Discovery of potent SOS1 inhibitors that block RAS activation via disruption of the RAS–SOS1 interaction

High-throughput screening identifies small molecules that bind to the RAS:SOS:RAS complex and perturb RAS signaling

(2018) Michael C. Burns et al.   ANALYTICAL BIOCHEMISTRY

Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor

(2018) Matthew R. Janes et al.   CELL

Small Molecule–Mediated Activation of RAS Elicits Biphasic Modulation of Phospho-ERK Levels that Are Regulated through Negative Feedback on SOS1

(2018) Jennifer E. Howes et al.   MOLECULAR CANCER THERAPEUTICS

Latest Advances Towards Ras Inhibition: A Medicinal Chemistry Perspective

(2016) Brice Sautier et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

RAS isoforms and mutations in cancer at a glance

(2016) G. Aaron Hobbs et al.   JOURNAL OF CELL SCIENCE

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

XDSAPP2.0

(2016) Karine M. Sparta et al.   JOURNAL OF APPLIED CRYSTALLOGRAPHY

Small Molecule Binding Sites on the Ras:SOS Complex Can Be Exploited for Inhibition of Ras Activation

(2015) Jon J. G. Winter et al.   JOURNAL OF MEDICINAL CHEMISTRY

Biochemical and Structural Analysis of Common Cancer-Associated KRAS Mutations

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

Direct inhibition of oncogenic KRAS by hydrocarbon-stapled SOS1 helices

(2015) Elizaveta S. Leshchiner et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

Identification and characterization of essential genes in the human genome

(2015) T. Wang et al.   SCIENCE

Dragging Ras Back in the Ring

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

Rational Design of Small Molecule Inhibitors Targeting the Ras GEF, SOS1

(2014) Chris R. Evelyn et al.   CHEMISTRY & BIOLOGY

Drugging the undruggable RAS: Mission Possible?

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

Approach for targeting Ras with small molecules that activate SOS-mediated nucleotide exchange

(2014) Michael C. Burns et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

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

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

REFMAC5 for the refinement of macromolecular crystal structures

(2011) Garib N. Murshudov et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Overview of theCCP4 suite and current developments

(2011) Martyn D. Winn et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Novel Substituted Quinazolines for Potent EGFR Tyrosine Kinase Inhibitors

(2011) O. Cruz-Lopez et al.   CURRENT MEDICINAL CHEMISTRY

An orthosteric inhibitor of the Ras-Sos interaction

(2011) Anupam Patgiri et al.   Nature Chemical Biology

XDS

(2010) Wolfgang Kabsch   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Features and development ofCoot

(2010) P. Emsley et al.   ACTA CRYSTALLOGRAPHICA SECTION D-BIOLOGICAL CRYSTALLOGRAPHY

Drug Combination Studies and Their Synergy Quantification Using the Chou-Talalay Method

(2010) T.-C. Chou   CANCER RESEARCH