[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 dimerization impacts MEK inhibitor sensitivity and oncogenic activity of mutant KRAS

C Ambrogio, J Köhler, ZW Zhou, H Wang, R Paranal… - Cell, 2018 - cell.com
The mechanism by which the wild-type KRAS allele imparts a growth inhibitory effect to
oncogenic KRAS in various cancers, including lung adenocarcinoma (LUAD), is poorly …

Oncogenic KRAS blockade therapy: renewed enthusiasm and persistent challenges

D Tang, G Kroemer, R Kang - Molecular cancer, 2021 - Springer
Across a broad range of human cancers, gain-of-function mutations in RAS genes (HRAS,
NRAS, and KRAS) lead to constitutive activity of oncoproteins responsible for tumorigenesis …

Targeting the MAPK pathway in KRAS-driven tumors

M Drosten, M Barbacid - Cancer cell, 2020 - cell.com
KRAS mutations occur in a quarter of all of human cancers, yet no selective drug has been
approved to treat these tumors. Despite the recent development of drugs that block KRAS …

Precise characterization of KRAS4b proteoforms in human colorectal cells and tumors reveals mutation/modification cross-talk

I Ntai, L Fornelli, CJ DeHart, JE Hutton… - Proceedings of the …, 2018 - National Acad Sciences
Mutations of the KRAS gene are found in human cancers with high frequency and result in
the constitutive activation of its protein products. This leads to aberrant regulation of …

Selective inhibition of oncogenic KRAS output with small molecules targeting the inactive state

MP Patricelli, MR Janes, LS Li, R Hansen, U Peters… - Cancer discovery, 2016 - AACR
KRAS gain-of-function mutations occur in approximately 30% of all human cancers. Despite
more than 30 years of KRAS-focused research and development efforts, no targeted therapy …

KRAS as a druggable target in NSCLC: Rising like a phoenix after decades of development failures

A Friedlaender, A Drilon, GJ Weiss, GL Banna… - Cancer treatment …, 2020 - Elsevier
Cancers of nearly all lineages harbor alterations that deregulate mitogen-activated protein
kinase signaling, a crucial signaling pathway for tumor formation and maintenance. Of these …

Drugging KRAS: current perspectives and state-of-art review

K Parikh, G Banna, SV Liu, A Friedlaender… - Journal of hematology & …, 2022 - Springer
After decades of efforts, we have recently made progress into targeting KRAS mutations in
several malignancies. Known as the 'holy grail'of targeted cancer therapies, KRAS is the …

Comparative analysis of KRAS codon 12, 13, 18, 61 and 117 mutations using human MCF10A isogenic cell lines

B Stolze, S Reinhart, L Bulllinger, S Fröhling… - Scientific reports, 2015 - nature.com
KRAS mutations occur in one third of human cancers and cluster in several hotspots, with
codons 12 and 13 being most commonly affected. It has been suggested that the position …

[HTML][HTML] Differential effector engagement by oncogenic KRAS

TL Yuan, A Amzallag, R Bagni, M Yi, S Afghani… - Cell reports, 2018 - cell.com
KRAS can bind numerous effector proteins, which activate different downstream signaling
events. The best known are RAF, phosphatidylinositide (PI)-3′ kinase, and RalGDS …