The ERK mitogen-activated protein kinase signaling network: the final frontier in RAS signal transduction

Cancer statistics, 2020

(2020) Rebecca L. Siegel et al.   CA-A CANCER JOURNAL FOR CLINICIANS

Pulsatile MAPK Signaling Modulates p53 Activity to Control Cell Fate Decisions at the G2 Checkpoint for DNA Damage

(2020) Siddharth De et al.   Cell Reports

Germline and sporadic cancers driven by the RAS pathway: parallels and contrasts

(2020) V. Dunnett-Kane et al.   ANNALS OF ONCOLOGY

EGFR blockade reverts resistance to KRAS G12C inhibition in colorectal cancer

(2020) Vito Amodio et al.   Cancer Discovery

Disentangling Pro-mitotic Signaling during Cell Cycle Progression using Time-Resolved Single-Cell Imaging

(2020) Manuela Benary et al.   Cell Reports

Signaling diversity enabled by Rap1-regulated plasma membrane ERK with distinct temporal dynamics

(2020) Jeremiah Keyes et al.   eLife

A Live-Cell Screen for Altered Erk Dynamics Reveals Principles of Proliferative Control

(2020) Alexander G. Goglia et al.   Cell Systems

RAS-targeted therapies: is the undruggable drugged?

(2020) Amanda R. Moore et al.   NATURE REVIEWS DRUG DISCOVERY

Multiple low dose therapy as an effective strategy to treat EGFR inhibitor-resistant NSCLC tumours

(2020) João M. Fernandes Neto et al.   Nature Communications

Low-Dose Vertical Inhibition of the RAF-MEK-ERK Cascade Causes Apoptotic Death of KRAS Mutant Cancers

(2020) Irem Ozkan-Dagliyan et al.   Cell Reports

Identification of TNO155, an Allosteric SHP2 Inhibitor for the Treatment of Cancer

(2020) Matthew J. LaMarche et al.   JOURNAL OF MEDICINAL CHEMISTRY

BI-3406, a potent and selective SOS1::KRAS interaction inhibitor, is effective in KRAS-driven cancers through combined MEK inhibition

(2020) Marco H Hofmann et al.   Cancer Discovery

MAP kinase and autophagy pathways cooperate to maintain RAS mutant cancer cell survival

(2019) Chih-Shia Lee et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Protective autophagy elicited by RAF→MEK→ERK inhibition suggests a treatment strategy for RAS-driven cancers

(2019) Conan G. Kinsey et al.   NATURE MEDICINE

Combination of ERK and autophagy inhibition as a treatment approach for pancreatic cancer

(2019) Kirsten L. Bryant et al.   NATURE MEDICINE

Nuclear ERK: Mechanism of Translocation, Substrates, and Role in Cancer

(2019) Galia Maik-Rachline et al.   INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES

Cell type-dependent differential activation of ERK by oncogenic KRAS in colon cancer and intestinal epithelium

(2019) Raphael Brandt et al.   Nature Communications

Encorafenib, Binimetinib, and Cetuximab in BRAF V600E–Mutated Colorectal Cancer

(2019) Scott Kopetz et al.   NEW ENGLAND JOURNAL OF MEDICINE

Development of combination therapies to maximize the impact of KRAS-G12C inhibitors in lung cancer

(2019) Miriam Molina-Arcas et al.   Science Translational Medicine

Drp1 Promotes KRas-Driven Metabolic Changes to Drive Pancreatic Tumor Growth

(2019) Sarbajeet Nagdas et al.   Cell Reports

Vertical pathway inhibition overcomes adaptive feedback resistance to KRASG12C inhibition

(2019) Meagan B. Ryan et al.   CLINICAL CANCER RESEARCH

The clinical KRAS(G12C) inhibitor AMG 510 drives anti-tumour immunity

(2019) Jude Canon et al.   NATURE

The KRASG12C Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients

(2019) Jill Hallin et al.   Cancer Discovery

c-RAF Ablation Induces Regression of Advanced Kras/Trp 53 Mutant Lung Adenocarcinomas by a Mechanism Independent of MAPK Signaling

(2018) Manuel Sanclemente et al.   CANCER CELL

ERK regulates mitochondrial membrane potential in fission deficient Drosophila follicle cells during differentiation

(2018) Darshika Tomer et al.   DEVELOPMENTAL BIOLOGY

Ras-Mediated Activation of the Raf Family Kinases

(2018) Elizabeth M. Terrell et al.   Cold Spring Harbor Perspectives in Medicine

SPRINT: Phase II study of the MEK 1/2 inhibitor selumetinib (AZD6244, ARRY-142886) in children with neurofibromatosis type 1 (NF1) and inoperable plexiform neurofibromas (PN).

