A patent review of RAF kinase inhibitors (2010–2018)

Cutaneous adverse reactions in B-RAF positive metastatic melanoma following sequential treatment with B-RAF/MEK inhibitors and immune checkpoint blockade or vice versa. A single-institutional case-series

(2019) Abdul Rafeh Naqash et al.   Journal for ImmunoTherapy of Cancer

In silico-in vitro discovery of untargeted kinase–inhibitor interactions from kinase-targeted therapies: A case study on the cancer MAPK signaling pathway

(2018) Li Meng et al.   COMPUTATIONAL BIOLOGY AND CHEMISTRY

Downregulation of Raf-1 kinase inhibitory protein as a sorafenib resistance mechanism in hepatocellular carcinoma cell lines

(2018) Jin Sun Kim et al.   JOURNAL OF CANCER RESEARCH AND CLINICAL ONCOLOGY

Targeting few to help hundreds: JAK, MAPK and ROCK pathways as druggable targets in atypical chronic myeloid leukemia

(2018) Stefania Rocca et al.   Molecular Cancer

Dissecting RAF Inhibitor Resistance by Structure-based Modeling Reveals Ways to Overcome Oncogenic RAS Signaling

(2018) Oleksii S. Rukhlenko et al.   Cell Systems

Targeting oncogenic Raf protein-serine/threonine kinases in human cancers

(2018) Robert Roskoski   PHARMACOLOGICAL RESEARCH

Rituximab prevents long-term relapses in TTP

(2018)   BLOOD

Pharmacological Induction of RAS-GTP Confers RAF Inhibitor Sensitivity in KRAS Mutant Tumors

(2018) Ivana Yen et al.   CANCER CELL

KinaMetrix: a web resource to investigate kinase conformations and inhibitor space

(2018) Rayees Rahman et al.   NUCLEIC ACIDS RESEARCH

Discovery of a novel pan-RAF inhibitor with potent anti-tumor activity in preclinical models of BRAF V600E mutant cancer

(2017) Sung Pyo Hong et al.   LIFE SCIENCES

A Braf kinase-inactive mutant induces lung adenocarcinoma

(2017) Patricia Nieto et al.   NATURE

Promoter methylation and expression of Raf kinase inhibitory protein in esophageal squamous cell carcinoma

(2017) Hong Wei et al.   Oncology Letters

Recurrent Tumor Cell–Intrinsic and –Extrinsic Alterations during MAPKi-Induced Melanoma Regression and Early Adaptation

(2017) Chunying Song et al.   Cancer Discovery

Chemically Linked Vemurafenib Inhibitors Promote an Inactive BRAFV600E Conformation

(2016) Michael Grasso et al.   ACS Chemical Biology

Sentinel Lymph Node Genes to Predict Prognosis in Node-Positive Melanoma Patients

(2016) Hongying Hao et al.   ANNALS OF SURGICAL ONCOLOGY

B-Raf Inhibition in the Clinic: Present and Future

(2016) Warren Fiskus et al.   Annual Review of Medicine

Mutant B-Raf Kinase Inhibitors as Anticancer Agents

(2016) Vivek Asati et al.   Anti-Cancer Agents in Medicinal Chemistry

Identification and Characterization of Small-Molecule Inhibitors to Selectively Target the DFG-in over the DFG-out Conformation of the B-Raf Kinase V600E Mutant in Colorectal Cancer

(2016) Huixiang Yao et al.   ARCHIV DER PHARMAZIE

An Integrated Model of RAF Inhibitor Action Predicts Inhibitor Activity against Oncogenic BRAF Signaling

(2016) Zoi Karoulia et al.   CANCER CELL

Encorafenib (LGX818), a potent BRAF inhibitor, induces senescence accompanied by autophagy in BRAFV600E melanoma cells

(2016) Zhen Li et al.   CANCER LETTERS

Increased Expression of miR-23a Mediates a Loss of Expression in the RAF Kinase Inhibitor Protein RKIP

(2016) S. Hatzl et al.   CANCER RESEARCH

A Novel RAF Kinase Inhibitor with DFG-Out-Binding Mode: High Efficacy in BRAF-Mutant Tumor Xenograft Models in the Absence of Normal Tissue Hyperproliferation

