New RAF kinase inhibitors in cancer therapy

Relationship of EGFR-independent activation of PI3K in KRAS wild-type colorectal cancers and cetuximab resistance.

(2017) Ryan Bruce Corcoran et al.   JOURNAL OF CLINICAL ONCOLOGY

Prospects for MEK inhibitors for treating cancer

(2014) Juan Martin-Liberal et al.   Expert Opinion On Drug Safety

Safety and efficacy of vemurafenib in BRAFV600E and BRAFV600K mutation-positive melanoma (BRIM-3): extended follow-up of a phase 3, randomised, open-label study

(2014) Grant A McArthur et al.   LANCET ONCOLOGY

Expression and mutational status of treatment-relevant targets and key oncogenes in 123 malignant salivary gland tumours

(2013) J. Cros et al.   ANNALS OF ONCOLOGY

Molecular Pathways: Mitogen-Activated Protein Kinase Pathway Mutations and Drug Resistance

(2013) A. L. Pritchard et al.   CLINICAL CANCER RESEARCH

Phase I/II RAF kinase inhibitors in cancer therapy

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

Phase II Trial (BREAK-2) of the BRAF Inhibitor Dabrafenib (GSK2118436) in Patients With Metastatic Melanoma

(2013) Paolo A. Ascierto et al.   JOURNAL OF CLINICAL ONCOLOGY

B-Raf and the inhibitors: from bench to bedside

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

Which drug, and when, for patients with BRAF-mutant melanoma?

(2013) Sekwon Jang et al.   LANCET ONCOLOGY

Tumor adaptation and resistance to RAF inhibitors

(2013) Piro Lito et al.   NATURE MEDICINE

Paradoxical oncogenesis—the long-term effects of BRAF inhibition in melanoma

(2013) Geoffrey T. Gibney et al.   Nature Reviews Clinical Oncology

Dabrafenib; Preclinical Characterization, Increased Efficacy when Combined with Trametinib, while BRAF/MEK Tool Combination Reduced Skin Lesions

(2013) Alastair J. King et al.   PLoS One

A Genome-Scale RNA Interference Screen Implicates NF1 Loss in Resistance to RAF Inhibition

(2013) Steven R. Whittaker et al.   Cancer Discovery

Relief of Feedback Inhibition of HER3 Transcription by RAF and MEK Inhibitors Attenuates Their Antitumor Effects in BRAF -Mutant Thyroid Carcinomas

(2013) Cristina Montero-Conde et al.   Cancer Discovery

BRAF as a Target for Cancer Therapy

(2012) Rodrigo Dienstmann et al.   Anti-Cancer Agents in Medicinal Chemistry

PK-PD modeling of combination efficacy effect from administration of the MEK inhibitor GDC-0973 and PI3K inhibitor GDC-0941 in A2058 xenografts

(2012) Edna F. Choo et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Abstract 3790: Preclinical profile of LGX818: A potent and selective RAF kinase inhibitor

(2012) Darrin D. Stuart et al.   CANCER RESEARCH

Bridging the Gap between Preclinical and Clinical Studies Using Pharmacokinetic-Pharmacodynamic Modeling: An Analysis of GDC-0973, a MEK Inhibitor

(2012) H. Wong et al.   CLINICAL CANCER RESEARCH

Phase II Efficacy and Pharmacogenomic Study of Selumetinib (AZD6244; ARRY-142886) in Iodine-131 Refractory Papillary Thyroid Carcinoma with or without Follicular Elements

(2012) D. N. Hayes et al.   CLINICAL CANCER RESEARCH

Targeting the MAPK–RAS–RAF signaling pathway in cancer therapy

(2012) Libero Santarpia et al.   EXPERT OPINION ON THERAPEUTIC TARGETS

Phase II Study of the MEK1/MEK2 Inhibitor Trametinib in Patients With MetastaticBRAF-Mutant Cutaneous Melanoma Previously Treated With or Without a BRAF Inhibitor

(2012) Kevin B. Kim et al.   JOURNAL OF CLINICAL 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

Activity of the oral MEK inhibitor trametinib in patients with advanced melanoma: a phase 1 dose-escalation trial

(2012) Gerald S Falchook et al.   LANCET ONCOLOGY

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

Dabrafenib in patients with Val600Glu or Val600Lys BRAF-mutant melanoma metastatic to the brain (BREAK-MB): a multicentre, open-label, phase 2 trial

(2012) Georgina V Long et al.   LANCET ONCOLOGY

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

(2012) Anirudh Prahallad 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

Improved Survival with MEK Inhibition in BRAF-Mutated Melanoma

(2012) Keith T. Flaherty 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

ARAF acts as a scaffold to stabilize BRAF:CRAF heterodimers

(2012) A P Rebocho et al.   ONCOGENE

Elucidating Distinct Roles for NF1 in Melanomagenesis

(2012) Ophélia Maertens et al.   Cancer Discovery

Targeted therapy and immunotherapy in advanced melanoma: an evolving paradigm

(2012) Muhammad Khattak et al.   Therapeutic Advances in Medical Oncology

NRAS mutation status is an independent prognostic factor in metastatic melanoma

(2011) John A. Jakob et al.   CANCER

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

Intermittent Administration of MEK Inhibitor GDC-0973 plus PI3K Inhibitor GDC-0941 Triggers Robust Apoptosis and Tumor Growth Inhibition

(2011) K. P. Hoeflich et al.   CANCER RESEARCH

Skin Tumors Induced by Sorafenib; Paradoxic RAS-RAF Pathway Activation and Oncogenic Mutations of HRAS, TP53, and TGFBR1

(2011) J. P. Arnault et al.   CLINICAL CANCER RESEARCH

Phase II, Open-Label, Randomized Trial of the MEK1/2 Inhibitor Selumetinib as Monotherapy versus Temozolomide in Patients with Advanced Melanoma

(2011) J. M. Kirkwood et al.   CLINICAL CANCER RESEARCH

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

A phase II open-label randomized study to assess the efficacy and safety of selumetinib (AZD6244 [ARRY-142886]) versus capecitabine in patients with advanced or metastatic pancreatic cancer who have failed first-line gemcitabine therapy

(2011) György Bodoky et al.   INVESTIGATIONAL NEW DRUGS

Phase II Study of the Mitogen-Activated Protein Kinase 1/2 Inhibitor Selumetinib in Patients With Advanced Hepatocellular Carcinoma

(2011) Bert H. O'Neil et al.   JOURNAL OF CLINICAL ONCOLOGY

Prognostic and Clinicopathologic Associations of OncogenicBRAFin Metastatic Melanoma

(2011) Georgina V. Long et al.   JOURNAL OF CLINICAL ONCOLOGY

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

Evolutionary expansion of the Ras switch regulatory module in eukaryotes

(2011) Diego Díez et al.   NUCLEIC ACIDS RESEARCH

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

(2011) F Xing et al.   ONCOGENE

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

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

RAF protein-serine/threonine kinases: Structure and regulation

(2010) Robert Roskoski   BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS

Genetic alterations in the RAS/RAF/mitogen-activated protein kinase and phosphatidylinositol 3-kinase/Akt signaling pathways in the follicular variant of papillary thyroid carcinoma

(2010) Libero Santarpia et al.   CANCER

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

(2010) Sonja J. Heidorn et al.   CELL

How ERK1/2 activation controls cell proliferation and cell death: Is subcellular localization the answer?

(2010) Yohannes Mebratu et al.   CELL CYCLE

A Phase II, open-label, randomised study to assess the efficacy and safety of the MEK1/2 inhibitor AZD6244 (ARRY-142886) versus capecitabine monotherapy in patients with colorectal cancer who have failed one or two prior chemotherapeutic regimens

(2010) Jaafar Bennouna et al.   INVESTIGATIONAL NEW DRUGS

A Phase II, Open-Label, Randomized Study to Assess the Efficacy and Safety of AZD6244 (ARRY-142886) Versus Pemetrexed in Patients with Non-small Cell Lung Cancer Who Have Failed One or Two Prior Chemotherapeutic Regimens

(2010) John D. Hainsworth et al.   Journal of Thoracic Oncology

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

(2010) Poulikos I. Poulikakos 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

RAS Mutations Are the Predominant Molecular Alteration in Poorly Differentiated Thyroid Carcinomas and Bear Prognostic Impact

(2009) Marco Volante et al.   JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM

Gastrosplenic Fistula From Hodgkin's Lymphoma

(2009) Carolyn D. Seib et al.   JOURNAL OF CLINICAL ONCOLOGY

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

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

(2008) C. Montagut et al.   CANCER RESEARCH

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