(2018) Andrea M. Gross et al.   JOURNAL OF CLINICAL ONCOLOGY

Hyperactivation of MAPK Signaling is Deleterious to RAS/RAF Mutant Melanoma

(2018) Grace P Leung et al.   MOLECULAR CANCER RESEARCH

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

(2018) Ivana Yen et al.   CANCER CELL

Genetically Encoded Fluorescent Biosensors Illuminate the Spatiotemporal Regulation of Signaling Networks

(2018) Eric C. Greenwald et al.   CHEMICAL REVIEWS

Therapeutic strategies to target RAS-mutant cancers

(2018) Meagan B. Ryan et al.   Nature Reviews Clinical Oncology

Integrating chemical and mechanical signals through dynamic coupling between cellular protrusions and pulsed ERK activation

(2018) Jr-Ming Yang et al.   Nature Communications

ER translocation of the MAPK pathway drives therapy resistance in BRAF mutant melanoma

(2018) Rani Ojha et al.   Cancer Discovery

Hyperactivation of ERK by multiple mechanisms is toxic to RTK-RAS mutation-driven lung adenocarcinoma cells

(2018) Arun M Unni et al.   eLife

A compendium of ERK targets

(2017) Evrim B. Ünal et al.   FEBS LETTERS

Selumetinib Plus Docetaxel Compared With Docetaxel Alone and Progression-Free Survival in Patients With KRAS-Mutant Advanced Non–Small Cell Lung Cancer

(2017) Pasi A. Jänne et al.   JAMA-JOURNAL OF THE AMERICAN MEDICAL ASSOCIATION

Time-resolved Phosphoproteome Analysis of Paradoxical RAF Activation Reveals Novel Targets of ERK

(2017) Peter Kubiniok et al.   MOLECULAR & CELLULAR PROTEOMICS

Cancer drug addiction is relayed by an ERK2-dependent phenotype switch

(2017) Xiangjun Kong et al.   NATURE

An approach to suppress the evolution of resistance in BRAFV600E-mutant cancer

(2017) Yaohua Xue et al.   NATURE MEDICINE

Exploiting Drug Addiction Mechanisms to Select against MAPKi-Resistant Melanoma

(2017) Aayoung Hong et al.   Cancer Discovery

Linear Integration of ERK Activity Predominates over Persistence Detection in Fra-1 Regulation

(2017) Taryn E. Gillies et al.   Cell Systems

Combined MEK and ERK inhibition overcomes therapy-mediated pathway reactivation in RAS mutant tumors

(2017) Mark Merchant et al.   PLoS One

Long-Term ERK Inhibition in KRAS-Mutant Pancreatic Cancer Is Associated with MYC Degradation and Senescence-like Growth Suppression

(2016) Tikvah K. Hayes et al.   CANCER CELL

The Emerging Hallmarks of Cancer Metabolism

(2016) Natalya N. Pavlova et al.   Cell Metabolism

Negative feedback regulation of the ERK1/2 MAPK pathway

(2016) David Lake et al.   CELLULAR AND MOLECULAR LIFE SCIENCES

The dynamic subcellular localization of ERK: mechanisms of translocation and role in various organelles

(2016) Ehud Wainstein et al.   CURRENT OPINION IN CELL BIOLOGY

Phosphoproteome analysis of the MAPK pathway reveals previously undetected feedback mechanisms

(2016) Florian Gnad et al.   PROTEOMICS

Opposing effects of Elk-1 multisite phosphorylation shape its response to ERK activation

(2016) A. Mylona et al.   SCIENCE

Allele-specific inhibitors inactivate mutant KRAS G12C by a trapping mechanism

(2016) P. Lito et al.   SCIENCE

A randomized phase II study of the MEK1/MEK2 inhibitor trametinib (GSK1120212) compared with docetaxel in KRAS-mutant advanced non-small-cell lung cancer (NSCLC)†

(2015) G. R. Blumenschein et al.   ANNALS OF ONCOLOGY

Tunable-Combinatorial Mechanisms of Acquired Resistance Limit the Efficacy of BRAF/MEK Cotargeting but Result in Melanoma Drug Addiction

(2015) Gatien Moriceau et al.   CANCER CELL

A phase I/Ib study of trametinib (GSK1120212) alone and in combination with gemcitabine in Japanese patients with advanced solid tumors

(2015) Akiyoshi Kasuga et al.   INVESTIGATIONAL NEW DRUGS

Receptor Level Mechanisms Are Required for Epidermal Growth Factor (EGF)-stimulated Extracellular Signal-regulated Kinase (ERK) Activity Pulses