(2016) I. C. Waizenegger et al.   MOLECULAR CANCER THERAPEUTICS

Classification of small molecule protein kinase inhibitors based upon the structures of their drug-enzyme complexes

(2016) Robert Roskoski   PHARMACOLOGICAL RESEARCH

Preclinical efficacy of a RAF inhibitor that evades paradoxical MAPK pathway activation in protein kinaseBRAF-mutant lung cancer

(2016) Ross A. Okimoto et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

BRAF V600E Kinase Domain Duplication Identified in Therapy-Refractory Melanoma Patient-Derived Xenografts

(2016) Kristel Kemper et al.   Cell Reports

Non-p.V600E BRAF Mutations Are Common Using a More Sensitive and Broad Detection Tool

(2015) Jamal Carter et al.   AMERICAN JOURNAL OF CLINICAL PATHOLOGY

Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers

(2015) Sheng-Bin Peng et al.   CANCER CELL

Phase II Pilot Study of Vemurafenib in Patients With Metastatic BRAF-Mutated Colorectal Cancer

(2015) Scott Kopetz et al.   JOURNAL OF CLINICAL ONCOLOGY

Discovery of 1-(3,3-Dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyrido[2,3-d]pyrimidin-6-yl)phenyl)urea (LY3009120) as a Pan-RAF Inhibitor with Minimal Paradoxical Activation and Activity against BRAF or RAS Mutant Tumor Cells

(2015) James R. Henry et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Effect of a Widespread Cancer-Causing Mutation on the Inactive to Active Dynamics of the B-Raf Kinase

(2015) Kristen A. Marino et al.   JOURNAL OF THE AMERICAN CHEMICAL SOCIETY

BGB-283, a Novel RAF Kinase and EGFR Inhibitor, Displays Potent Antitumor Activity in BRAF-Mutated Colorectal Cancers

(2015) Z. Tang et al.   MOLECULAR CANCER THERAPEUTICS

RAF inhibitors that evade paradoxical MAPK pathway activation

(2015) Chao Zhang et al.   NATURE

Regulation of RAF protein kinases in ERK signalling

(2015) Hugo Lavoie et al.   NATURE REVIEWS MOLECULAR CELL BIOLOGY

The MAPK pathway as an apoptosis enhancer in melanoma

(2015) Johannes M. Haydn et al.   Oncotarget

Dabrafenib Therapy for Advanced Melanoma

(2014) Van Anh Trinh et al.   ANNALS OF PHARMACOTHERAPY

Optimization of Diarylthiazole B-Raf Inhibitors: Identification of a Compound Endowed with High Oral Antitumor Activity, Mitigated hERG Inhibition, and Low Paradoxical Effect

(2014) Maurizio Pulici et al.   ChemMedChem

Design and synthesis of novel 2-(4-(2-(dimethylamino)ethyl)-4H-1,2,4-triazol-3-yl)pyridines as potential antitumor agents

(2014) Mingze Qin et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

MEK1/2 inhibitors in the treatment of gynecologic malignancies

(2014) Caela R. Miller et al.   GYNECOLOGIC ONCOLOGY

Mitogen-activated Protein Kinase (MAPK) Hyperactivation and Enhanced NRAS Expression Drive Acquired Vemurafenib Resistance in V600E BRAF Melanoma Cells

(2014) Michael Lidsky et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Kinases and Pseudokinases: Lessons from RAF

(2014) A. S. Shaw et al.   MOLECULAR AND CELLULAR BIOLOGY

Targeting RAS–ERK signalling in cancer: promises and challenges

(2014) Ahmed A. Samatar et al.   NATURE REVIEWS DRUG DISCOVERY

Combined Vemurafenib and Cobimetinib in BRAF-Mutated Melanoma

(2014) James Larkin et al.   NEW ENGLAND JOURNAL OF MEDICINE

Inhibition of mutant BRAF splice variant signaling by next-generation, selective RAF inhibitors

(2014) Kevin J. Basile et al.   Pigment Cell & Melanoma Research

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

Targeting BRAF mutant metastatic colorectal cancer: clinical implications and emerging therapeutic strategies

