[HTML][HTML] SHP2 Inhibitors Undergo Exploration in Combinations
S Morris - 2023 - targetedonc.com
… Johnson said that SHP2 inhibitor therapy “is an area of active investigation—none of the …
is, ‘Are SHP2 inhibitors something that we can add when patients develop resistance to a …
is, ‘Are SHP2 inhibitors something that we can add when patients develop resistance to a …
SHP2 inhibition as the backbone of targeted therapy combinations for the treatment of cancers driven by oncogenic mutations in the RAS pathway
JA Smith, M Singh, RJ Nichols, ES Koltun, YC Yang… - Cancer Research, 2020 - AACR
… In the context of adaptive resistance to mutant-selective inhibitors, SHP2 inhibition has the
… Here we show, using in vitro and in vivo systems, that SHP2 inhibitors have the potential to …
… Here we show, using in vitro and in vivo systems, that SHP2 inhibitors have the potential to …
Crystallographic landscape of SHP2 provides molecular insights for SHP2 targeted drug discovery
Y Song, X Yang, S Wang, M Zhao… - Medicinal Research …, 2022 - Wiley Online Library
… Given the drug resistance of reported SHP2 inhibitors, in-… SHP2 proteins may facilitate the
development of inhibitors targeting SHP2 mutations for patients with specific adaptive resistant …
development of inhibitors targeting SHP2 mutations for patients with specific adaptive resistant …
RTK/SHP2 dependency and feedback adaptation to MEK inhibition defines sensitivity of RAS-mutant proteins to SHP2 inhibitor-based therapies
B Baars, C Adamopoulos, A Orive-Ramos… - Cancer Research, 2023 - AACR
… that, MAPK inhibition using MEK inhibitors (MEKi) have limited effectiveness in such tumors
due to adaptive resistance. A major mechanism of adaptive resistance involves relief of …
due to adaptive resistance. A major mechanism of adaptive resistance involves relief of …
Combined inhibition of SHP2 and CXCR1/2 promotes antitumor T-cell response in NSCLC
… These results show that Cxcl1/5 induction is a consequence of SHP2 inhibition, rather
than an off-target effect of SHP099. Allografts established with SHP099-resistant KP cells still …
than an off-target effect of SHP099. Allografts established with SHP099-resistant KP cells still …
[HTML][HTML] PTPRS drives adaptive resistance to MEK/ERK inhibitors through SRC
TB Davis, M Yang, H Wang, C Lee, TJ Yeatman… - Oncotarget, 2019 - ncbi.nlm.nih.gov
… in developing adaptive resistance to MEK/ERK inhibitors (MEKi/… averting adaptive resistance
through the use of the SRC inhibitor, … adaptive resistance pathways operating through SRC. …
through the use of the SRC inhibitor, … adaptive resistance pathways operating through SRC. …
TGFβ Antagonizes IFNγ-Mediated Adaptive Immune Evasion via Activation of the AKT–Smad3–SHP1 Axis in Lung Adenocarcinoma
F Ye, Z Cai, B Wang, C Zeng, Y Xi, S Hu, R Qu… - Cancer …, 2023 - aacrjournals.org
… Indeed, inhibition of tumor IFN signaling renders highly resistant … of SHP2 at Tyr542 can
be used as an indicator of SHP2 … of SHP2 did not reverse TGFb-mediated inhibition of IFNg-…
be used as an indicator of SHP2 … of SHP2 did not reverse TGFb-mediated inhibition of IFNg-…
Genome-wide CRISPR/Cas9 Screens Reveal Shared and Bespoke Mechanisms of Resistance to SHP2 inhibition
W Wei - 2023 - search.proquest.com
… prospectively identify resistance mechanisms to SHP2 inhibition, using the prototype allosteric
inhibitor SHP099, because as I discussed in this section earlier that resistance to targeted …
inhibitor SHP099, because as I discussed in this section earlier that resistance to targeted …
[HTML][HTML] SHP2 inhibition restores sensitivity to ALK inhibitors in resistant ALK-rearranged non-small cell lung cancer
L Dardaei, HQ Wang, M Singh, P Fordjour… - Nature …, 2018 - ncbi.nlm.nih.gov
… and adaptive resistance … SHP2 inhibition can overcome resistance in multiple contexts of
tyrosine kinase mediated bypass signaling leading to survival in the presence of ALK inhibition…
tyrosine kinase mediated bypass signaling leading to survival in the presence of ALK inhibition…
[HTML][HTML] Mechanism of activating mutations and allosteric drug inhibition of the phosphatase SHP2
… as for wild-type SHP2, which falls at the far tail of the inhibition curve. … the inhibition of SHP2
in the absence of the activating peptide. … may prevent the emergence of resistance mutations. …
in the absence of the activating peptide. … may prevent the emergence of resistance mutations. …