmacodynamic study of the oral MEK inhibitor CI-1040 in patients with advanced malignancies. J Clin Oncol (2005) 2.32

Renewing the conspiracy theory debate: does Raf function alone to mediate Ras oncogenesis? Trends Cell Biol (2004) 2.32

Clinical experience of MEK inhibitors in cancer therapy. Biochim Biophys Acta (2006) 2.28

BRAF V600E disrupts AZD6244-induced abrogation of negative feedback pathways between extracellular signal-regulated kinase and Raf proteins. Cancer Res (2008) 2.03

A phase I trial of the oral, multikinase inhibitor sorafenib in combination with carboplatin and paclitaxel. Clin Cancer Res (2008) 1.99

Ras regulates assembly of mitogenic signalling complexes through the effector protein IMP. Nature (2004) 1.87

A proline-rich sequence unique to MEK1 and MEK2 is required for raf binding and regulates MEK function. Mol Cell Biol (1995) 1.82

Positive and negative regulation of Raf kinase activity and function by phosphorylation. EMBO J (2001) 1.81

Pharmacodynamic and toxicokinetic evaluation of the novel MEK inhibitor, PD0325901, in the rat following oral and intravenous administration. Cancer Chemother Pharmacol (2006) 1.71

Potential tumor suppressive pathway involving DUSP6/MKP-3 in pancreatic cancer. Am J Pathol (2003) 1.70

14-3-3: modulators of signaling proteins? Science (1994) 1.60

Human melanocyte senescence and melanoma susceptibility genes. Oncogene (2003) 1.56

The ras/mitogen-activated protein kinase pathway inhibitor and likely tumor suppressor proteins, sprouty 1 and sprouty 2 are deregulated in breast cancer. Cancer Res (2004) 1.54

Down-regulation of Sprouty2 in non-small cell lung cancer contributes to tumor malignancy via extracellular signal-regulated kinase pathway-dependent and -independent mechanisms. Mol Cancer Res (2007) 1.52

Sprouty 2, an inhibitor of mitogen-activated protein kinase signaling, is down-regulated in hepatocellular carcinoma. Cancer Res (2006) 1.52

SPRY2 is an inhibitor of the ras/extracellular signal-regulated kinase pathway in melanocytes and melanoma cells with wild-type BRAF but not with the V599E mutant. Cancer Res (2004) 1.51

Sprouty2 inhibits the Ras/MAP kinase pathway by inhibiting the activation of Raf. J Biol Chem (2001) 1.46

Integration of genomic analysis and in vivo transfection to identify sprouty 2 as a candidate tumor suppressor in liver cancer. Hepatology (2008) 1.35

Distinct progression pathways involving the dysfunction of DUSP6/MKP-3 in pancreatic intraepithelial neoplasia and intraductal papillary-mucinous neoplasms of the pancreas. Mod Pathol (2005) 1.17

p16/cyclin-dependent kinase inhibitor 2A deficiency in human melanocyte senescence, apoptosis, and immortalization: possible implications for melanoma progression. J Natl Cancer Inst (2003) 1.16

Sprouty2 association with B-Raf is regulated by phosphorylation and kinase conformation. Cancer Res (2009) 1.05

3'-deoxy-3'-[18F]fluorothymidine positron emission tomography is a sensitive method for imaging the response of BRAF-dependent tumors to MEK inhibition. Cancer Res (2007) 1.04

Exploration of genetic alterations in human endometrial cancer and melanoma: distinct tumorigenic pathways that share a frequent abnormal PI3K/AKT cascade. Oncol Rep (2005) 0.86

Articles by these authors

RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E). Nature (2011) 10.77

Tumour micro-environment elicits innate resistance to RAF inhibitors through HGF secretion. Nature (2012) 10.39

(V600E)BRAF is associated with disabled feedback inhibition of RAF-MEK signaling and elevated transcriptional output of the pathway. Proc Natl Acad Sci U S A (2009) 6.78

Genome sequencing identifies a basis for everolimus sensitivity. Science (2012) 6.71

The RAF inhibitor PLX4032 inhibits ERK signaling and tumor cell proliferation in a V600E BRAF-selective manner. Proc Natl Acad Sci U S A (2010) 6.54

The BAD protein integrates survival signaling by EGFR/MAPK and PI3K/Akt kinase pathways in PTEN-deficient tumor cells. Cancer Cell (2005) 4.48

4E-BP1 is a key effector of the oncogenic activation of the AKT and ERK signaling pathways that integrates their function in tumors. Cancer Cell (2010) 4.48

Akt forms an intracellular complex with heat shock protein 90 (Hsp90) and Cdc37 and is destabilized by inhibitors of Hsp90 function. J Biol Chem (2002) 3.70

Transcriptional pathway signatures predict MEK addiction and response to selumetinib (AZD6244). Cancer Res (2010) 3.54

Genomic and biological characterization of exon 4 KRAS mutations in human cancer. Cancer Res (2010) 3.24

Tumor adaptation and resistance to RAF inhibitors. Nat Med (2013) 3.11

The draft genome of sweet orange (Citrus sinensis). Nat Genet (2012) 2.81

Combination of trastuzumab and tanespimycin (17-AAG, KOS-953) is safe and active in trastuzumab-refractory HER-2 overexpressing breast cancer: a phase I dose-escalation study. J Clin Oncol (2007) 2.80

Comparative genomic analysis of primary versus metastatic colorectal carcinomas. J Clin Oncol (2012) 2.74

Genetic predictors of MEK dependence in non-small cell lung cancer. Cancer Res (2008) 2.71

Imaging the pharmacodynamics of HER2 degradation in response to Hsp90 inhibitors. Nat Biotechnol (2004) 2.66

Somatic mutations of the Parkinson's disease-associated gene PARK2 in glioblastoma and other human malignancies. Nat Genet (2009) 2.51

BRAF(L597) mutations in melanoma are associated with sensitivity to MEK inhibitors. Cancer Discov (2012) 2.48

Ansamycin antibiotics inhibit Akt activation and cyclin D expression in breast cancer cells that overexpress HER2. Oncogene (2002) 2.34

Progression of RAS-mutant leukemia during RAF inhibitor treatment. N Engl J Med (2012) 2.19

Development of new mouse lung tumor models expressing EGFR T790M mutants associated with clinical resistance to kinase inhibitors. PLoS One (2007) 2.14

The tyrosine phosphatase PTPRD is a tumor suppressor that is frequently inactivated and mutated in glioblastoma and other human cancers. Proc Natl Acad Sci U S A (2009) 2.09

Prevalence and co-occurrence of actionable genomic alterations in high-grade bladder cancer. J Clin Oncol (2013) 1.92

Targeting the mitogen-activated protein kinase pathway: physiological feedback and drug response. Clin Cancer Res (2010) 1.77

PIK3CA mutation uncouples tumor growth and cyclin D1 regulation from MEK/ERK and mutant KRAS signaling. Cancer Res (2010) 1.77

Comparative sequencing analysis reveals high genomic concordance between matched primary and metastatic colorectal cancer lesions. Genome Biol (2014) 1.76

Therapeutic strategies for inhibiting oncogenic BRAF signaling. Curr Opin Pharmacol (2008) 1.75

Inhibition of Hsp90 down-regulates mutant epidermal growth factor receptor (EGFR) expression and sensitizes EGFR mutant tumors to paclitaxel. Cancer Res (2008) 1.74

The current state of preclinical prostate cancer animal models. Prostate (2008) 1.68

SNX2112, a synthetic heat shock protein 90 inhibitor, has potent antitumor activity against HER kinase-dependent cancers. Clin Cancer Res (2008) 1.66

Resistance to MEK inhibitors: should we co-target upstream? Sci Signal (2011) 1.66

Loss of NF1 in cutaneous melanoma is associated with RAS activation and MEK dependence. Cancer Res (2014) 1.55

Association with HSP90 inhibits Cbl-mediated down-regulation of mutant epidermal growth factor receptors. Cancer Res (2006) 1.54

HER kinase activation confers resistance to MET tyrosine kinase inhibition in MET oncogene-addicted gastric cancer cells. Mol Cancer Ther (2008) 1.52

Genomic complexity and AKT dependence in serous ovarian cancer. Cancer Discov (2012) 1.50

Randomized, phase II study of the insulin-like growth factor-1 receptor inhibitor IMC-A12, with or without cetuximab, in patients with cetuximab- or panitumumab-refractory metastatic colorectal cancer. J Clin Oncol (2010) 1.38

Phase II trial of MEK inhibitor selumetinib (AZD6244, ARRY-142886) in patients with BRAFV600E/K-mutated melanoma. Clin Cancer Res (2013) 1.34

Peptide-conjugated antisense oligonucleotides for targeted inhibition of a transcriptional regulator in vivo. Nat Biotechnol (2008) 1.33

BRAF mutation predicts for poor outcomes after metastasectomy in patients with metastatic colorectal cancer. Cancer (2014) 1.32

Targeting HER2 in prostate cancer: where to next? J Clin Oncol (2007) 1.29

Biochemical genomics approach to map activities to genes. Methods Enzymol (2002) 1.26

Efficacy of intermittent combined RAF and MEK inhibition in a patient with concurrent BRAF- and NRAS-mutant malignancies. Cancer Discov (2014) 1.25

KRAS and BRAF: drug targets and predictive biomarkers. J Pathol (2010) 1.23

Mapping the molecular determinants of BRAF oncogene dependence in human lung cancer. Proc Natl Acad Sci U S A (2014) 1.15

A phase 2 study of the insulin-like growth factor-1 receptor inhibitor MK-0646 in patients with metastatic, well-differentiated neuroendocrine tumors. Cancer (2012) 1.13

Phase II study of everolimus in metastatic urothelial cancer. BJU Int (2013) 1.07

Angiogenesis impairment in Id-deficient mice cooperates with an Hsp90 inhibitor to completely suppress HER2/neu-dependent breast tumors. Proc Natl Acad Sci U S A (2003) 1.07

A phase I trial of intermittent high-dose gefitinib and fixed-dose docetaxel in patients with advanced solid tumors. Cancer Chemother Pharmacol (2006) 1.05

Somatic mutation of fibroblast growth factor receptor-3 (FGFR3) defines a distinct morphological subtype of high-grade urothelial carcinoma. J Pathol (2011) 1.05

Therapeutic strategies for targeting BRAF in human cancer. Rev Recent Clin Trials (2007) 1.04

The promoter of miR-663 is hypermethylated in Chinese pediatric acute myeloid leukemia (AML). BMC Med Genet (2013) 1.03

The "SWOT" of BRAF inhibition in melanoma: RAF inhibitors, MEK inhibitors or both? Curr Oncol Rep (2011) 1.03

Induction of cutaneous squamous cell carcinomas by RAF inhibitors: cause for concern? J Clin Oncol (2011) 1.03

RAS mutations affect pattern of metastatic spread and increase propensity for brain metastasis in colorectal cancer. Cancer (2014) 1.03

Combination treatment with 17-N-allylamino-17-demethoxy geldanamycin and acute irradiation produces supra-additive growth suppression in human prostate carcinoma spheroids. Cancer Res (2003) 1.02

A role for Id proteins in mammary gland physiology and tumorigenesis. Adv Cancer Res (2004) 0.97

Mutant N-RAS protects colorectal cancer cells from stress-induced apoptosis and contributes to cancer development and progression. Cancer Discov (2012) 0.96

Randomized phase II study of pulse erlotinib before or after carboplatin and paclitaxel in current or former smokers with advanced non-small-cell lung cancer. J Clin Oncol (2008) 0.93