(2015) Breanne Sparta et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A Phosphoproteomic Comparison of B-RAFV600Eand MKK1/2 Inhibitors in Melanoma Cells

(2015) Scott A. Stuart et al.   MOLECULAR & CELLULAR PROTEOMICS

Combination of pan-RAF and MEK inhibitors in NRAS mutant melanoma

(2015) Mohammad Atefi et al.   Molecular Cancer

Mitochondrial Division Is Requisite to RAS-Induced Transformation and Targeted by Oncogenic MAPK Pathway Inhibitors

(2015) Madhavika N. Serasinghe et al.   MOLECULAR CELL

Improved Overall Survival in Melanoma with Combined Dabrafenib and Trametinib

(2015) Caroline Robert et al.   NEW ENGLAND JOURNAL OF MEDICINE

Oncogene-induced senescence underlies the mutual exclusive nature of oncogenic KRAS and BRAF

(2015) J Cisowski et al.   ONCOGENE

ERK reinforces actin polymerization to power persistent edge protrusion during motility

(2015) Michelle C. Mendoza et al.   Science Signaling

The nuclear translocation of ERK1/2 as an anticancer target

(2015) Alexander Plotnikov et al.   Nature Communications

Evidence that synthetic lethality underlies the mutual exclusivity of oncogenic KRAS and EGFR mutations in lung adenocarcinoma

(2015) Arun M Unni et al.   eLife

ERK reinforces actin polymerization to power persistent edge protrusion during motility

(2015) Michelle C. Mendoza et al.   Science Signaling

Phosphoproteomic Analysis of Cell-Based Resistance to BRAF Inhibitor Therapy in Melanoma

(2015) Robert Parker et al.   Frontiers in Oncology

Novel Reporter for Faithful Monitoring of ERK2 Dynamics in Living Cells and Model Organisms

(2015) François Sipieter et al.   PLoS One

High-Sensitivity Measurements of Multiple Kinase Activities in Live Single Cells

(2014) Sergi Regot et al.   CELL

Combined MEK and PI3K Inhibition in a Mouse Model of Pancreatic Cancer

(2014) B. Alagesan et al.   CLINICAL CANCER RESEARCH

Antitumor Activity in RAS-Driven Tumors by Blocking AKT and MEK

(2014) A. W. Tolcher et al.   CLINICAL CANCER RESEARCH

A randomised, double-blind, placebo-controlled trial of trametinib, an oral MEK inhibitor, in combination with gemcitabine for patients with untreated metastatic adenocarcinoma of the pancreas

(2014) Jeffrey R. Infante et al.   EUROPEAN JOURNAL OF CANCER

Identification of Extracellular Signal-regulated Kinase 1 (ERK1) Direct Substrates using Stable Isotope Labeled Kinase Assay-Linked Phosphoproteomics

(2014) Liang Xue et al.   MOLECULAR & CELLULAR PROTEOMICS

Phosphoproteomics of MAPK Inhibition in BRAF-Mutated Cells and a Role for the Lethal Synergism of Dual BRAF and CK2 Inhibition

(2014) R. Parker et al.   MOLECULAR CANCER THERAPEUTICS

Modeling Targeted Inhibition of MEK and PI3 Kinase in Human Pancreatic Cancer

(2014) M. R. Junttila et al.   MOLECULAR CANCER THERAPEUTICS

Drugging the undruggable RAS: Mission Possible?

(2014) Adrienne D. Cox et al.   NATURE REVIEWS DRUG DISCOVERY

Combined BRAF and MEK Inhibition versus BRAF Inhibition Alone in Melanoma

(2014) Georgina V. Long et al.   NEW ENGLAND JOURNAL OF MEDICINE

Combined Vemurafenib and Cobimetinib in BRAF-Mutated Melanoma

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

Optimization of ERK Activity Biosensors for both Ratiometric and Lifetime FRET Measurements

(2014) Pauline Vandame et al.   SENSORS

RAF Suppression Synergizes with MEK Inhibition in KRAS Mutant Cancer Cells

(2014) Simona Lamba et al.   Cell Reports

Phosphoproteome dynamics reveal novel ERK1/2 MAP kinase substrates with broad spectrum of functions

(2013) M. Courcelles et al.   Molecular Systems Biology

Macropinocytosis of protein is an amino acid supply route in Ras-transformed cells

(2013) Cosimo Commisso et al.   NATURE

Glutamine supports pancreatic cancer growth through a KRAS-regulated metabolic pathway

(2013) Jaekyoung Son et al.   NATURE

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

(2013) Meghna Das Thakur et al.   NATURE

A Versatile Toolkit to Produce Sensitive FRET Biosensors to Visualize Signaling in Time and Space

