[HTML][HTML] Impact of SHP2 tyrosine phosphorylation on the development of acquired resistance to allosteric SHP2 inhibitors

G Franciosa, JV Olsen - Oncotarget, 2023 - ncbi.nlm.nih.gov
… is only effective as combination treatment with inhibitors of other nodes of the RAS-ERK …
adaptive resistance after prolonged treatment in vitro with the allosteric SHP2 inhibitor SHP099. …

Activating mutation of SHP2 establishes a tumorigenic phonotype through cell-autonomous and non-cell-autonomous mechanisms

L Dong, D Han, X Meng, M Xu, C Zheng… - Frontiers in Cell and …, 2021 - frontiersin.org
… Since SHP2 is considered as a novel antitumor target, we also summarized currently used
SHP2 inhibitors … of adaptive resistance, whereas SHP2 inhibitor SHP099 combined with MEK …

Shp2: A pleiotropic target at the interface of cancer and its microenvironment

NM Sodir, G Pathria, JI Adamkewicz, EH Kelley… - Cancer discovery, 2023 - AACR
… A genome-wide CRISPR screen has identified that loss of INPPL1, MAP4K5, or LZTR1
genes results in resistance to SHP2 inhibition in vitro and in vivo by MAPK reactivation (123), as …

Combination of KRASG12C (ON) and SHP2 inhibitors overcomes adaptive resistance and enhances anti-tumour immunity

P Anastasiou, J Boumelha, E Mugarza… - European Journal of …, 2022 - ejcancer.com
… ON) inhibitor, RM-029, which targets the GTP-bound active state, with the SHP2 inhibitor
RMC-… tumor microenvironment (TME) which can lead to adaptive anti-tumor immune responses. …

Combining EGFR inhibitors with SHP2 or LSD1 inhibitors to overcome multidrug resistance in cancer

H Zhang, X Yang, Y Song, B Yu - Future Medicinal Chemistry, 2022 - Taylor & Francis
… Given the roles of SHP2 in growth factor receptor-mediated signaling pathways, the …
EGFR/SHP2 inhibitors may also be an effective strategy for treating adaptive resistance cancers. …

DETERMINING THE MECHANISMS BEHIND ADAPTIVE RESISTANCE IN FLT3/ITD AML

T Seale - 2022 - jscholarship.library.jhu.edu
… AXL as a therapeutic target, we hypothesized that inhibiting SHP2, a signaling node directly
… TKI to combat against adaptive resistance. Using the allosteric SHP2 inhibitor SHP099, we …

[HTML][HTML] Developing SHP2-based combination therapy for KRAS-amplified cancer

T Li, O Kikuchi, J Zhou, Y Wang, B Pokharel, K Bastl… - JCI insight, 2023 - ncbi.nlm.nih.gov
SHP2 inhibition is also being evaluated for its ability to block adaptive resistance to other …
role in combination with MAPK inhibition, we hypothesize that SHP2 inhibition may serve as a …

[HTML][HTML] Targeting SHP2 sensitizes differentiated thyroid carcinoma to the MEK inhibitor

J Zhi, J Yi, X Hou, W Wang, W Yang, L Hu… - American Journal of …, 2022 - ncbi.nlm.nih.gov
… and resistance to MEKi in DTC, which is reversed by SHP2 blockade. As a novel active inhibitor
of SHP2… is a promising therapeutic approach for advanced DTC and MEKi-resistant one. …

PI3K inhibition circumvents resistance to SHP2 blockade in metastatic triple-negative breast cancer

RJ Amante, C Jehanno, D De Silva… - Journal of mammary …, 2023 - Springer
… PI3K inhibition circumvents SHP2i resistance but, given the pleiotropic activity of SHP2,
additional mechanisms of resistance … It has been reported for example that resistance to SHP099 …

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 to both catalytic and allosteric SHP2 inhibitors. … receptor (EGFR) drug resistance
in both lung and colorectal … the resistance of KRAS Q61H mutant cells to SHP2 inhibitors