Tumor intrinsic efficacy by SHP2 and RTK inhibitors in KRAS-mutant cancers
HX Hao, H Wang, C Liu, S Kovats, R Velazquez… - Molecular cancer …, 2019 - AACR
… that the effect of SHP2 inhibition in KRAS-mutant cancers could be recapitulated with RTK
inhibitors. We first evaluated the efficacy of an RTK inhibitor cocktail, targeting ERBBs, FGFRs, …
inhibitors. We first evaluated the efficacy of an RTK inhibitor cocktail, targeting ERBBs, FGFRs, …
[HTML][HTML] KRAS mutation: from undruggable to druggable in cancer
L Huang, Z Guo, F Wang, L Fu - Signal transduction and targeted …, 2021 - nature.com
… were associated with genomic aberrations that were associated with the RAS/RTK pathway
79 . … Selective inhibitors targeting specific KRAS mutations are urgently needed to effectively …
79 . … Selective inhibitors targeting specific KRAS mutations are urgently needed to effectively …
SHP2 inhibition overcomes RTK-mediated pathway reactivation in KRAS-mutant tumors treated with MEK inhibitors
H Lu, C Liu, R Velazquez, H Wang, LM Dunkl… - Molecular cancer …, 2019 - AACR
… MEK inhibition, using an SHP2 inhibitor (SHP099) that blocks RAS activation mediated
by multiple RTKs. We find that RTK-driven feedback activation widely exists in KRAS-mutant …
by multiple RTKs. We find that RTK-driven feedback activation widely exists in KRAS-mutant …
The KRASG12C Inhibitor MRTX849 Provides Insight toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients
J Hallin, LD Engstrom, L Hargis, A Calinisan, R Aranda… - Cancer discovery, 2020 - AACR
… upstream signaling with RTK inhibitors that increase the activity of KRAS G12C … RTK
signaling to KRAS. Accordingly, SHP2 inhibitors are active in cancers driven by KRAS mutations …
signaling to KRAS. Accordingly, SHP2 inhibitors are active in cancers driven by KRAS mutations …
Targeting KRAS mutant lung cancer: light at the end of the tunnel
M Drosten, M Barbacid - Molecular oncology, 2022 - Wiley Online Library
… effect of RTK inhibition may be … inhibition could be effective in patients with KRAS mutant
lung tumors [[114]]. Interestingly, CDK4/6 inhibitors also synergized with KRAS G12C inhibitors …
lung tumors [[114]]. Interestingly, CDK4/6 inhibitors also synergized with KRAS G12C inhibitors …
[HTML][HTML] Escaping KRAS: gaining autonomy and resistance to KRAS inhibition in KRAS mutant cancers
Y Adachi, R Kimura, K Hirade, H Ebi - Cancers, 2021 - mdpi.com
… lung cancer, EMT has been shown to play a defining role in the feedback reactivation of
RTK signaling following MEK inhibition. In epithelial-like cells, this feedback was mediated by …
RTK signaling following MEK inhibition. In epithelial-like cells, this feedback was mediated by …
Breaking oncogene addiction: getting RTK/RAS-mutated cancers off the SOS
E Sheffels, RL Kortum - Journal of Medicinal Chemistry, 2021 - ACS Publications
… survival in KRAS mutant cancer cells, (… inhibitor of proximal RTK signaling may be a common
therapeutic strategy to enhance RTK inhibitor efficacy and treat cancers dependent on RTK …
therapeutic strategy to enhance RTK inhibitor efficacy and treat cancers dependent on RTK …
Overcoming KRAS-Mutant Lung Cancer
… KRAS mutations impart insensitivity to inhibitors of upstream … mutations within KRAS and
associated RTK and MAPK signaling molecules, acquired resistance to KRAS G12C inhibitors …
associated RTK and MAPK signaling molecules, acquired resistance to KRAS G12C inhibitors …
[HTML][HTML] Targeting KRAS mutant cancers: from druggable therapy to drug resistance
C Zhu, X Guan, X Zhang, X Luan, Z Song, X Cheng… - Molecular cancer, 2022 - Springer
… Research on direct inhibition of KRAS mutations date back to the discovery of RAS-… Unlike
NSCLC cell lines, the KRAS (G12C) CRC models have a high basal level of RTK activation …
NSCLC cell lines, the KRAS (G12C) CRC models have a high basal level of RTK activation …
Targeting mutant KRAS for anticancer therapy
F Chen, MP Alphonse, Y Liu… - Current topics in medicinal …, 2019 - ingentaconnect.com
… for inhibiting KRAS signaling and blocking KRAS functions, in … nanoparticles together with
the RTK inhibitor erlotinib. This … thus a mechanistic understanding of KRAS mutations and their …
the RTK inhibitor erlotinib. This … thus a mechanistic understanding of KRAS mutations and their …