Targeting KRAS mutant cancers by preventing signaling transduction in the MAPK pathway

KRAS G12C Game of Thrones, which direct KRAS inhibitor will claim the iron throne?

(2020) Misako Nagasaka et al.   CANCER TREATMENT REVIEWS

Targeting the untargetable KRAS in cancer therapy

(2019) Pingyu Liu et al.   Acta Pharmaceutica Sinica B

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

(2019) Roman C. Hillig et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

K-Ras G-domain binding with signaling lipid Phosphatidyl inositol (4,5) phosphate (PIP2): Membrane association, protein orientation and function

(2019) Shufen Cao et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A Potent Isoprenylcysteine Carboxylmethyltransferase (ICMT) Inhibitor Improves Survival in Ras-Driven Acute Myeloid Leukemia

(2019) Nagore I. Marín-Ramos et al.   JOURNAL OF MEDICINAL CHEMISTRY

BRAF inhibitors promote intermediate BRAF(V600E) conformations and binary interactions with activated RAS

(2019) Ruth Röck et al.   Science Advances

Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor

(2018) Matthew R. Janes et al.   CELL

Blocking Ras inhibition as an antitumor strategy

(2018) Nagore I. Marín-Ramos et al.   SEMINARS IN CANCER BIOLOGY

Posttranslational Modifications of RAS Proteins

(2018) Ian Ahearn et al.   Cold Spring Harbor Perspectives in Medicine

Pharmacological targeting of RAS: Recent success with direct inhibitors

(2018) John P. O’Bryan   PHARMACOLOGICAL RESEARCH

Zoledronic acid enhances the efficacy of the MEK inhibitor trametinib in KRAS mutant cancers

(2018) Xinyu Dai et al.   CANCER LETTERS

Inhibition of Isoprenylcysteine Carboxylmethyltransferase Induces Cell-Cycle Arrest and Apoptosis through p21 and p21-Regulated BNIP3 Induction in Pancreatic Cancer

(2017) Kanjoormana Aryan Manu et al.   MOLECULAR CANCER THERAPEUTICS

Implications of farnesyltransferase and its inhibitors as a promising strategy for cancer therapy

(2017) Sergey G. Klochkov et al.   SEMINARS IN CANCER BIOLOGY

Selumetinib with and without erlotinib in KRAS mutant and KRAS wild-type advanced nonsmall-cell lung cancer

(2016) C. A. Carter et al.   ANNALS OF ONCOLOGY

8-Hydroxyquinoline-based inhibitors of the Rce1 protease disrupt Ras membrane localization in human cells

(2016) Idrees Mohammed et al.   BIOORGANIC & MEDICINAL CHEMISTRY

A Small Molecule RAS-Mimetic Disrupts RAS Association with Effector Proteins to Block Signaling

(2016) Sai Krishna Athuluri-Divakar et al.   CELL

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

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

Antitumor effect of manumycin on colorectal cancer cells by increasing the reactive oxygen species production and blocking PI3K-AKT pathway

(2016) Jingyu Zhang et al.   OncoTargets and Therapy

Farnesyl transferase inhibitor FTI-277 inhibits breast cell invasion and migration by blocking H-Ras activation

(2016) Kyung Hun Lee et al.   Oncology Letters

Inhibition of Ras Signaling by Blocking Ras-Effector Interactions with Cyclic Peptides

(2015) Punit Upadhyaya et al.   ANGEWANDTE CHEMIE-INTERNATIONAL EDITION

A randomized phase II study of the MEK1/MEK2 inhibitor trametinib (GSK1120212) compared with docetaxel in KRAS-mutant advanced non-small-cell lung cancer (NSCLC)†

(2015) G. R. Blumenschein et al.   ANNALS OF ONCOLOGY

Inhibitors of Ras-SOS Interactions

(2015) Shaoyong Lu et al.   ChemMedChem

MEK inhibitors beyond monotherapy: current and future development

(2015) Ian E Templeton et al.   CURRENT OPINION IN PHARMACOLOGY

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

Targeted therapy for non-small-cell lung cancer: past, present and future

(2013) Patrick M Forde et al.   Expert Review of Anticancer Therapy

Bisphenol A Binds to Ras Proteins and Competes with Guanine Nucleotide Exchange: Implications for GTPase-Selective Antagonists

(2013) Miriam Schöpel et al.   JOURNAL OF MEDICINAL CHEMISTRY

Andrographolide derivatives inhibit guanine nucleotide exchange and abrogate oncogenic Ras function

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

In silico discovery of small-molecule Ras inhibitors that display antitumor activity by blocking the Ras-effector interaction

(2013) F. Shima 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

Prognostic and predictive biomarkers for epidermal growth factor receptor-targeted therapy in colorectal cancer: Beyond KRAS mutations

(2012) Ana Custodio et al.   CRITICAL REVIEWS IN ONCOLOGY HEMATOLOGY

Selumetinib plus docetaxel for KRAS-mutant advanced non-small-cell lung cancer: a randomised, multicentre, placebo-controlled, phase 2 study

(2012) Pasi A Jänne et al.   LANCET ONCOLOGY

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

Phase 1 first-in-human clinical study of S-trans, trans-farnesylthiosalicylic acid (salirasib) in patients with solid tumors

(2009) Apostolia Maria Tsimberidou et al.   CANCER CHEMOTHERAPY AND PHARMACOLOGY

Sorafenib Inhibits Non-Small Cell Lung Cancer Cell Growth by Targeting B-RAF in KRAS Wild-Type Cells and C-RAF in KRAS Mutant Cells

(2009) K. Takezawa et al.   CANCER RESEARCH

Typhonium flagelliforme inhibits cancer cell growth in vitro and induces apoptosis: An evaluation by the bioactivity guided approach

(2008) Choon-Sheen Lai et al.   JOURNAL OF ETHNOPHARMACOLOGY

K-rasMutations and Benefit from Cetuximab in Advanced Colorectal Cancer

(2008) Christos S. Karapetis et al.   NEW ENGLAND JOURNAL OF MEDICINE

The GAP arginine finger movement into the catalytic site of Ras increases the activation entropy

(2008) C. Kotting et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA