Progress in targeting RAS with small molecule drugs

Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor

(2018) Matthew R. Janes et al.   CELL

Oncogenic Signaling Pathways in The Cancer Genome Atlas

(2018) Francisco Sanchez-Vega et al.   CELL

KRAS: Reasons for optimism in lung cancer

(2018) C.R. Lindsay et al.   EUROPEAN JOURNAL OF CANCER

Novel K-Ras G12C Switch-II Covalent Binders Destabilize Ras and Accelerate Nucleotide Exchange

(2018) Chimno I. Nnadi et al.   Journal of Chemical Information and Modeling

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

Differential Effector Engagement by Oncogenic KRAS

(2018) Tina L. Yuan et al.   Cell Reports

Abstract 4642: Personalized cancer-specific protein corona affects the therapeutic impact of nanoparticles

(2018) Claudia Corbo et al.   CANCER RESEARCH

Small molecule inhibitors of RAS-effector protein interactions derived using an intracellular antibody fragment

(2018) Camilo E. Quevedo et al.   Nature Communications

Nucleoplasmic lamins define growth-regulating functions of lamina-associated polypeptide 2α in progeria cells

(2017) Sandra Vidak et al.   JOURNAL OF CELL SCIENCE

RasIns: Genetically Encoded Intrabodies of Activated Ras Proteins

(2017) Mehmet Cetin et al.   JOURNAL OF MOLECULAR BIOLOGY

Tracking the Evolution of Non–Small-Cell Lung Cancer

(2017) Mariam Jamal-Hanjani et al.   NEW ENGLAND JOURNAL OF MEDICINE

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

Codon bias imposes a targetable limitation on KRAS-driven therapeutic resistance

(2017) Moiez Ali et al.   Nature Communications

Antibody targeting intracellular oncogenic Ras mutants exerts anti-tumour effects after systemic administration

(2017) Seung-Min Shin et al.   Nature Communications

Structural and functional characterization of a DARPin which inhibits Ras nucleotide exchange

(2017) Sandrine Guillard et al.   Nature Communications

Efforts to Develop KRAS Inhibitors

(2017) Matthew Holderfield   Cold Spring Harbor Perspectives in Medicine

Inhibition of prenylated KRAS in a lipid environment

(2017) Johanna M. Jansen et al.   PLoS One

Heterogeneity of KRAS Mutations in Pancreatic Ductal Adenocarcinoma

(2016) Daisuke Hashimoto et al.   PANCREAS

Structural basis of recognition of farnesylated and methylated KRAS4b by PDEδ

(2016) Srisathiyanarayanan Dharmaiah et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

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

K-Ras Promotes Tumorigenicity through Suppression of Non-canonical Wnt Signaling

(2015) Man-Tzu Wang et al.   CELL

Targeting RAS Membrane Association: Back to the Future for Anti-RAS Drug Discovery?

(2015) A. D. Cox et al.   CLINICAL CANCER RESEARCH

K-Ras4A splice variant is widely expressed in cancer and uses a hybrid membrane-targeting motif

(2015) Frederick D. Tsai et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Allosteric Effects of the Oncogenic RasQ61L Mutant on Raf-RBD

(2015) Susan K. Fetics et al.   STRUCTURE

Curation of the Mammalian Palmitoylome Indicates a Pivotal Role for Palmitoylation in Diseases and Disorders of the Nervous System and Cancers

(2015) Shaun S. Sanders et al.   PLoS Computational Biology

Dragging Ras Back in the Ring

(2014) Andrew G. Stephen et al.   CANCER CELL

Yap1 Activation Enables Bypass of Oncogenic Kras Addiction in Pancreatic Cancer

(2014) Avnish Kapoor et al.   CELL

Structure Guided Design and Kinetic Analysis of Highly Potent Benzimidazole Inhibitors Targeting the PDEδ Prenyl Binding Site

(2014) Gunther Zimmermann et al.   JOURNAL OF MEDICINAL CHEMISTRY

Drugging the undruggable RAS: Mission Possible?

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

Therapeutic Targeting of Oncogenic K-Ras by a Covalent Catalytic Site Inhibitor

(2013) Sang Min Lim et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

The RasGAP Gene, RASAL2, Is a Tumor and Metastasis Suppressor

(2013) Sara Koenig McLaughlin et al.   CANCER CELL

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

(2013) Jonathan M. Ostrem et al.   NATURE

Small molecule inhibition of the KRAS–PDEδ interaction impairs oncogenic KRAS signalling

(2013) Gunther Zimmermann et al.   NATURE

Discovery of Small Molecules that Bind to K-Ras and Inhibit Sos-Mediated Activation

(2012) Qi Sun et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

A Comprehensive Survey of Ras Mutations in Cancer

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

Molecular Epidemiology of EGFR and KRAS Mutations in 3,026 Lung Adenocarcinomas: Higher Susceptibility of Women to Smoking-Related KRAS-Mutant Cancers

(2012) S. Dogan et al.   CLINICAL CANCER RESEARCH

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

An orthosteric inhibitor of the Ras-Sos interaction

(2011) Anupam Patgiri et al.   Nature Chemical Biology

K-Ras4B phosphorylation at Ser181 is inhibited by calmodulin and modulates K-Ras activity and function

(2010) B Alvarez-Moya et al.   ONCOGENE

A Gene Expression Signature Associated with “K-Ras Addiction” Reveals Regulators of EMT and Tumor Cell Survival

(2009) Anurag Singh et al.   CANCER CELL

Activated Kras, but Not Hras or Nras, May Initiate Tumors of Endodermal Origin via Stem Cell Expansion

(2008) M. P. Quinlan et al.   MOLECULAR AND CELLULAR BIOLOGY

Kras regulatory elements and exon 4A determine mutation specificity in lung cancer

(2008) Minh D To et al.   NATURE GENETICS

SOS1 mutations are rare in human malignancies: Implications for Noonan syndrome patients

(2007) Kenneth D. Swanson et al.   GENES CHROMOSOMES & CANCER