Vemurafenib: the first drug approved for BRAF-mutant cancer

Pharmacodynamic Characterization of the Efficacy Signals Due to Selective BRAF Inhibition with PLX4032 in Malignant Melanoma

(2015) William D. Tap et al.   NEOPLASIA

RAF265 Inhibits the Growth of Advanced Human Melanoma Tumors

(2012) Y. Su et al.   CLINICAL CANCER RESEARCH

Analytical Performance of a Real-time PCR-based Assay for V600 Mutations in the BRAF Gene, Used as the Companion Diagnostic Test for the Novel BRAF Inhibitor Vemurafenib in Metastatic Melanoma

(2012) Harkanwal Halait et al.   DIAGNOSTIC MOLECULAR PATHOLOGY

Marked, Homogeneous, and Early [18F]Fluorodeoxyglucose–Positron Emission Tomography Responses to Vemurafenib in BRAF-Mutant Advanced Melanoma

(2012) Grant A. McArthur et al.   JOURNAL OF CLINICAL ONCOLOGY

A Patient With BRAF V600E Lung Adenocarcinoma Responding to Vemurafenib

(2012) Oliver Gautschi et al.   Journal of Thoracic Oncology

Dabrafenib in patients with melanoma, untreated brain metastases, and other solid tumours: a phase 1 dose-escalation trial

(2012) Gerald S Falchook et al.   LANCET

Dabrafenib in BRAF-mutated metastatic melanoma: a multicentre, open-label, phase 3 randomised controlled trial

(2012) Axel Hauschild et al.   LANCET

CEP-32496: A Novel Orally Active BRAFV600E Inhibitor with Selective Cellular and In Vivo Antitumor Activity

(2012) J. James et al.   MOLECULAR CANCER THERAPEUTICS

Unresponsiveness of colon cancer to BRAF(V600E) inhibition through feedback activation of EGFR

(2012) Anirudh Prahallad et al.   NATURE

Tumour micro-environment elicits innate resistance to RAF inhibitors through HGF secretion

(2012) Ravid Straussman et al.   NATURE

Widespread potential for growth-factor-driven resistance to anticancer kinase inhibitors

(2012) Timothy R. Wilson et al.   NATURE

BRAF Inhibition in Refractory Hairy-Cell Leukemia

(2012) Sascha Dietrich et al.   NEW ENGLAND JOURNAL OF MEDICINE

Survival in BRAF V600–Mutant Advanced Melanoma Treated with Vemurafenib

(2012) Jeffrey A. Sosman et al.   NEW ENGLAND JOURNAL OF MEDICINE

RASMutations in Cutaneous Squamous-Cell Carcinomas in Patients Treated with BRAF Inhibitors

(2012) Fei Su et al.   NEW ENGLAND JOURNAL OF MEDICINE

Structural approaches to obtain kinase selectivity

(2012) Richard A. Norman et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

BRAF and PIK3CA genes are somatically mutated in hepatocellular carcinoma among patients from South Italy

(2012) M Colombino et al.   Cell Death & Disease

Melanoma whole-exome sequencing identifies V600E B-RAF amplification-mediated acquired B-RAF inhibitor resistance

(2012) Hubing Shi et al.   Nature Communications

EGFR-Mediated Reactivation of MAPK Signaling Contributes to Insensitivity of BRAF -Mutant Colorectal Cancers to RAF Inhibition with Vemurafenib

(2012) Ryan B. Corcoran et al.   Cancer Discovery

Analysis of BRAF V600E mutation in 1,320 nervous system tumors reveals high mutation frequencies in pleomorphic xanthoastrocytoma, ganglioglioma and extra-cerebellar pilocytic astrocytoma

(2011) Genevieve Schindler et al.   ACTA NEUROPATHOLOGICA

Antitumor Activity of BRAF Inhibitor Vemurafenib in Preclinical Models of BRAF-Mutant Colorectal Cancer

(2011) H. Yang et al.   CANCER RESEARCH

PTEN Loss Confers BRAF Inhibitor Resistance to Melanoma Cells through the Suppression of BIM Expression

(2011) K. H. T. Paraiso et al.   CANCER RESEARCH

Mutationally Activated BRAFV600E Elicits Papillary Thyroid Cancer in the Adult Mouse

(2011) R.-P. Charles et al.   CANCER RESEARCH

Targeted Therapy for BRAFV600E Malignant Astrocytoma

(2011) T. P. Nicolaides et al.   CLINICAL CANCER RESEARCH

RAF Inhibitor-Induced KSR1/B-RAF Binding and Its Effects on ERK Cascade Signaling

(2011) Melissa M. McKay et al.   CURRENT BIOLOGY

Small-molecule MAPK inhibitors restore radioiodine incorporation in mouse thyroid cancers with conditional BRAF activation

(2011) Debyani Chakravarty et al.   JOURNAL OF CLINICAL INVESTIGATION

RASMutations Are Associated With the Development of Cutaneous Squamous Cell Tumors in Patients Treated With RAF Inhibitors

