Stamping out RAF and MEK1/2 to inhibit the ERK1/2 pathway: an emerging threat to anticancer therapy
Published 2015 View Full Article
- Home
- Publications
- Publication Search
- Publication Details
Title
Stamping out RAF and MEK1/2 to inhibit the ERK1/2 pathway: an emerging threat to anticancer therapy
Authors
Keywords
-
Journal
ONCOGENE
Volume 35, Issue 20, Pages 2547-2561
Publisher
Springer Nature
Online
2015-09-14
DOI
10.1038/onc.2015.329
References
Ask authors/readers for more resources
Related references
Note: Only part of the references are listed.- Paradox-Breaking RAF Inhibitors that Also Target SRC Are Effective in Drug-Resistant BRAF Mutant Melanoma
- (2015) Maria Romina Girotti et al. CANCER CELL
- Regulation of RAF protein kinases in ERK signalling
- (2015) Hugo Lavoie et al. NATURE REVIEWS MOLECULAR CELL BIOLOGY
- Potential Therapeutic Strategies to Overcome Acquired Resistance to BRAF or MEK Inhibitors in BRAF Mutant Cancers
- (2015) Ryan B. Corcoran et al. Oncotarget
- Intrinsic and acquired resistance to MEK1/2 inhibitors in cancer
- (2014) Matthew J. Sale et al. BIOCHEMICAL SOCIETY TRANSACTIONS
- Disruption of CRAF-Mediated MEK Activation Is Required for Effective MEK Inhibition in KRAS Mutant Tumors
- (2014) Piro Lito et al. CANCER CELL
- Abstract 2337: Efficacy of the RAF/PI3Kα/anti-EGFR triple combination LGX818 + BYL719 + cetuximab in BRAFV600Ecolorectal tumor models.
- (2014) Giordano Caponigro et al. CANCER RESEARCH
- BRAF Inhibitor Resistance Mechanisms in Metastatic Melanoma: Spectrum and Clinical Impact
- (2014) H. Rizos et al. CLINICAL CANCER RESEARCH
- Dabrafenib and Trametinib, Alone and in Combination for BRAF-Mutant Metastatic Melanoma
- (2014) A. M. Menzies et al. CLINICAL CANCER RESEARCH
- Phase I study of XL281 (BMS-908662), a potent oral RAF kinase inhibitor, in patients with advanced solid tumors
- (2014) Mark A. Dickson et al. INVESTIGATIONAL NEW DRUGS
- Novel ATP-Competitive MEK Inhibitor E6201 Is Effective against Vemurafenib-Resistant Melanoma Harboring the MEK1-C121S Mutation in a Preclinical Model
- (2014) Y. Narita et al. MOLECULAR CANCER THERAPEUTICS
- The clinical development of MEK inhibitors
- (2014) Yujie Zhao et al. Nature Reviews Clinical Oncology
- Rasfonin, a novel 2-pyrone derivative, induces ras-mutated Panc-1 pancreatic tumor cell death in nude mice
- (2014) Z Xiao et al. Cell Death & Disease
- 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
- A phase I dose-finding, safety and tolerability study of AZD8330 in patients with advanced malignancies
- (2013) Roger B. Cohen et al. EUROPEAN JOURNAL OF CANCER
- Antitumor activity of pimasertib, a selective MEK 1/2 inhibitor, in combination with PI3K/mTOR inhibitors or with multi-targeted kinase inhibitors in pimasertib-resistant human lung and colorectal cancer cells
- (2013) Erika Martinelli et al. INTERNATIONAL JOURNAL OF CANCER
- Pharmacodynamic Effects and Mechanisms of Resistance to Vemurafenib in Patients With Metastatic Melanoma
- (2013) Kerstin Trunzer et al. JOURNAL OF CLINICAL ONCOLOGY
- MEK and the inhibitors: from bench to bedside
- (2013) Akintunde Akinleye et al. Journal of Hematology & Oncology
- B-Raf and the inhibitors: from bench to bedside
- (2013) Tiangui Huang et al. Journal of Hematology & Oncology
- MEK162 for patients with advanced melanoma harbouring NRAS or Val600 BRAF mutations: a non-randomised, open-label phase 2 study
- (2013) Paolo A Ascierto et al. LANCET ONCOLOGY
- pERK 1/2 inhibit Caspase-8 induced apoptosis in cancer cells by phosphorylating it in a cell cycle specific manner
- (2013) Ranadip Mandal et al. Molecular Oncology
- Small molecule inhibition of the KRAS–PDEδ interaction impairs oncogenic KRAS signalling
- (2013) Gunther Zimmermann et al. NATURE
- Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancers
- (2013) Georgia Hatzivassiliou et al. NATURE
- Drug for an 'undruggable' protein
- (2013) Nicole M. Baker et al. NATURE
- BRAF inhibitors in cancer therapy
- (2013) Carolina Hertzman Johansson et al. PHARMACOLOGY & THERAPEUTICS
- Andrographolide derivatives inhibit guanine nucleotide exchange and abrogate oncogenic Ras function
- (2013) H. J. Hocker et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- MEK inhibitors as a chemotherapeutic intervention in multiple myeloma
- (2013) C Chang-Yew Leow et al. Blood Cancer Journal
- Concurrent MEK2 Mutation and BRAF Amplification Confer Resistance to BRAF and MEK Inhibitors in Melanoma
- (2013) Jessie Villanueva et al. Cell Reports
- Tumour cell responses to MEK1/2 inhibitors: acquired resistance and pathway remodelling
- (2012) Annette S. Little et al. BIOCHEMICAL SOCIETY TRANSACTIONS
- Abstract 3790: Preclinical profile of LGX818: A potent and selective RAF kinase inhibitor
- (2012) Darrin D. Stuart et al. CANCER RESEARCH
- Abstract 3739: TAK-733, an investigational, selective MEK1/2 inhibitor, in combination with alisertib (MLN8237), an investigational, selective Aurora A kinase inhibitor is tolerated and results in additive to synergistic antitumor activity: Results from In Vivo Studies
- (2012) Robyn Fabrey et al. CANCER RESEARCH
- Abstract 3738: A rationale for combining the targeted investigational agents TAK-733, a MEK1/2 inhibitor, with alisertib (MLN8237), an Aurora A kinase inhibitor, for cancer therapy
- (2012) Sabrina Collins et al. CANCER RESEARCH
- Receptor tyrosine kinases in cancer escape from BRAF inhibitors
- (2012) Roger S Lo CELL RESEARCH
- Phase I Dose-Escalation Study of the Safety, Pharmacokinetics, and Pharmacodynamics of the MEK Inhibitor RO4987655 (CH4987655) in Patients with Advanced Solid Tumors
- (2012) S. Leijen et al. CLINICAL CANCER RESEARCH
- RAF265 Inhibits the Growth of Advanced Human Melanoma Tumors
- (2012) Y. Su et al. CLINICAL CANCER RESEARCH
- First-in-Human, Phase I Dose-Escalation Study of the Safety, Pharmacokinetics, and Pharmacodynamics of RO5126766, a First-in-Class Dual MEK/RAF Inhibitor in Patients with Solid Tumors
- (2012) M. Martinez-Garcia et al. CLINICAL CANCER RESEARCH
- 358 A Multi-arm Phase 1 Dose Escalation Study of Safety, Pharmacokinetics, and Pharmacodynamics of the Dual PI3K/mTOR Inhibitors PF-04691502 (oral) and PF-05212384 (IV) in Combination with the MEK Inhibitor PD-0325901 or Irinotecan in Patients with Advanced Cancer
- (2012) C. Britten et al. EUROPEAN JOURNAL OF CANCER
- Tumour micro-environment elicits innate resistance to RAF inhibitors through HGF secretion
- (2012) Ravid Straussman et al. NATURE
- Vemurafenib: the first drug approved for BRAF-mutant cancer
- (2012) Gideon Bollag et al. NATURE REVIEWS DRUG DISCOVERY
- Mechanisms of acquired resistance to ERK1/2 pathway inhibitors
- (2012) A S Little et al. ONCOGENE
- Small-molecule ligands bind to a distinct pocket in Ras and inhibit SOS-mediated nucleotide exchange activity
- (2012) T. Maurer et al. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
- Mutant BRAF Melanomas—Dependence and Resistance
- (2011) Poulikos I. Poulikakos et al. CANCER CELL
- Resistance to BRAF Inhibitors: Unraveling Mechanisms and Future Treatment Options
- (2011) J. Villanueva et al. CANCER RESEARCH
- Vemurafenib and BRAF Inhibition: A New Class of Treatment for Metastatic Melanoma
- (2011) J. J. Luke 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
- Dissecting Therapeutic Resistance to RAF Inhibition in Melanoma by Tumor Genomic Profiling
- (2011) Nikhil Wagle et al. JOURNAL OF CLINICAL ONCOLOGY
- Future perspectives in melanoma research. Meeting report from the "Melanoma Research: a bridge Naples-USA. Naples, December 6th-7 th2010"
- (2011) Paolo A Ascierto et al. Journal of Translational Medicine
- Activation and Function of the MAPKs and Their Substrates, the MAPK-Activated Protein Kinases
- (2011) M. Cargnello et al. MICROBIOLOGY AND MOLECULAR BIOLOGY REVIEWS
- BRAFV600E: Implications for Carcinogenesis and Molecular Therapy
- (2011) E. R. Cantwell-Dorris et al. MOLECULAR CANCER THERAPEUTICS
- Comprehensive Predictive Biomarker Analysis for MEK Inhibitor GSK1120212
- (2011) J. Jing et al. MOLECULAR CANCER THERAPEUTICS
- RAF inhibitor resistance is mediated by dimerization of aberrantly spliced BRAF(V600E)
- (2011) Poulikos I. Poulikakos et al. NATURE
- 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
- Functional and molecular interactions between ERK and CHK2 in diffuse large B-cell lymphoma
- (2011) Bojie Dai et al. Nature Communications
- The Raf Inhibitor Paradox: Unexpected Consequences of Targeted Drugs
- (2010) Adrienne D. Cox 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
- Kinase-Dead BRAF and Oncogenic RAS Cooperate to Drive Tumor Progression through CRAF
- (2010) Sonja J. Heidorn et al. CELL
- Phase II Clinical Trial of Sorafenib in Metastatic Medullary Thyroid Cancer
- (2010) Elaine T. Lam et al. JOURNAL OF CLINICAL ONCOLOGY
- From basic research to clinical development of MEK1/2 inhibitors for cancer therapy
- (2010) Christophe Frémin et al. Journal of Hematology & Oncology
- Identification of Predictive Markers of Response to the MEK1/2 Inhibitor Selumetinib (AZD6244) in K-ras-Mutated Colorectal Cancer
- (2010) J. J. Tentler et al. MOLECULAR CANCER THERAPEUTICS
- 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
- COT drives resistance to RAF inhibition through MAP kinase pathway reactivation
- (2010) Cory M. Johannessen et al. NATURE
- 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
- 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
- ERK-1 MAP kinase prevents TNF-induced apoptosis through bad phosphorylation and inhibition of Bax translocation in HeLa Cells
- (2009) Bruna Pucci et al. JOURNAL OF CELLULAR BIOCHEMISTRY
- MAPK signaling pathways in the regulation of hematopoiesis
- (2009) Christian R. Geest et al. JOURNAL OF LEUKOCYTE BIOLOGY
- Impact of Feedback Phosphorylation and Raf Heterodimerization on Normal and Mutant B-Raf Signaling
- (2009) D. A. Ritt et al. MOLECULAR AND CELLULAR BIOLOGY
- KRAS/BRAF mutation status and ERK1/2 activation as biomarkers for MEK1/2 inhibitor therapy in colorectal cancer
- (2009) J. J. Yeh et al. MOLECULAR CANCER THERAPEUTICS
- Negative Regulation of the EGFR-MAPK Cascade by Actin-MAL-Mediated Mig6/Errfi-1 Induction
- (2009) Arnaud Descot 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
- Advances in Targeting the Ras/Raf/MEK/Erk Mitogen-Activated Protein Kinase Cascade with MEK Inhibitors for Cancer Therapy
- (2008) B. B. Friday et al. CLINICAL CANCER RESEARCH
- The regulation of extracellular signal-regulated kinase (ERK) in mammalian cells
- (2008) Joe W. Ramos INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY
- Phase I Pharmacokinetic and Pharmacodynamic Study of the Oral, Small-Molecule Mitogen-Activated Protein Kinase Kinase 1/2 Inhibitor AZD6244 (ARRY-142886) in Patients With Advanced Cancers
- (2008) Alex A. Adjei et al. JOURNAL OF CLINICAL ONCOLOGY
- Adaptor SKAP-55 Binds p21ras Activating Exchange Factor RasGRP1 and Negatively Regulates the p21ras-ERK Pathway in T-Cells
- (2008) Helga Schneider et al. PLoS One
- 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
Add your recorded webinar
Do you already have a recorded webinar? Grow your audience and get more views by easily listing your recording on Peeref.
Upload NowAsk a Question. Answer a Question.
Quickly pose questions to the entire community. Debate answers and get clarity on the most important issues facing researchers.
Get Started