[HTML][HTML] Targeting the untargetable KRAS in cancer therapy

P Liu, Y Wang, X Li - Acta Pharmaceutica Sinica B, 2019 - Elsevier
RAS is one of the most well-known proto-oncogenes. Its gain-of-function mutations occur in
approximately 30% of all human cancers. As the most frequently mutated RAS isoform …

KRAS oncogene in non-small cell lung cancer: clinical perspectives on the treatment of an old target

M Román, I Baraibar, I López, E Nadal, C Rolfo… - Molecular cancer, 2018 - Springer
Lung neoplasms are the leading cause of death by cancer worldwide. Non-small cell lung
cancer (NSCLC) constitutes more than 80% of all lung malignancies and the majority of …

Defining the KRAS-and ERK-dependent transcriptome in KRAS-mutant cancers

JA Klomp, JE Klomp, CA Stalnecker, KL Bryant… - Science, 2024 - science.org
How the KRAS oncogene drives cancer growth remains poorly understood. Therefore, we
established a systemwide portrait of KRAS-and extracellular signal–regulated kinase (ERK) …

[HTML][HTML] Targeting KRAS mutant cancers with a covalent G12C-specific inhibitor

MR Janes, J Zhang, LS Li, R Hansen, U Peters, X Guo… - Cell, 2018 - cell.com
Summary KRAS G12C was recently identified to be potentially druggable by allele-specific
covalent targeting of Cys-12 in vicinity to an inducible allosteric switch II pocket (S-IIP) …

A gene–environment-induced epigenetic program initiates tumorigenesis

D Alonso-Curbelo, YJ Ho, C Burdziak, JLV Maag… - Nature, 2021 - nature.com
Tissue damage increases the risk of cancer through poorly understood mechanisms. In
mouse models of pancreatic cancer, pancreatitis associated with tissue injury collaborates …

Determining the ERK-regulated phosphoproteome driving KRAS-mutant cancer

JE Klomp, JN Diehl, JA Klomp, AC Edwards, R Yang… - Science, 2024 - science.org
To delineate the mechanisms by which the ERK1 and ERK2 mitogen-activated protein
kinases support mutant KRAS–driven cancer growth, we determined the ERK-dependent …

[HTML][HTML] Epigenomic state transitions characterize tumor progression in mouse lung adenocarcinoma

LM LaFave, VK Kartha, S Ma, K Meli, I Del Priore… - Cancer cell, 2020 - cell.com
Regulatory networks that maintain functional, differentiated cell states are often dysregulated
in tumor development. Here, we use single-cell epigenomics to profile chromatin state …

TEAD Inhibition Overcomes YAP1/TAZ-Driven Primary and Acquired Resistance to KRASG12C Inhibitors

AC Edwards, CA Stalnecker, A Jean Morales… - Cancer …, 2023 - aacrjournals.org
Primary/intrinsic and treatment-induced acquired resistance limit the initial response rate to
and long-term efficacy of direct inhibitors of the KRASG12C mutant in cancer. To identify …

Erianin inhibits the growth and metastasis through autophagy-dependent ferroptosis in KRASG13D colorectal cancer

Q Miao, W Deng, W Lyu, Z Sun, S Fan, M Qi… - Free Radical Biology …, 2023 - Elsevier
Colorectal cancer (CRC) is the third most common cause of cancer mortality worldwide.
Approximately 40% of CRC patients are KRAS sequence variation, including KRAS G13D …

KRASG12C inhibition produces a driver-limited state revealing collateral dependencies

K Lou, V Steri, AY Ge, YC Hwang, CH Yogodzinski… - Science …, 2019 - science.org
Inhibitors targeting KRASG12C, a mutant form of the guanosine triphosphatase (GTPase)
KRAS, are a promising new class of oncogene-specific therapeutics for the treatment of …