A first-in-class selective inhibitor of EGFR and PI3K offers a single ...
WEBJul 11, 2024 — Here we evaluated the pharmacological profile of MTX-531 that was computationally designed to selectively target two key resistance drivers, epidermal growth factor receptor and...
Dual inhibition of EGFR and PI3K with a single drug - Nature
WEBAug 16, 2024 — Signaling pathways that involve epidermal growth factor receptor (EGFR) or phosphoinositide-3-kinase (PI3K) are two highly interconnected and frequently dysregulated pathways that drive...
Blocking EGFR palmitoylation suppresses PI3K signaling and
WEBMar 3, 2020 — Palmitoylated EGFR interacted with the PI3K regulatory subunit PIK3R1 (p85) and increased the recruitment of the PI3K heterodimer to the plasma membrane. Alternatively, blocking palmitoylation increased the association of EGFR with the MAPK adaptor Grb2 and decreased that with p85.
Blocking EGFR palmitoylation suppresses PI3K signaling and
WEBMar 3, 2020 — These findings suggest a mechanism whereby oncogenic KRAS saturates signaling through unpalmitoylated EGFR, reducing formation of the PI3K signaling complex. Future development of DHHC20 inhibitors to reduce EGFR-PI3K signaling could be beneficial to patients with KRAS-mutant tumors.
Epidermal Growth Factor Receptor Cell Proliferation Signaling …
WEBMay 17, 2017 — Epidermal growth factor receptor (EGFR) signaling pathways leading to G1/S cell cycle progression activated by EGF activation. Depicted are the RAS-RAF-MEK-ERK MAPK and PI3K-AKT-mTOR pathways. EGF activation of the EGFR induces receptor dimerization and transphosphorylation of the C-terminal domain.
Regulation of EGF-stimulated activation of the PI-3K/AKT
WEBNov 29, 2022 — These experiments demonstrate that exocyst-mediated exocytosis-by regulating PI(3,4,5)P 3 levels at the plasma membrane-subserves activation of the PI-3K/AKT pathway by EGFR in epithelial cells. Keywords: …
The efficacy of PI3Kγ and EGFR inhibitors on the suppression of …
WEBJan 10, 2022 — Thus, these data suggest that the inhibitiors of PI3K and EGFR, especially PI3Kγ, might be a promising therapeutic strategy against CSCs defeating cancer in the near future.
Dual blockade of EGFR and PI3K signaling pathways offers a …
WEBDec 18, 2023 — Our findings demonstrate that the combined blockade of the EGFR/MEK/ERK and PI3K/AKT/mTOR pathways is more effective against GBM than inhibition of each pathway alone, both in vitro and in vivo. Our results suggest that AZD-9291 combined with GDC-0084 may be considered as a potential treatment strategy in future clinical trials.
EGFR and PI3K Signalling Pathways as Promising Targets on …
WEBMay 20, 2024 — Compensatory MAPK/ERK pathway upregulation by PI3K/Akt suppression was overcome by combination treatment with the EGFR inhibitor gefitinib, which was strongly synergistic. PIK-75 plus gefitinib significantly impaired UWG02CTC invasion in an organotypic assay.
Molecular Pathways in Head and Neck Cancer: EGFR, PI3K, and …
WEBMay 16, 2013 — Morris LG, Taylor BS, Bivona TG, et al. Genomic dissection of the epidermal growth factor receptor (EGFR)/PI3K pathway reveals frequent deletion of the EGFR phosphatase PTPRS in head and neck cancers.