“RAF” neighborhood: Protein-protein interaction in the Raf/Mek/Erk pathway

Disruption of CRAF-Mediated MEK Activation Is Required for Effective MEK Inhibition in KRAS Mutant Tumors

(2014) Piro Lito et al.   CANCER CELL

Reversible and adaptive resistance to BRAF(V600E) inhibition in melanoma

(2014) Chong Sun et al.   NATURE

BRAF Inhibitors Induce Metastasis in RAS Mutant or Inhibitor-Resistant Melanoma Cells by Reactivating MEK and ERK Signaling

(2014) B. Sanchez-Laorden et al.   Science Signaling

MEK-1 activates C-Raf through a Ras-independent mechanism

(2013) Deborah T. Leicht et al.   BIOCHIMICA ET BIOPHYSICA ACTA-MOLECULAR CELL RESEARCH

RAF Inhibitors Activate the MAPK Pathway by Relieving Inhibitory Autophosphorylation

(2013) Matthew Holderfield et al.   CANCER CELL

Skin Tumorigenesis Stimulated by Raf Inhibitors Relies Upon Raf Functions That Are Dependent and Independent of ERK

(2013) E. Doma et al.   CANCER RESEARCH

Enhanced Inhibition of ERK Signaling by a Novel Allosteric MEK Inhibitor, CH5126766, That Suppresses Feedback Reactivation of RAF Activity

(2013) Nobuya Ishii et al.   CANCER RESEARCH

Allosteric Activation of Functionally Asymmetric RAF Kinase Dimers

(2013) Jiancheng Hu et al.   CELL

Dabrafenib: First Global Approval

(2013) Anita D. Ballantyne et al.   DRUGS

Clinical development of dabrafenib in BRAF mutant melanoma and other malignancies

(2013) Geoffrey T Gibney et al.   Expert Opinion on Drug Metabolism & Toxicology

Phase I/II RAF kinase inhibitors in cancer therapy

(2013) Samra Turajlic et al.   EXPERT OPINION ON INVESTIGATIONAL DRUGS

MEK1 Is Required for PTEN Membrane Recruitment, AKT Regulation, and the Maintenance of Peripheral Tolerance

(2013) Katarina Zmajkovicova et al.   MOLECULAR CELL

Effects of Raf Dimerization and Its Inhibition on Normal and Disease-Associated Raf Signaling

(2013) Alyson K. Freeman et al.   MOLECULAR CELL

A melanocyte lineage program confers resistance to MAP kinase pathway inhibition

(2013) Cory M. Johannessen et al.   NATURE

Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers

(2013) Georgia Hatzivassiliou et al.   NATURE

Modelling vemurafenib resistance in melanoma reveals a strategy to forestall drug resistance

(2013) Meghna Das Thakur et al.   NATURE

Melanoma combination therapies ward off tumor resistance

(2013) Ken Garber   NATURE BIOTECHNOLOGY

Relief of Profound Feedback Inhibition of Mitogenic Signaling by RAF Inhibitors Attenuates Their Activity in BRAFV600E Melanomas

(2012) Piro Lito et al.   CANCER CELL

Distinct requirement for an intact dimer interface in wild-type, V600E and kinase-dead B-Raf signalling

(2012) Michael Röring et al.   EMBO JOURNAL

Dual-specificity MAP kinase phosphatases (MKPs)

(2012) Christopher J. Caunt et al.   FEBS Journal

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

(2012) Axel Hauschild et al.   LANCET

Safety, pharmacokinetic, pharmacodynamic, and efficacy data for the oral MEK inhibitor trametinib: a phase 1 dose-escalation trial

(2012) Jeffrey R Infante et al.   LANCET ONCOLOGY

Successful rechallenge in two patients with BRAF-V600-mutant melanoma who experienced previous progression during treatment with a selective BRAF inhibitor

(2012) Amélie Clémentine Seghers et al.   MELANOMA RESEARCH

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

Combined BRAF and MEK Inhibition in Melanoma with BRAF V600 Mutations

(2012) Keith T. Flaherty 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

Essential, non-redundant roles of B-Raf and Raf-1 in Ras-driven skin tumorigenesis