(2014) Jeanne Tie et al.   Targeted Oncology

Increased MAPK reactivation in early resistance to dabrafenib/trametinib combination therapy of BRAF-mutant metastatic melanoma

(2014) Georgina V. Long et al.   Nature Communications

Phase I and pharmacokinetic/pharmacodynamic study of RO5126766, a first-in-class dual Raf/MEK inhibitor, in Japanese patients with advanced solid tumors

(2013) Kazunori Honda et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

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

B-Raf and the inhibitors: from bench to bedside

(2013) Tiangui Huang et al.   Journal of Hematology & Oncology

Signatures of mutational processes in human cancer

(2013) Ludmil B. Alexandrov et al.   NATURE

Acquired Resistance and Clonal Evolution in Melanoma during BRAF Inhibitor Therapy

(2013) H. Shi et al.   Cancer Discovery

MAP Kinase Pathway Alterations in BRAF-Mutant Melanoma Patients with Acquired Resistance to Combined RAF/MEK Inhibition

(2013) N. Wagle et al.   Cancer Discovery

Novel small molecule Raf kinase inhibitors for targeted cancer therapeutics

(2012) Do-Hee Kim et al.   ARCHIVES OF PHARMACAL RESEARCH

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

(2012) Piro Lito et al.   CANCER CELL

Decreased Expression and Aberrant Methylation of Raf Kinase Inhibitory Protein Gene in Esophageal Squamous Cell Carcinoma

(2012) Wei Guo et al.   CANCER INVESTIGATION

Dynamic Reprogramming of the Kinome in Response to Targeted MEK Inhibition in Triple-Negative Breast Cancer

(2012) James S. Duncan et al.   CELL

BRAF mutations in melanoma and colorectal cancer: A single oncogenic mutation with different tumour phenotypes and clinical implications

(2012) F. Sclafani et al.   CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY

Raf Inhibitors Target Ras Spatiotemporal Dynamics

(2012) Kwang-jin Cho et al.   CURRENT BIOLOGY

The RAS/RAF/MEK/ERK and the PI3K/AKT signalling pathways: role in cancer pathogenesis and implications for therapeutic approaches

(2012) Antonella De Luca et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Conformation-Specific Effects of Raf Kinase Inhibitors

(2012) Xiaolun Wang et al.   JOURNAL OF MEDICINAL CHEMISTRY

Combinations of BRAF, MEK, and PI3K/mTOR Inhibitors Overcome Acquired Resistance to the BRAF Inhibitor GSK2118436 Dabrafenib, Mediated by NRAS or MEK Mutations

(2012) J. G. Greger et al.   MOLECULAR CANCER THERAPEUTICS

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

Vemurafenib: the first drug approved for BRAF-mutant cancer

(2012) Gideon Bollag et al.   NATURE REVIEWS DRUG DISCOVERY

Survival in BRAF V600–Mutant Advanced Melanoma Treated with Vemurafenib

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

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

ABCB5 Identifies a Therapy-Refractory Tumor Cell Population in Colorectal Cancer Patients

(2011) B. J. Wilson et al.   CANCER RESEARCH

The novel Raf inhibitor Raf265 decreases Bcl-2 levels and confers TRAIL-sensitivity to neuroendocrine tumour cells

(2011) K. Zitzmann et al.   ENDOCRINE-RELATED CANCER

Identification of 1-(3-(6,7-Dimethoxyquinazolin-4-yloxy)phenyl)-3-(5-(1,1,1-trifluoro-2-methylpropan-2-yl)isoxazol-3-yl)urea Hydrochloride (CEP-32496), a Highly Potent and Orally Efficacious Inhibitor of V-RAF Murine Sarcoma Viral Oncogene Homologue B1 (BRAF) V600E

(2011) Martin W. Rowbottom et al.   JOURNAL OF MEDICINAL CHEMISTRY

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

The design, synthesis, and evaluation of 8 hybrid DFG-out allosteric kinase inhibitors: A structural analysis of the binding interactions of Gleevec®, Nexavar®, and BIRB-796

(2010) Justin Dietrich et al.   BIOORGANIC & MEDICINAL CHEMISTRY

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

(2010) Sonja J. Heidorn et al.   CELL

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

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

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