Drugging the undruggable: advances on RAS targeting in cancer

M Molina-Arcas, A Samani, J Downward - Genes, 2021 - mdpi.com
… Interestingly, only those cells bearing KRAS mutations that maintain intrinsic GTPase …
Furthermore, gene expression signatures may help stratify patients for optimal RTK inhibitors [107]. …

[HTML][HTML] Concomitant inhibition of receptor tyrosine kinases and downstream AKT synergistically inhibited growth of KRAS/BRAF mutant colorectal cancer cells

Q Song, X Sun, H Guo, Q Yu - Oncotarget, 2017 - ncbi.nlm.nih.gov
… of the RTK-PI3K-AKT pathway in the KRAS/BRAF mutant CRC … of BRAF/KRAS mutant CRC
cells mainly by inhibiting AKT … of six KRAS mutant CRC cell lines and two BRAF mutant CRC …

Targeting KRAS in colorectal cancer

C Wang, M Fakih - Current Oncology Reports, 2021 - Springer
… MEK inhibition in KRAS mutated colorectal cancer models, MEK inhibitor alone has shown
limited antitumor activity in KRAS … colorectal cancer cell lines have higher basal level of RTK

Targeting KRAS in Lung Cancer Beyond KRAS G12C Inhibitors: The Immune Regulatory Role of KRAS and Novel Therapeutic Strategies

M Cucurull, L Notario, M Sanchez-Cespedes… - Frontiers in …, 2022 - frontiersin.org
… We aim to summarize the tumor heterogeneity of KRAS mutant lung cancers and its … inhibitors
alone or in combination with RTK inhibitors have failed to prove effective in KRAS mutant

RAS, wanted dead or alive: Advances in targeting RAS mutant cancers

CA Stalnecker, CJ Der - Science signaling, 2020 - science.org
… McFall et al. report that other KRAS mutants are highly effective … of upstream RTK activity.
In contrast, they report that the … MAPK inhibition increased the dependency of KRAS mutant

KRASG12C-independent feedback activation of wild-type RAS constrains KRASG12C inhibitor efficacy

MB Ryan, O Coker, A Sorokin, K Fella, H Barnes… - Cell reports, 2022 - cell.com
… However, the exact mechanism by which RTK signaling leads to RAS-MAPK … of KRAS G12C
inhibitors is unclear. One proposed mechanism is that increased RTK signaling shifts KRAS

Targeting RTK signaling pathways in cancer

T Regad - Cancers, 2015 - mdpi.com
… kinase inhibitors act on the tyrosine kinase domain of RTK, … Mutations in RAS family of genes
(K-RAS, N-RAS, H-RAS) … High frequency of KRAS mutations are found in pancreatic, large …

Mechanisms of Resistance to KRASG12C Inhibitors

V Dunnett-Kane, P Nicola, F Blackhall, C Lindsay - Cancers, 2021 - mdpi.com
… G12C mutant xenografts [28] STK11 co-mutations in KRAS mutant NSCLC have been …
Furthermore, this study identified no single RTK that was critical for all KRAS G12C models …

KRAS, BRAF, PIK3CA, and PTEN mutations: implications for targeted therapies in metastatic colorectal cancer

W De Roock, V De Vriendt, N Normanno… - The lancet …, 2011 - thelancet.com
… from RTK signalling are needed, in which case KRAS-mutant tumours will still benefit from
RTK inhibition. Moreover, to define colorectal cancer as KRAS mutant versus KRAS wild-type …

[HTML][HTML] Targeting KRAS in non-small-cell lung cancer: recent progress and new approaches

M Reck, DP Carbone, M Garassino, F Barlesi - Annals of Oncology, 2021 - Elsevier
… with the highest rate of KRAS mutations are pancreatic (88%)… therapies specifically inhibiting
mutated forms of KRAS or its … (RTK); in particular, KRAS G12C - and KRAS-mutant NSCLC …