Small-molecule inhibition of MAP2K4 is synergistic with RAS inhibitors in KRAS-mutant cancers
RA Jansen, S Mainardi, MH Dias… - Proceedings of the …, 2024 - National Acad Sciences
The Kirsten rat sarcoma viral oncogene homologue KRAS is among the most commonly
mutated oncogenes in human cancers, thus representing an attractive target for precision …
mutated oncogenes in human cancers, thus representing an attractive target for precision …
KRAS: From undruggable to a druggable Cancer Target
D Uprety, AA Adjei - Cancer treatment reviews, 2020 - Elsevier
RAS is the most frequently mutated oncogene in human cancers, with mutations in about
30% of all cancers. RAS exists in three different isoforms (K-RAS, H-RAS and N-RAS) with …
30% of all cancers. RAS exists in three different isoforms (K-RAS, H-RAS and N-RAS) with …
[HTML][HTML] Mechanisms of Resistance to KRASG12C Inhibitors
V Dunnett-Kane, P Nicola, F Blackhall, C Lindsay - Cancers, 2021 - mdpi.com
Simple Summary KRAS is a gene that is commonly mutated in cancer, especially in
pancreatic, lung and colorectal cancers. Despite its importance, scientists have for many …
pancreatic, lung and colorectal cancers. Despite its importance, scientists have for many …
[HTML][HTML] Drugging KRAS: current perspectives and state-of-art review
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 …
several malignancies. Known as the 'holy grail'of targeted cancer therapies, KRAS is the …
Allosteric SHP2 inhibitors in cancer: Targeting the intersection of RAS, resistance, and the immune microenvironment
The nonreceptor protein tyrosine phosphatase SHP2 (encoded by PTPN11) integrates
growth and differentiation signals from receptor tyrosine kinases (RTKs) into the …
growth and differentiation signals from receptor tyrosine kinases (RTKs) into the …
Epithelial-to-Mesenchymal Transition Defines Feedback Activation of Receptor Tyrosine Kinase Signaling Induced by MEK Inhibition in KRAS-Mutant Lung Cancer
KRAS is frequently mutated in lung cancer. Whereas MAPK is a well-known effector pathway
of KRAS, blocking this pathway with clinically available MAPK inhibitors is relatively …
of KRAS, blocking this pathway with clinically available MAPK inhibitors is relatively …
Key roles of EMT for adaptive resistance to MEK inhibitor in KRAS mutant lung cancer
H Kitai, H Ebi - Small GTPases, 2017 - Taylor & Francis
ABSTRACT KRAS is frequently mutated in a variety of cancers including lung cancer.
Whereas the mitogen-activated protein kinase (MAPK) is a well-known effector pathway of …
Whereas the mitogen-activated protein kinase (MAPK) is a well-known effector pathway of …
Targeted degradation of the oncogenic phosphatase SHP2
V Vemulapalli, KA Donovan, TCM Seegar… - Biochemistry, 2021 - ACS Publications
SHP2 is a protein tyrosine phosphatase that plays a critical role in the full activation of the
Ras-MAPK pathway upon stimulation of receptor tyrosine kinases, which are frequently …
Ras-MAPK pathway upon stimulation of receptor tyrosine kinases, which are frequently …
[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 …
approximately 30% of all human cancers. As the most frequently mutated RAS isoform …
MEK Inhibition Remodels the Immune Landscape of Mutant KRAS Tumors to Overcome Resistance to PARP and Immune Checkpoint Inhibitors
B Yang, X Li, Y Fu, E Guo, Y Ye, F Li, S Liu, R Xiao… - Cancer research, 2021 - AACR
Mutant KRAS tumors are associated with poor outcomes, at least in part, due to decreased
therapeutic sensitivity. Here, we show that KRAS mutations are associated with resistance to …
therapeutic sensitivity. Here, we show that KRAS mutations are associated with resistance to …