Targeting BRAF and RAS in Colorectal Cancer

Exploiting allosteric properties of RAF and MEK inhibitors to target therapy-resistant tumors driven by oncogenic BRAF signaling

(2021) Christos Adamopoulos et al.   Cancer Discovery

Rapid non-uniform adaptation to conformation-specific KRAS(G12C) inhibition

(2020) Jenny Y. Xue et al.   NATURE

Prognostic and predictive value of the Immunoscore in stage III colon cancer patients treated with oxaliplatin in the prospective IDEA France PRODIGE-GERCOR cohort study

(2020) F. Pagès et al.   ANNALS OF ONCOLOGY

EGFR blockade reverts resistance to KRAS G12C inhibition in colorectal cancer

(2020) Vito Amodio et al.   Cancer Discovery

RAS-targeted therapies: is the undruggable drugged?

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

Individual Patient Data Meta-Analysis of FOLFOXIRI Plus Bevacizumab Versus Doublets Plus Bevacizumab as Initial Therapy of Unresectable Metastatic Colorectal Cancer

(2020) Chiara Cremolini et al.   JOURNAL OF CLINICAL ONCOLOGY

KRASG12C Inhibition with Sotorasib in Advanced Solid Tumors

(2020) David S. Hong et al.   NEW ENGLAND JOURNAL OF MEDICINE

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

Durable Suppression of Acquired MEK Inhibitor Resistance in Cancer by Sequestering MEK from ERK and Promoting Anti-Tumor T-cell Immunity

(2020) Aayoung Hong et al.   Cancer Discovery

Targeting Alterations in the RAF–MEK Pathway

(2019) Rona Yaeger et al.   Cancer Discovery

Explaining the unexplainable: discrepancies in results from the CALGB/SWOG 80405 and FIRE-3 studies

(2019) Dan Aderka et al.   LANCET ONCOLOGY

Mechanisms of Innate and Acquired Resistance to Anti-EGFR therapy: A Review of Current Knowledge with a Focus on Rechallenge Therapies

(2019) Christine M. Parseghian et al.   CLINICAL CANCER RESEARCH

Drugging an undruggable pocket on KRAS

(2019) Dirk Kessler et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Response to Anti-EGFR Therapy in Patients with BRAF non-V600–Mutant Metastatic Colorectal Cancer

(2019) Rona Yaeger et al.   CLINICAL CANCER RESEARCH

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

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

Artificial intelligence-guided tissue analysis combined with immune infiltrate assessment predicts stage III colon cancer outcomes in PETACC08 study

(2019) Cynthia Reichling et al.   GUT

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

Targeting Mutant KRAS for Immunogenic Cell Death Induction

(2019) Lorenzo Galluzzi   TRENDS IN PHARMACOLOGICAL SCIENCES

Signaling pathways involved in colorectal cancer progression

(2019) Zahra Koveitypour et al.   Cell and Bioscience

Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor

(2018) Matthew R. Janes et al.   CELL

The Association Between Mutations in BRAF and Colorectal Cancer–Specific Survival Depends on Microsatellite Status and Tumor Stage

(2018) Hendrik Bläker et al.   Clinical Gastroenterology and Hepatology

Evaluating the Combination of Microsatellite Instability and Mutation in BRAF as Prognostic Factors for Patients With Colorectal Cancer

(2018) Frank A. Sinicrope   Clinical Gastroenterology and Hepatology

International validation of the consensus Immunoscore for the classification of colon cancer: a prognostic and accuracy study

(2018) Franck Pagès et al.   LANCET

Association of Prognostic Value of Primary Tumor Location in Stage III Colon Cancer With RAS and BRAF Mutational Status

(2018) Julien Taieb et al.   JAMA Oncology

Development of small-molecule therapeutics and strategies for targeting RAF kinase in BRAF-mutant colorectal cancer

(2018) Jing-hua Pan et al.   Cancer Management and Research

Prognostic value of the combination of microsatellite instability and BRAF mutation in colorectal cancer

(2018) Yingchi Yang et al.   Cancer Management and Research

β‐Catenin‐RAS interaction serves as a molecular switch for RAS degradation via GSK3β

(2018) Sang‐Kyu Lee et al.   EMBO REPORTS

Non-V600BRAF Mutations Define a Clinically Distinct Molecular Subtype of Metastatic Colorectal Cancer

(2017) Jeremy C. Jones et al.   JOURNAL OF CLINICAL ONCOLOGY

Tumours with class 3 BRAF mutants are sensitive to the inhibition of activated RAS

