
Allosteric SHP2 Inhibitor, IACS-13909, Overcomes EGFR ... - PubMed
2020年11月1日 · SHP2 inhibition has demonstrated tumor growth inhibition in RTK-activated cancers in preclinical studies. The long-term effectiveness of tyrosine kinase inhibitors such as …
SHP2–EGFR States in Dephosphorylation Can Inform Selective SHP2 ...
2024年5月15日 · SHP2 is a positive regulator of the EGFR-dependent Ras/MAPK pathway. It dephosphorylates a regulatory phosphorylation site in EGFR that serves as the binding site to …
SHP2 inhibition enhances the anticancer effect of Osimertinib in EGFR …
2021年7月3日 · Here we report for the first time that proliferation of EGFR T790M mutant LUAD cells is significantly enhanced by SHP2, and knock-down of SHP2 limits proliferation and …
Allosteric inhibition of SHP2 phosphatase inhibits cancers
2016年6月29日 · Here we report the discovery of a highly potent (IC 50 = 0.071 μM), selective and orally bioavailable small-molecule SHP2 inhibitor, SHP099, that stabilizes SHP2 in an …
SHP2在非小细胞肺癌EGFR-TKI耐药中的作用及机制研究
目的:表皮生长因子受体(Epidermal growth factor receptor,EGFR)突变是非小细胞肺癌(Non-small cell lung cancer,NSCLC)最常见的驱动基因之一.靶向EGFR的酪氨酸激酶抑制剂(EGFR …
SHP2 Inhibition Benefits Epidermal Growth Factor Receptor ... - PubMed
Therefore, we hypothesize that SHP2 inhibitor might be a promising drug that could synergistically enhance or sensitize the anti-tumor efficacy of EGFR-TKIs in EGFR mutated NSCLC patients.
Targeting SHP2 for EGFR Inhibitor Resistant Non-Small Cell Lung ...
2013年10月4日 · We show that SHP2 is required for EGF-stimulated ERK1/2 phosphorylation and proliferation in EGFR inhibitor resistant NSCLC cell line H1975, which harbors the EGFR …
Diminished functional role and altered localization of SHP2 in …
2012年7月9日 · As ERK activity influences cellular response to EGFR inhibition, altered SHP2 function could have a role in the striking response to gefitinib witnessed with EGFR mutation. …
Allosteric SHP2 Inhibitor, IACS-13909, Overcomes EGFR …
2020年11月3日 · Together, our preclinical data demonstrate that the SHP2 inhibitor, IACS-13909, is effective in overcoming both EGFR-dependent and EGFR-independent resistance …
EGFR-activated Src family kinases maintain GAB1-SHP2 ... - Science
We explored how dynamics in the interactions among the epidermal growth factor (EGF) receptor (EGFR), GRB2-associated binder protein 1 (GAB1), and SH2 domain–containing phosphatase …