(2011) Patrick A. Oberholzer et al.   JOURNAL OF CLINICAL ONCOLOGY

Combination therapy with vemurafenib (PLX4032/RG7204) and metformin in melanoma cell lines with distinct driver mutations

(2011) Franziska Niehr et al.   Journal of Translational Medicine

A Raf-induced allosteric transition of KSR stimulates phosphorylation of MEK

(2011) Damian F. Brennan et al.   NATURE

RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E)

(2011) Poulikos I. Poulikakos et al.   NATURE

DHODH modulates transcriptional elongation in the neural crest and melanoma

(2011) Richard Mark White et al.   NATURE

Initial genome sequencing and analysis of multiple myeloma

(2011) Michael A. Chapman et al.   NATURE

BRAFMutations in Hairy-Cell Leukemia

(2011) Enrico Tiacci et al.   NEW ENGLAND JOURNAL OF MEDICINE

Resistance to BRAF Inhibition in Melanomas

(2011) David B. Solit et al.   NEW ENGLAND JOURNAL OF MEDICINE

Improved Survival with Vemurafenib in Melanoma with BRAF V600E Mutation

(2011) Paul B. Chapman et al.   NEW ENGLAND JOURNAL OF MEDICINE

Concurrent loss of the PTEN and RB1 tumor suppressors attenuates RAF dependence in melanomas harboring V600EBRAF

(2011) F Xing et al.   ONCOGENE

Adaptive upregulation of FOXD3 and resistance to PLX4032/4720-induced cell death in mutant B-RAF melanoma cells

(2011) K J Basile et al.   ONCOGENE

Role and therapeutic potential of PI3K-mTOR signaling in de novo resistance to BRAF inhibition

(2011) W. Deng et al.   Pigment Cell & Melanoma Research

BRAF V600E Mutations Are Common in Pleomorphic Xanthoastrocytoma: Diagnostic and Therapeutic Implications

(2011) Dora Dias-Santagata et al.   PLoS One

Mutation that blocks ATP binding creates a pseudokinase stabilizing the scaffolding function of kinase suppressor of Ras, CRAF and BRAF

(2011) J. Hu et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Amplification of the Driving Oncogene, KRAS or BRAF, Underpins Acquired Resistance to MEK1/2 Inhibitors in Colorectal Cancer Cells

(2011) A. S. Little et al.   Science Signaling

Recurrent BRAF mutations in Langerhans cell histiocytosis

(2010) G. Badalian-Very et al.   BLOOD

Recovery of phospho-ERK activity allows melanoma cells to escape from BRAF inhibitor therapy

(2010) K H T Paraiso et al.   BRITISH JOURNAL OF CANCER

Acquired Resistance to BRAF Inhibitors Mediated by a RAF Kinase Switch in Melanoma Can Be Overcome by Cotargeting MEK and IGF-1R/PI3K

(2010) Jessie Villanueva et al.   CANCER CELL

RG7204 (PLX4032), a Selective BRAFV600E Inhibitor, Displays Potent Antitumor Activity in Preclinical Melanoma Models

(2010) H. Yang et al.   CANCER RESEARCH

Akt3-Mediated Resistance to Apoptosis in B-RAF-Targeted Melanoma Cells

(2010) Y. Shao et al.   CANCER RESEARCH

Selective BRAFV600E Inhibition Enhances T-Cell Recognition of Melanoma without Affecting Lymphocyte Function

(2010) A. Boni et al.   CANCER RESEARCH

Kinase-Dead BRAF and Oncogenic RAS Cooperate to Drive Tumor Progression through CRAF

(2010) Sonja J. Heidorn et al.   CELL

The Oncogenic BRAF Kinase Inhibitor PLX4032/RG7204 Does Not Affect the Viability or Function of Human Lymphocytes across a Wide Range of Concentrations

(2010) B. Comin-Anduix et al.   CLINICAL CANCER RESEARCH

Targeting the Mitogen-Activated Protein Kinase Pathway: Physiological Feedback and Drug Response

(2010) C. A. Pratilas et al.   CLINICAL CANCER RESEARCH

Differential sensitivity of melanoma cell lines with BRAFV600E mutation to the specific Raf inhibitor PLX4032

(2010) Jonas N Søndergaard et al.   Journal of Translational Medicine

RAF inhibitors transactivate RAF dimers and ERK signalling in cells with wild-type BRAF

(2010) Poulikos I. Poulikakos et al.   NATURE

RAF inhibitors prime wild-type RAF to activate the MAPK pathway and enhance growth

(2010) Georgia Hatzivassiliou et al.   NATURE

Clinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanoma

(2010) Gideon Bollag et al.   NATURE

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

(2010) Ramin Nazarian et al.   NATURE

Inhibition of Mutated, Activated BRAF in Metastatic Melanoma

(2010) Keith T. Flaherty et al.   NEW ENGLAND JOURNAL OF MEDICINE

Hyperactivation of MEK–ERK1/2 signaling and resistance to apoptosis induced by the oncogenic B-RAF inhibitor, PLX4720, in mutant N-RAS melanoma cells