(2017) Zhan Yao et al.   NATURE

BRAFMutations as Predictive Biomarker for Response to Anti‐EGFR Monoclonal Antibodies

(2017) Emilie M. J. van Brummelen et al.   ONCOLOGIST

DNA methylation epigenotype and clinical features of NRAS -mutation(+) colorectal cancer

(2017) Kiyoko Takane et al.   Cancer Medicine

Prognostic Survival Associated With Left-Sided vs Right-Sided Colon Cancer

(2017) Fausto Petrelli et al.   JAMA Oncology

Epidermal Growth Factor Receptor Cell Proliferation Signaling Pathways

(2017) et al.   Cancers

Randomized, Prospective Evaluation Comparing Intensity of Lymphodepletion Before Adoptive Transfer of Tumor-Infiltrating Lymphocytes for Patients With Metastatic Melanoma

(2016) Stephanie L. Goff et al.   JOURNAL OF CLINICAL ONCOLOGY

Prognostic Value ofBRAF and KRAS Mutations in MSI and MSS Stage III Colon Cancer

(2016) Julien Taieb et al.   JNCI-Journal of the National Cancer Institute

T-Cell Transfer Therapy Targeting Mutant KRAS in Cancer

(2016) Eric Tran et al.   NEW ENGLAND JOURNAL OF MEDICINE

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

(2016) P. Lito et al.   SCIENCE

Molecular pathological classification of colorectal cancer

(2016) Mike F. Müller et al.   VIRCHOWS ARCHIV

Phase IB Study of Vemurafenib in Combination with Irinotecan and Cetuximab in Patients with Metastatic Colorectal Cancer with BRAFV600E Mutation

(2016) D. S. Hong et al.   Cancer Discovery

Prognostic Value ofBRAF and KRAS Mutations in MSI and MSS Stage III Colon Cancer

(2016) Julien Taieb et al.   JNCI-Journal of the National Cancer Institute

Combined Epiregulin and Amphiregulin Expression Levels as a Predictive Biomarker for Panitumumab Therapy Benefit or Lack of Benefit in Patients WithRASWild-Type Advanced Colorectal Cancer

(2016) Jenny F. Seligmann et al.   JAMA Oncology

The RAS-Effector Interface: Isoform-Specific Differences in the Effector Binding Regions

(2016) Hossein Nakhaeizadeh et al.   PLoS One

BRAF Mutants Evade ERK-Dependent Feedback by Different Mechanisms that Determine Their Sensitivity to Pharmacologic Inhibition

(2015) Zhan Yao et al.   CANCER CELL

Predictive role of BRAF mutations in patients with advanced colorectal cancer receiving cetuximab and panitumumab: A meta-analysis

(2015) Filippo Pietrantonio et al.   EUROPEAN JOURNAL OF CANCER

Influence of mRNA expression of epiregulin and amphiregulin on outcome of patients with metastatic colorectal cancer treated with 5-FU/LV plus irinotecan or irinotecan plus oxaliplatin as first-line treatment (FIRE 1-trial)

(2015) A. Stahler et al.   INTERNATIONAL JOURNAL OF CANCER

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

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

Combined BRAF and MEK Inhibition With Dabrafenib and Trametinib in BRAF V600–Mutant Colorectal Cancer

(2015) Ryan B. Corcoran et al.   JOURNAL OF CLINICAL ONCOLOGY

The Worse Prognosis of Right-Sided Compared with Left-Sided Colon Cancers: a Systematic Review and Meta-analysis

(2015) Masashi Yahagi et al.   JOURNAL OF GASTROINTESTINAL SURGERY

The consensus molecular subtypes of colorectal cancer

(2015) Justin Guinney et al.   NATURE MEDICINE

Vemurafenib in Multiple Nonmelanoma Cancers with BRAF V600 Mutations

(2015) David M. Hyman et al.   NEW ENGLAND JOURNAL OF MEDICINE

BRAF V600E mutation and KRAS codon 13 mutations predict poor survival in Chinese colorectal cancer patients

(2014) Jing Chen et al.   BMC CANCER

KRAS Codon 12 and 13 Mutations in Relation to Disease-Free Survival in BRAF-Wild-Type Stage III Colon Cancers from an Adjuvant Chemotherapy Trial (N0147 Alliance)

(2014) H. H. Yoon et al.   CLINICAL CANCER RESEARCH

Identification of susceptibility loci for colorectal cancer in a genome-wide meta-analysis

(2014) N. Whiffin et al.   HUMAN MOLECULAR GENETICS

Role ofNRASmutations as prognostic and predictive markers in metastatic colorectal cancer

(2014) Marta Schirripa et al.   INTERNATIONAL JOURNAL OF CANCER

Panitumumab and irinotecan versus irinotecan alone for patients with KRAS wild-type, fluorouracil-resistant advanced colorectal cancer (PICCOLO): a prospectively stratified randomised trial

(2013) Matthew T Seymour et al.   LANCET ONCOLOGY

K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions

(2013) Jonathan M. Ostrem et al.   NATURE

Panitumumab–FOLFOX4 Treatment and RAS Mutations in Colorectal Cancer

(2013) Jean-Yves Douillard et al.   NEW ENGLAND JOURNAL OF MEDICINE

Molecular basis of MAP kinase regulation

(2013) Wolfgang Peti et al.   PROTEIN SCIENCE

Rare Though Not Mutually Exclusive: A Report of Three Cases of Concomitant KRAS and BRAF Mutation and a Review of the Literature

(2013) Ibrahim Halil Sahin et al.   Journal of Cancer

Predictive value of epidermal growth factor receptor expression for first-line chemotherapy plus cetuximab in patients with head and neck and colorectal cancer: Analysis of data from the EXTREME and CRYSTAL studies

(2012) Lisa Licitra et al.   EUROPEAN JOURNAL OF CANCER

Combined BRAF and MEK Inhibition in Melanoma with BRAF V600 Mutations

(2012) Keith T. Flaherty et al.   NEW ENGLAND JOURNAL OF MEDICINE

Sos-mediated cross-activation of wild-type Ras by oncogenic Ras is essential for tumorigenesis

(2012) Hao-Hsuan Jeng 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

Trends in colorectal cancer incidence: a period and birth-cohort analysis in a well-defined French population

(2011) Marion Chauvenet et al.   BMC CANCER

BRAF mutation is a powerful prognostic factor in advanced and recurrent colorectal cancer

(2011) T Yokota et al.   BRITISH JOURNAL OF CANCER

Increased Detection Sensitivity for KRAS Mutations Enhances the Prediction of Anti-EGFR Monoclonal Antibody Resistance in Metastatic Colorectal Cancer

(2011) F. Molinari et al.   CLINICAL CANCER RESEARCH

Addition of cetuximab to oxaliplatin-based first-line combination chemotherapy for treatment of advanced colorectal cancer: results of the randomised phase 3 MRC COIN trial

(2011) Timothy S Maughan et al.   LANCET

The prognostic impact of anti-cancer immune response: a novel classification of cancer patients

(2011) Gabriela Bindea et al.   Seminars in Immunopathology

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

(2010) Sonja J. Heidorn et al.   CELL

Colorectal cancer molecular biology moves into clinical practice

(2010) C. C. Pritchard et al.   GUT

Randomized, Phase III Trial of Panitumumab With Infusional Fluorouracil, Leucovorin, and Oxaliplatin (FOLFOX4) Versus FOLFOX4 Alone As First-Line Treatment in Patients With Previously Untreated Metastatic Colorectal Cancer: The PRIME Study

(2010) Jean-Yves Douillard et al.   JOURNAL OF CLINICAL ONCOLOGY

Effects of KRAS, BRAF, NRAS, and PIK3CA mutations on the efficacy of cetuximab plus chemotherapy in chemotherapy-refractory metastatic colorectal cancer: a retrospective consortium analysis

(2010) Wendy De Roock et al.   LANCET ONCOLOGY

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

(2010) Poulikos I. Poulikakos et al.   NATURE

KRAS codon 61, 146 and BRAF mutations predict resistance to cetuximab plus irinotecan in KRAS codon 12 and 13 wild-type metastatic colorectal cancer

(2009) F Loupakis et al.   BRITISH JOURNAL OF CANCER

Mucinous histology predicts for poor response rate and overall survival of patients with colorectal cancer and treated with first-line oxaliplatin- and/or irinotecan-based chemotherapy

(2009) V Catalano et al.   BRITISH JOURNAL OF CANCER

Cetuximab and Chemotherapy as Initial Treatment for Metastatic Colorectal Cancer

(2009) Eric Van Cutsem et al.   NEW ENGLAND JOURNAL OF MEDICINE

Hypermethylator Phenotype in Sporadic Colon Cancer: Study on a Population-Based Series of 582 Cases

(2008) L. Barault et al.   CANCER RESEARCH

Proximal and distal colorectal cancers show distinct gene-specific methylation profiles and clinical and molecular characteristics

(2008) Guoren Deng et al.   EUROPEAN JOURNAL OF CANCER