SHP2 is required for growth of KRAS-mutant non-small-cell lung cancer in vivo
S Mainardi, A Mulero-Sánchez, A Prahallad… - Nature medicine, 2018 - nature.com
… that SHP2 inhibition is synthetic lethal with MEK inhibition in … inhibition may further enhance
the effect of SHP2 inhibition. … inhibition of SHP2 could have clinical utility for KRAS-mutant …
the effect of SHP2 inhibition. … inhibition of SHP2 could have clinical utility for KRAS-mutant …
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
… We also found that combining SHP2 and MEK inhibitors led to enhanced antiproliferative
activity and MAPK pathway suppression in KRAS-mutant cells with RTK/SHP2–mediated …
activity and MAPK pathway suppression in KRAS-mutant cells with RTK/SHP2–mediated …
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 inhibition of SHP2 or RTKs is effective at treating a variety of KRAS mutant cancers that
are … on upstream growth factor signaling, including some KRAS G13D and Q61H mutants. …
are … on upstream growth factor signaling, including some KRAS G13D and Q61H mutants. …
A12 the SHP2 inhibitor RMC-4630 in patients with KRAS-mutant non-small cell lung cancer: preliminary evaluation of a first-in-man phase 1 clinical trial
SI Ou, M Koczywas, S Ulahannan, P Janne… - Journal of Thoracic …, 2020 - jto.org
… harboring KRAS/LKB1 comutation, which occurs in 30% of KRASmutant NSCLC, have a
significantly lower response rate to IOs compared to those with KRAS mutations alone or KRAS/…
significantly lower response rate to IOs compared to those with KRAS mutations alone or KRAS/…
SHP2 inhibitor specifically suppresses the stemness of KRAS-mutant non-small cell lung cancer cells
L Jiang, W Xu, Y Chen, Y Zhang - Artificial Cells, Nanomedicine …, 2019 - Taylor & Francis
… Finally, we revealed that SHP2 inhibitor increased the sensitivity of TKIs … inhibition. Our
results suggest a possibility of using a combination of SHP2 inhibitor and TKIs for KRAS-mutant …
results suggest a possibility of using a combination of SHP2 inhibitor and TKIs for KRAS-mutant …
Mutant KRAS-driven cancers depend on PTPN11/SHP2 phosphatase
DA Ruess, GJ Heynen, KJ Ciecielski, J Ai… - Nature medicine, 2018 - nature.com
… Although KRAS mutations are virtually universal in pancreatic ductal adenocarcinoma (…
rationale for a dual SHP2/MEK inhibition, we targeted SHP2 in co-inhibition assays with two …
rationale for a dual SHP2/MEK inhibition, we targeted SHP2 in co-inhibition assays with two …
SHP2 inhibition prevents adaptive resistance to MEK inhibitors in multiple cancer models
… To more directly interrogate the effects of SHP2 inhibition on other KRAS mutants, we
used RAS-less mouse embryonic fibroblasts (MEF; ref. 19). As in MIAPaCa-2 cells, …
used RAS-less mouse embryonic fibroblasts (MEF; ref. 19). As in MIAPaCa-2 cells, …
PCC0208023, a potent SHP2 allosteric inhibitor, imparts an antitumor effect against KRAS mutant colorectal cancer
X Chen, F Zou, Z Hu, G Du, P Yu, W Wang… - Toxicology and Applied …, 2020 - Elsevier
… In the present study, PCC0208023 was synthesized to investigated its inhibitory effects
against SHP2 enzyme, the KRAS-mutant CRC in vitro and in vivo, and the RAS/MAPK signaling …
against SHP2 enzyme, the KRAS-mutant CRC in vitro and in vivo, and the RAS/MAPK signaling …
The Q61H mutation decouples KRAS from upstream regulation and renders cancer cells resistant to SHP2 inhibitors
T Gebregiworgis, Y Kano, J St-Germain… - Nature …, 2021 - nature.com
… resistance associated with Q61H, we first compared the nucleotide-exchange properties of
six oncogenic KRAS mutants, as one of the established functions of SHP2 is to promote the …
six oncogenic KRAS mutants, as one of the established functions of SHP2 is to promote the …
Targeting wild-type KRAS-amplified gastroesophageal cancer through combined MEK and SHP2 inhibition
… , events that were almost exclusive to gastroesophageal tumors, with exome sequencing
demonstrating that the majority of these tumors lack detectable KRAS mutations 3,4 . …
demonstrating that the majority of these tumors lack detectable KRAS mutations 3,4 . …
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