(2012) F Kern et al.   ONCOGENE

ERK1/2 MAP kinases: Structure, function, and regulation

(2012) Robert Roskoski   PHARMACOLOGICAL RESEARCH

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

MEK1/2 dual-specificity protein kinases: Structure and regulation

(2011) Robert Roskoski   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

c-Raf, but Not B-Raf, Is Essential for Development of K-Ras Oncogene-Driven Non-Small Cell Lung Carcinoma

(2011) Rafael B. Blasco et al.   CANCER CELL

Resistance to Selective BRAF Inhibition Can Be Mediated by Modest Upstream Pathway Activation

(2011) F. Su et al.   CANCER RESEARCH

ERK dimers and scaffold proteins: Unexpected partners for a forgotten (cytoplasmic) task

(2011) Berta Casar et al.   CELL CYCLE

GSK1120212 (JTP-74057) Is an Inhibitor of MEK Activity and Activation with Favorable Pharmacokinetic Properties for Sustained In Vivo Pathway Inhibition

(2011) A. G. Gilmartin 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

Angiogenic Sprouting Requires the Fine Tuning of Endothelial Cell Cohesion by the Raf-1/Rok-α Complex

(2011) Reiner Wimmer et al.   DEVELOPMENTAL CELL

Dissecting Therapeutic Resistance to RAF Inhibition in Melanoma by Tumor Genomic Profiling

(2011) Nikhil Wagle et al.   JOURNAL OF CLINICAL ONCOLOGY

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

Strong negative feedback from Erk to Raf confers robustness to MAPK signalling

(2011) R. Fritsche-Guenther et al.   Molecular Systems Biology

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

Improved Survival with Vemurafenib in Melanoma with BRAF V600E Mutation

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

C-Raf Is Required for the Initiation of Lung Cancer by K-Ras G12D

(2011) Florian A. Karreth et al.   Cancer Discovery

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

Heterogeneous Nuclear Ribonucleoprotein H Blocks MST2-Mediated Apoptosis in Cancer Cells by Regulating a-raf Transcription

(2010) J. Rauch et al.   CANCER RESEARCH

Targets of Raf in tumorigenesis

(2010) T. S. Niault et al.   CARCINOGENESIS

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

(2010) Sonja J. Heidorn et al.   CELL

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

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

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

The Mammalian MAPK/ERK Pathway Exhibits Properties of a Negative Feedback Amplifier

(2010) O. E. Sturm et al.   Science Signaling

Partner exchange: protein–protein interactions in the Raf pathway

(2010) Reiner Wimmer et al.   TRENDS IN BIOCHEMICAL SCIENCES

Raf-1 Addiction in Ras-Induced Skin Carcinogenesis

(2009) Karin Ehrenreiter et al.   CANCER CELL

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

PI3K Pathway Activation Mediates Resistance to MEK Inhibitors in KRAS Mutant Cancers

(2009) S. Wee et al.   CANCER RESEARCH

In vivo Antitumor Activity of MEK and Phosphatidylinositol 3-Kinase Inhibitors in Basal-Like Breast Cancer Models

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

ERK Nuclear Translocation Is Dimerization-independent but Controlled by the Rate of Phosphorylation

(2009) Diane S. Lidke et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

From autoinhibition to inhibition in trans: the Raf-1 regulatory domain inhibits Rok-α kinase activity

(2009) Théodora Niault et al.   JOURNAL OF CELL BIOLOGY

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

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

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

C-Raf Inhibits MAPK Activation and Transformation by B-RafV600E

(2009) Florian A. Karreth et al.   MOLECULAR CELL

A dimerization-dependent mechanism drives RAF catalytic activation

(2009) Thanashan Rajakulendran et al.   NATURE

A Mek1–Mek2 heterodimer determines the strength and duration of the Erk signal

(2009) Federica Catalanotti et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

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

The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901

(2008) Stephen D. Barrett 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

Essential role of B-Raf in oligodendrocyte maturation and myelination during postnatal central nervous system development

(2008) Gergana Galabova-Kovacs et al.   JOURNAL OF CELL BIOLOGY

Essential Role of ERK Dimers in the Activation of Cytoplasmic but Not Nuclear Substrates by ERK-Scaffold Complexes

(2008) Berta Casar et al.   MOLECULAR CELL

B-Raf is required for ERK activation and tumor progression in a mouse model of pancreatic β-cell carcinogenesis

(2008) I Sobczak et al.   ONCOGENE