KRASG12C-independent feedback activation of wild-type RAS constrains KRASG12C inhibitor efficacy

Encorafenib Plus Cetuximab as a New Standard of Care for Previously Treated BRAF V600E–Mutant Metastatic Colorectal Cancer: Updated Survival Results and Subgroup Analyses from the BEACON Study

(2021) Josep Tabernero et al.   JOURNAL OF CLINICAL ONCOLOGY

99O_PR KRYSTAL-1: Activity and preliminary pharmacodynamic (PD) analysis of adagrasib (MRTX849) in patients (Pts) with advanced non–small cell lung cancer (NSCLC) harboring KRASG12C mutation

(2021) G.J. Riely et al.   Journal of Thoracic Oncology

Clinical acquired resistance to KRASG12C inhibition through a novel KRAS switch-II pocket mutation and polyclonal alterations converging on RAS-MAPK reactivation

(2021) Noritaka Tanaka et al.   Cancer Discovery

LBA6 KRYSTAL-1: Adagrasib (MRTX849) as monotherapy or combined with cetuximab (Cetux) in patients (Pts) with colorectal cancer (CRC) harboring a KRASG12C mutation

(2021) J. Weiss et al.   ANNALS OF ONCOLOGY

434P CodeBreaK 101 subprotocol H: Phase Ib study evaluating combination of sotorasib (Soto), a KRASG12C inhibitor, and panitumumab (PMab), an EGFR inhibitor, in advanced KRAS p.G12C-mutated colorectal cancer (CRC)

(2021) M. Fakih et al.   ANNALS OF ONCOLOGY

Overall survival and exploratory subgroup analyses from the phase 2 CodeBreaK 100 trial evaluating sotorasib in pretreated KRAS p.G12C mutated non-small cell lung cancer.

(2021) Ferdinandos Skoulidis et al.   JOURNAL OF CLINICAL ONCOLOGY

Acquired Resistance to KRASG12C Inhibition in Cancer

(2021) Mark M. Awad et al.   NEW ENGLAND JOURNAL OF MEDICINE

Oncogenic KRAS engages an RSK1/NF1 pathway to inhibit wild-type RAS signaling in pancreatic cancer

(2021) Derek K. Cheng et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Sotorasib for previously treated colorectal cancers with KRASG12C mutation (CodeBreaK100): a prespecified analysis of a single-arm, phase 2 trial

(2021) Marwan G Fakih et al.   LANCET ONCOLOGY

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

(2020) Jenny Y. Xue et al.   NATURE

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

Targeting KRAS(G12C): From Inhibitory Mechanism to Modulation of Antitumor Effects in Patients

(2020) Dongsung Kim et al.   CELL

KRYSTAL-1: Activity and Safety of Adagrasib (MRTX849) in Patients with Colorectal Cancer (CRC) and Other Solid Tumors Harboring a KRAS G12C Mutation

(2020) M.L. Johnson et al.   EUROPEAN JOURNAL OF CANCER

SHP2 inhibition diminishes KRASG12C cycling and promotes tumor microenvironment remodeling

(2020) Carmine Fedele et al.   JOURNAL OF EXPERIMENTAL MEDICINE

KRASG12C Inhibition with Sotorasib in Advanced Solid Tumors

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

KRASG12C inhibition produces a driver-limited state revealing collateral dependencies

(2019) Kevin Lou et al.   Science Signaling

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

Vertical pathway inhibition overcomes adaptive feedback resistance to KRASG12C inhibition

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

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

Convergent Therapeutic Strategies to Overcome the Heterogeneity of Acquired Resistance in BRAF V600E Colorectal Cancer

(2018) Mehlika Hazar-Rethinam et al.   Cancer Discovery

Combined BRAF, EGFR, and MEK Inhibition in Patients with BRAF V600E -Mutant Colorectal Cancer

(2018) Ryan B. Corcoran et al.   Cancer Discovery

KRAS G12C NSCLC Models Are Sensitive to Direct Targeting of KRAS in Combination with PI3K Inhibition

(2018) Sandra Misale et al.   CLINICAL CANCER RESEARCH

Therapeutic strategies to target RAS-mutant cancers

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

Modeling of Patient-Derived Xenografts in Colorectal Cancer

(2017) Anastasia Katsiampoura et al.   MOLECULAR CANCER THERAPEUTICS

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

(2016) P. Lito et al.   SCIENCE

The role of wild type RAS isoforms in cancer

(2016) Bingying Zhou et al.   SEMINARS IN CELL & DEVELOPMENTAL BIOLOGY

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

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

Drugging the undruggable RAS: Mission Possible?

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

Patient-derived models of acquired resistance can identify effective drug combinations for cancer

(2014) Adam S. Crystal et al.   SCIENCE

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

(2013) Jonathan M. Ostrem et al.   NATURE

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

(2012) Anirudh Prahallad et al.   NATURE

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

Oncogenic and Wild-type Ras Play Divergent Roles in the Regulation of Mitogen-Activated Protein Kinase Signaling

(2012) Amy Young et al.   Cancer Discovery

Identification of Optimal Drug Combinations Targeting Cellular Networks: Integrating Phospho-Proteomics and Computational Network Analysis

(2010) S. Iadevaia et al.   CANCER RESEARCH