(2013) R. D. Fritz et al.   Science Signaling

A Comprehensive Survey of Ras Mutations in Cancer

(2012) I. A. Prior et al.   CANCER RESEARCH

The Clinical Effect of the Dual-Targeting Strategy Involving PI3K/AKT/mTOR and RAS/MEK/ERK Pathways in Patients with Advanced Cancer

(2012) T. Shimizu et al.   CLINICAL CANCER RESEARCH

PTMScan Direct: Identification and Quantification of Peptides from Critical Signaling Proteins by Immunoaffinity Enrichment Coupled with LC-MS/MS

(2012) Matthew P. Stokes et al.   MOLECULAR & CELLULAR PROTEOMICS

Frequency-Modulated Pulses of ERK Activity Transmit Quantitative Proliferation Signals

(2012) John G. Albeck et al.   MOLECULAR CELL

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

RASMutations in Cutaneous Squamous-Cell Carcinomas in Patients Treated with BRAF Inhibitors

(2012) Fei Su et al.   NEW ENGLAND JOURNAL OF MEDICINE

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

(2012) Robert Roskoski   PHARMACOLOGICAL RESEARCH

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

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

Pancreatic cancers require autophagy for tumor growth

(2011) S. Yang et al.   GENES & DEVELOPMENT

Activated Ras requires autophagy to maintain oxidative metabolism and tumorigenesis

(2011) J. Y. Guo et al.   GENES & DEVELOPMENT

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

Activation and Function of the MAPKs and Their Substrates, the MAPK-Activated Protein Kinases

(2011) M. Cargnello et al.   MICROBIOLOGY AND MOLECULAR BIOLOGY REVIEWS

Spatiotemporally Regulated Protein Kinase A Activity Is a Critical Regulator of Growth Factor-Stimulated Extracellular Signal-Regulated Kinase Signaling in PC12 Cells

(2011) K. J. Herbst et al.   MOLECULAR AND CELLULAR BIOLOGY

Development of an optimized backbone of FRET biosensors for kinases and GTPases

(2011) Naoki Komatsu et al.   MOLECULAR BIOLOGY OF THE CELL

Two Phases of Mitogenic Signaling Unveil Roles for p53 and EGR1 in Elimination of Inconsistent Growth Signals

(2011) Yaara Zwang et al.   MOLECULAR CELL

ERK-MAPK Drives Lamellipodia Protrusion by Activating the WAVE2 Regulatory Complex

(2011) Michelle C. Mendoza et al.   MOLECULAR CELL

A Two-Dimensional ERK-AKT Signaling Code for an NGF-Triggered Cell-Fate Decision

(2011) Jia-Yun Chen et al.   MOLECULAR CELL

Large-Scale Discovery of ERK2 Substrates Identifies ERK-Mediated Transcriptional Regulation by ETV3

(2011) S. M. Carlson et al.   Science Signaling

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

Gene ontology analysis for RNA-seq: accounting for selection bias

(2010) Matthew D Young et al.   GENOME BIOLOGY

Global Effects of Kinase Inhibitors on Signaling Networks Revealed by Quantitative Phosphoproteomics

(2009) Cuiping Pan et al.   MOLECULAR & CELLULAR PROTEOMICS

Functional Proteomics Identifies Targets of Phosphorylation by B-Raf Signaling in Melanoma

(2009) William M. Old et al.   MOLECULAR CELL

Rapid and sustained nuclear–cytoplasmic ERK oscillations induced by epidermal growth factor

(2009) Harish Shankaran et al.   Molecular Systems Biology

Cell fate decisions are specified by the dynamic ERK interactome

(2009) Alex von Kriegsheim et al.   NATURE CELL BIOLOGY

Phosphoproteomics reveals new ERK MAP kinase targets and links ERK to nucleoporin-mediated nuclear transport

(2009) Hidetaka Kosako et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Understanding the Warburg Effect: The Metabolic Requirements of Cell Proliferation

(2009) M. G. Vander Heiden et al.   SCIENCE

Genetic Predictors of MEK Dependence in Non-Small Cell Lung Cancer

(2008) C. A. Pratilas et al.   CANCER RESEARCH

Active Ras Triggers Death in Glioblastoma Cells through Hyperstimulation of Macropinocytosis

(2008) J. H. Overmeyer et al.   MOLECULAR CANCER RESEARCH

Modelling Myc inhibition as a cancer therapy

(2008) Laura Soucek et al.   NATURE

A genetically encoded fluorescent sensor of ERK activity

(2008) C. D. Harvey et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA