Targeted inhibition of BRAF kinase: opportunities and challenges for therapeutics in melanoma

Mutant BRAF Melanomas—Dependence and Resistance

(2011) Poulikos I. Poulikakos et al.   CANCER CELL

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

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

RAF inhibition and induction of cutaneous squamous cell carcinoma

(2011) Caroline Robert et al.   CURRENT OPINION IN ONCOLOGY

35th ESMO Congress Organization

(2010)   ANNALS OF ONCOLOGY

BRAF as therapeutic target in melanoma

(2010) Claudia Wellbrock et al.   BIOCHEMICAL PHARMACOLOGY

Targeting BRAF for patients with melanoma

(2010) H-T Arkenau et al.   BRITISH JOURNAL OF CANCER

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

BRAF, a target in melanoma

(2010) Keith T. Flaherty et al.   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

Metformin: A Therapeutic Opportunity in Breast Cancer

(2010) A. M. Gonzalez-Angulo et al.   CLINICAL CANCER RESEARCH

Metformin: Taking away the candy for cancer?

(2010) Mathilde Jalving et al.   EUROPEAN JOURNAL OF CANCER

Skin Toxicity Evaluation Protocol With Panitumumab (STEPP), a Phase II, Open-Label, Randomized Trial Evaluating the Impact of a Pre-Emptive Skin Treatment Regimen on Skin Toxicities and Quality of Life in Patients With Metastatic Colorectal Cancer

(2010) Mario E. Lacouture et al.   JOURNAL OF CLINICAL ONCOLOGY

Nevi, Family History, and Fair Skin Increase the Risk of Second Primary Melanoma

(2010) Victor Siskind et al.   JOURNAL OF INVESTIGATIVE DERMATOLOGY

KRAS and BRAF: drug targets and predictive biomarkers

(2010) Efsevia Vakiani et al.   JOURNAL OF PATHOLOGY

Incidence of the V600K mutation among melanoma patients with BRAF mutations, and potential therapeutic response to the specific BRAF inhibitor PLX4032

(2010) Jill C Rubinstein et al.   Journal of Translational Medicine

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

Dependence on Phosphoinositide 3-Kinase and RAS-RAF Pathways Drive the Activity of RAF265, a Novel RAF/VEGFR2 Inhibitor, and RAD001 (Everolimus) in Combination

(2010) P. Mordant et al.   MOLECULAR CANCER THERAPEUTICS

Sorafenib, a Multikinase Inhibitor, Enhances the Response of Melanoma to Regional Chemotherapy

(2010) C. K. Augustine et al.   MOLECULAR CANCER THERAPEUTICS

Metformin in Cancer Therapy: A New Perspective for an Old Antidiabetic Drug?

(2010) I. Ben Sahra et al.   MOLECULAR CANCER THERAPEUTICS

How melanomas bypass new therapy

(2010) David Solit et al.   NATURE

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

COT drives resistance to RAF inhibition through MAP kinase pathway reactivation

(2010) Cory M. Johannessen 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

Improved Survival with Ipilimumab in Patients with Metastatic Melanoma

(2010) F. Stephen Hodi et al.   NEW ENGLAND JOURNAL OF MEDICINE

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

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

Gatekeeper Mutations Mediate Resistance to BRAF-Targeted Therapies

(2010) S. Whittaker et al.   Science Translational Medicine

Small molecules and targeted therapies in distant metastatic disease

(2009) P. Hersey et al.   ANNALS OF ONCOLOGY

Antitumor Efficacy of the Novel RAF Inhibitor GDC-0879 Is Predicted by BRAFV600E Mutational Status and Sustained Extracellular Signal-Regulated Kinase/Mitogen-Activated Protein Kinase Pathway Suppression

(2009) K. P. Hoeflich et al.   CANCER RESEARCH

Scaffold-based design of kinase inhibitors for cancer therapy

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

Pharmacodynamics of 2- ethan-1-ol (GDC-0879), a Potent and Selective B-Raf Kinase Inhibitor: Understanding Relationships between Systemic Concentrations, Phosphorylated Mitogen-Activated Protein Kinase Kinase 1 Inhibition, and Efficacy

(2009) H. Wong et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Oncogenic B-RAF Negatively Regulates the Tumor Suppressor LKB1 to Promote Melanoma Cell Proliferation

(2009) Bin Zheng et al.   MOLECULAR CELL

MEK1 mutations confer resistance to MEK and B-RAF inhibition

(2009) C. M. Emery et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

V600EBRAF is associated with disabled feedback inhibition of RAF-MEK signaling and elevated transcriptional output of the pathway

(2009) C. A. Pratilas et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Potent and selective pyrazole-based inhibitors of B-Raf kinase

(2008) Joshua D. Hansen et al.   BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

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

(2008) C. Montagut et al.   CANCER RESEARCH

Increased cyclin D1 expression can mediate BRAF inhibitor resistance in BRAF V600E-mutated melanomas

(2008) K. S.M. Smalley et al.   MOLECULAR CANCER THERAPEUTICS

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