(2010) F M Kaplan et al.   ONCOGENE

PLX4032, a potent inhibitor of the B-Raf V600E oncogene, selectively inhibits V600E-positive melanomas

(2010) John T. Lee et al.   Pigment Cell & Melanoma Research

PLX4032, a selective BRAFV600E kinase inhibitor, activates the ERK pathway and enhances cell migration and proliferation of BRAFWT melanoma cells

(2010) Ruth Halaban et al.   Pigment Cell & Melanoma Research

A Phase II Trial of Sorafenib in Metastatic Melanoma with Tissue Correlates

(2010) Patrick A. Ott et al.   PLoS One

The RAF inhibitor PLX4032 inhibits ERK signaling and tumor cell proliferation in a V600E BRAF-selective manner

(2010) E. W. Joseph et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

BRAF Gene Amplification Can Promote Acquired Resistance to MEK Inhibitors in Cancer Cells Harboring the BRAF V600E Mutation

(2010) R. B. Corcoran et al.   Science Signaling

Apoptosis of human melanoma cells induced by inhibition of B-RAFV600E involves preferential splicing of bimS

(2010) C C Jiang et al.   Cell Death & Disease

Duplication of 7q34 in Pediatric Low-Grade Astrocytomas Detected by High-Density Single-Nucleotide Polymorphism-Based Genotype Arrays Results in a NovelBRAFFusion Gene

(2009) Angela J. Sievert et al.   BRAIN PATHOLOGY

Scaffold-based design of kinase inhibitors for cancer therapy

(2009) Chao Zhang et al.   CURRENT OPINION IN GENETICS & DEVELOPMENT

Cytostatic Activity of Adenosine Triphosphate-Competitive Kinase Inhibitors inBRAFMutant Thyroid Carcinoma Cells

(2009) Paolo Salerno et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

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

(2009) Axel Hauschild et al.   JOURNAL OF CLINICAL ONCOLOGY

Phase II Trial of Infusional Fluorouracil, Irinotecan, and Bevacizumab for Metastatic Colorectal Cancer: Efficacy and Circulating Angiogenic Biomarkers Associated With Therapeutic Resistance

(2009) Scott Kopetz et al.   JOURNAL OF CLINICAL ONCOLOGY

Impact of Feedback Phosphorylation and Raf Heterodimerization on Normal and Mutant B-Raf Signaling

(2009) D. A. Ritt et al.   MOLECULAR AND CELLULAR BIOLOGY

A dimerization-dependent mechanism drives RAF catalytic activation

(2009) Thanashan Rajakulendran et al.   NATURE

The rise of fragment-based drug discovery

(2009) Christopher W. Murray et al.   Nature Chemistry

BrafV600E cooperates with Pten loss to induce metastatic melanoma

(2009) David Dankort et al.   NATURE GENETICS

Melanocytic nevus-like hyperplasia and melanoma in transgenic BRAFV600E mice

(2009) V K Goel et al.   ONCOGENE

Sorafenib for the Treatment of Unresectable Hepatocellular Carcinoma

(2009) R. C. Kane et al.   ONCOLOGIST

Uncoupling of the LKB1-AMPKα Energy Sensor Pathway by Growth Factors and Oncogenic BRAFV600E

(2009) Rosaura Esteve-Puig et al.   PLoS One

Melanoma Drug Vindicates Targeted Approach

(2009) K. Garber   SCIENCE

Elevated CRAF as a Potential Mechanism of Acquired Resistance to BRAF Inhibition in Melanoma

(2008) C. Montagut et al.   CANCER RESEARCH

Tandem Duplication Producing a Novel OncogenicBRAFFusion Gene Defines the Majority of Pilocytic Astrocytomas

(2008) David T.W. Jones et al.   CANCER RESEARCH

A Phase I Trial of the Oral, Multikinase Inhibitor Sorafenib in Combination with Carboplatin and Paclitaxel

(2008) K. T. Flaherty et al.   CLINICAL CANCER RESEARCH

Novel V600E BRAF mutations in imatinib-naive and imatinib-resistant gastrointestinal stromal tumors

(2008) Narasimhan P. Agaram et al.   GENES CHROMOSOMES & CANCER

BRAF gene duplication constitutes a mechanism of MAPK pathway activation in low-grade astrocytomas

(2008) Stefan Pfister et al.   JOURNAL OF CLINICAL INVESTIGATION

BRAF Silencing by Short Hairpin RNA or Chemical Blockade by PLX4032 Leads to Different Responses in Melanoma and Thyroid Carcinoma Cells

(2008) E. Sala et al.   MOLECULAR CANCER RESEARCH

BRAF Activation Initiates but Does Not Maintain Invasive Prostate Adenocarcinoma

(2008) Joseph H. Jeong et al.   PLoS One

Scaffold-based discovery of indeglitazar, a PPAR pan-active anti-diabetic agent

(2008) D. R. Artis et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Discovery of a selective inhibitor of oncogenic B-Raf kinase with potent antimelanoma activity

(2008) J. Tsai et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA