KRAS is vulnerable to reversible switch-II pocket engagement in cells

KRAS secondary mutations that confer acquired resistance to KRAS G12C inhibitors, sotorasib and adagrasib, and overcoming strategies: insights from the in vitro experiments

(2021) Takamasa Koga et al.   Journal of Thoracic Oncology

Selective and noncovalent targeting of RAS mutants for inhibition and degradation

(2021) Kai Wen Teng et al.   Nature Communications

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

Development of a High-throughput NanoBRET Screening Platform to Identify Modulators of the RAS/RAF Interaction

(2021) David E. Durrant et al.   MOLECULAR CANCER THERAPEUTICS

Acquired Resistance to KRASG12C Inhibition in Cancer

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

Drugging the Undruggable: Advances on RAS Targeting in Cancer

(2021) Miriam Molina-Arcas et al.   Genes

The small molecule BI-2852 induces a nonfunctional dimer of KRAS

(2020) Timothy H. Tran et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer

(2020) Jay B. Fell et al.   JOURNAL OF MEDICINAL CHEMISTRY

Analysis of RAS protein interactions in living cells reveals a mechanism for pan-RAS depletion by membrane-targeted RAS binders

(2020) Yao-Cheng Li et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Quantifying CDK inhibitor selectivity in live cells

(2020) Carrow I. Wells et al.   Nature Communications

RAS-targeted therapies: is the undruggable drugged?

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

Real-Time In-Cell NMR Reveals the Intracellular Modulation of GTP-Bound Levels of RAS

(2020) Qingci Zhao et al.   Cell Reports

GTP-State-Selective Cyclic Peptide Ligands of K-Ras(G12D) Block Its Interaction with Raf

(2020) Ziyang Zhang et al.   ACS Central Science

Exquisitely Specific anti-KRAS Biodegraders Inform on the Cellular Prevalence of Nucleotide-Loaded States

(2020) Shuhui Lim et al.   ACS Central Science

Drugging an undruggable pocket on KRAS

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

1H, 15N backbone assignment and comparative analysis of the wild type and G12C, G12D, G12V mutants of K-Ras bound to GDP at physiological pH

(2019) Gyula Pálfy et al.   Biomolecular NMR Assignments

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

(2019) Jude Canon et al.   NATURE

Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors

(2019) Brian A. Lanman et al.   JOURNAL OF MEDICINAL CHEMISTRY

Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor

(2018) Matthew R. Janes et al.   CELL

The reactivity-driven biochemical mechanism of covalent KRASG12C inhibitors

(2018) Rasmus Hansen et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

The reactivity-driven biochemical mechanism of covalent KRASG12C inhibitors

(2018) Rasmus Hansen et al.   NATURE STRUCTURAL & MOLECULAR BIOLOGY

Crystal Structure of a Human K-Ras G12D Mutant in Complex with GDP and the Cyclic Inhibitory Peptide KRpep-2d

(2017) Satoshi Sogabe et al.   ACS Medicinal Chemistry Letters

CcpNmr AnalysisAssign: a flexible platform for integrated NMR analysis

(2016) Simon P. Skinner et al.   JOURNAL OF BIOMOLECULAR NMR

Direct small-molecule inhibitors of KRAS: from structural insights to mechanism-based design

(2016) Jonathan M. L. Ostrem et al.   NATURE REVIEWS DRUG DISCOVERY

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

(2016) P. Lito et al.   SCIENCE

Selective Inhibition of Oncogenic KRAS Output with Small Molecules Targeting the Inactive State

(2016) M. P. Patricelli et al.   Cancer Discovery

NanoLuc Complementation Reporter Optimized for Accurate Measurement of Protein Interactions in Cells

(2015) Andrew S. Dixon et al.   ACS Chemical Biology

Biochemical and Structural Analysis of Common Cancer-Associated KRAS Mutations

(2015) J. C. Hunter et al.   MOLECULAR CANCER RESEARCH

Seeing is believing: Ras dimers observed in live cells: Fig. 1.

(2015) Mark R. Philips et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Ras-GTP dimers activate the Mitogen-Activated Protein Kinase (MAPK) pathway

(2015) Xiaolin Nan et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Target engagement and drug residence time can be observed in living cells with BRET

(2015) Matthew B. Robers et al.   Nature Communications

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

(2013) Jonathan M. Ostrem et al.   NATURE

NMR-based functional profiling of RASopathies and oncogenic RAS mutations

(2013) M. J. Smith et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

Organization, dynamics, and segregation of Ras nanoclusters in membrane domains

(2012) L. Janosi et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Assignments of backbone 1H, 13C and 15N resonances in H-Ras (1–166) complexed with GppNHp at physiological pH

(2011) Casey O’Connor et al.   Biomolecular NMR Assignments