Activation of phosphorylating-p38 mitogen-activated protein kinase and its relationship with localization of intestinal stem cells in rats after ischemia-reperfusion injury. World J Gastroenterol (2003) 0.93

Total synthesis as a resource in the discovery of potentially valuable antitumor agents: cycloproparadicicol. Angew Chem Int Ed Engl (2003) 0.92

Generation of DOTA-conjugated antibody fragments for radioimmunoimaging. Methods Enzymol (2004) 0.91

Analyzing the gene expression profile of pediatric acute myeloid leukemia with real-time PCR arrays. Cancer Cell Int (2012) 0.90

Oncogenic activation of Pak1-dependent pathway of macropinocytosis determines BCG entry into bladder cancer cells. Cancer Res (2013) 0.90

A phase I trial of docetaxel and pulse-dose 17-allylamino-17-demethoxygeldanamycin in adult patients with solid tumors. Cancer Chemother Pharmacol (2011) 0.89

Antitumor activity of SNX-2112, a synthetic heat shock protein-90 inhibitor, in MET-amplified tumor cells with or without resistance to selective MET Inhibition. Clin Cancer Res (2011) 0.88

RAF/MEK dependence of KRAS-mutant pancreatic ductal adenocarcinomas. Cancer Discov (2012) 0.87

Will Hsp90 inhibitors prove effective in BRAF-mutant melanomas? Clin Cancer Res (2012) 0.85

ERK pathway inhibitors: how low should we go? Cancer Discov (2013) 0.85

Evaluation of plasma insulin-like growth factor binding protein 2 and Her-2 extracellular domain as biomarkers for 17-allylamino-17-demethoxygeldanamycin treatment of adult patients with advanced solid tumors. Clin Cancer Res (2007) 0.84

Different expression patterns of PRRSV mediator genes in the lung tissues of PRRSV resistant and susceptible pigs. Dev Comp Immunol (2012) 0.83

Application of a single-objective, hybrid genetic algorithm approach to pharmacokinetic model building. J Pharmacokinet Pharmacodyn (2012) 0.80

Genome-wide characterization and expression analysis of genetic variants in sweet orange. Plant J (2013) 0.80

Translational medicine: Primed for resistance. Nature (2012) 0.79

Single-crystal AlN nanonecklaces. Nanotechnology (2008) 0.79

Inhibition of the ecto-beta subunit of F1F0-ATPase inhibits proliferation and induces apoptosis in acute myeloid leukemia cell lines. J Exp Clin Cancer Res (2012) 0.79

Monitoring the induction of heat shock factor 1/heat shock protein 70 expression following 17-allylamino-demethoxygeldanamycin treatment by positron emission tomography and optical reporter gene imaging. Mol Imaging (2012) 0.78

Clinical significance of Sam68 expression in endometrial carcinoma. Tumour Biol (2015) 0.78

Identification of a novel nurr1-interacting protein. J Neurosci (2008) 0.77

A highly sensitive and robust UPLC-MS with electrospray ionization method for quantitation of taxifolin in rat plasma. J Chromatogr B Analyt Technol Biomed Life Sci (2009) 0.76

Lung cancer profiling: Genetic and molecular predictors of MEK-dependence. Cancer Biol Ther (2009) 0.75

Population pharmacokinetic analysis of 17-dimethylaminoethylamino-17-demethoxygeldanamycin (17-DMAG) in adult patients with solid tumors. Cancer Chemother Pharmacol (2012) 0.75

Effect of Salvia miltiorrhiza on retinopathy. Asian Pac J Trop Med (2013) 0.75

12th Annual meeting of the Society of Urologic Oncology (SUO) bladder cancer sessions I and II summary report. Urol Oncol (2012) 0.75

Erratum: Mutational landscape of metastatic cancer revealed from prospective clinical sequencing of 10,000 patients. Nat Med (2017) 0.75

[Performance of FibroScan in evaluating the curative effects of traditional Chinese medicine on liver fibrosis]. Zhonghua Gan Zang Bing Za Zhi (2014) 0.75