Chemical genetics screen identifies COPB2 tool compounds that alters ER stress response and induces RTK dysregulation in lung cancer cells

P Saraon, J Snider, W Schormann, A Rai… - Journal of Molecular …, 2021 - Elsevier
Activating mutations in the epidermal growth factor receptor (EGFR) are common driver
mutations in non-small cell lung cancer (NSCLC). First, second and third generation EGFR …

Structural Mechanism and Inhibitors Targeting EGFR Exon 20 Insertion (Ex20ins) Mutations

H Chen, S Hu, AV Patterson, JB Smaill… - Journal of medicinal …, 2023 - ACS Publications
Epidermal growth factor receptor (EGFR) targeted therapy is one of the most important and
effective strategies to combat EGFR mutant nonsmall-cell lung cancer (NSCLC). However, a …

CBX5 loss drives EGFR inhibitor resistance and results in therapeutically actionable vulnerabilities in lung cancer

S Bugide, YJK Edwards, R Gupta… - Proceedings of the …, 2023 - National Acad Sciences
Although epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (EGFRi) are
approved for treating EGFR-mutant lung adenocarcinoma (LUAD), emergence of acquired …

Discovery of mobocertinib, a new irreversible tyrosine kinase inhibitor indicated for the treatment of non-small-cell lung cancer harboring EGFR exon 20 insertion …

J Wang, D Lam, J Yang, L Hu - Medicinal Chemistry Research, 2022 - Springer
Epidermal growth factor receptor (EGFR) is essential for normal cellular functions. Mutations
of EGFR's kinase domain can cause dysregulation leading to non-small cell lung cancer …

Mobocertinib (TAK-788): A Targeted Inhibitor of EGFR Exon 20 Insertion Mutants in Non–Small Cell Lung Cancer

F Gonzalvez, S Vincent, TE Baker, AE Gould, S Li… - Cancer discovery, 2021 - AACR
Most EGFR exon 20 insertion (EGFR ex20ins) driver mutations in non–small cell lung
cancer (NSCLC) are insensitive to approved EGFR tyrosine kinase inhibitors (TKI). To …

A small-molecule compound D6 overcomes EGFR-T790M-mediated resistance in non-small cell lung cancer

X Tang, L Cheng, G Li, YM Yan, F Su… - Communications …, 2021 - nature.com
Non-small cell lung cancer (NSCLC) is a deadly and highly prevalent malignancy. Targeting
activated-EGFR mutations in NSCLC via EGFR tyrosine kinase inhibitor (EGFR-TKI) initially …

[HTML][HTML] Discovery of mobocertinib, a potent, oral inhibitor of EGFR exon 20 insertion mutations in non–small cell lung cancer

WS Huang, F Li, Y Gong, Y Zhang… - Bioorganic & medicinal …, 2023 - Elsevier
In the treatment of non–small cell lung cancer (NSCLC), patients harboring exon 20
insertion mutations in the epidermal growth factor receptor (EGFR) gene (EGFR) have few …

Emerging molecular dependencies of mutant EGFR-driven non-small cell lung cancer

DA Farnsworth, YT Chen, G de Rappard Yuswack… - Cells, 2021 - mdpi.com
Epidermal growth factor receptor (EGFR) mutations are the molecular driver of a subset of
non-small cell lung cancers (NSCLC); tumors that harbor these mutations are often …

Dynamic EGFR interactomes reveal differential association of signaling modules with wildtype and Exon19-del EGFR in NSCLC cell lines

X Zhang, Y Chen, SY Jung, X Li, F Meng, B Zhong… - Journal of …, 2022 - Elsevier
Protein-protein interaction networks (PPIs) govern the majority of biological processes, but
how oncogenic mutations impact these interactions and their functions at a network scale is …

[HTML][HTML] Overexpression of OCT4 is associated with gefitinib resistance in non-small cell lung cancer

B Li, Z Yao, Y Wan, D Lin - Oncotarget, 2016 - ncbi.nlm.nih.gov
Epidermal growth factor receptor (EGFR)-targeted tyrosine kinase inhibitors (TKIs) have
emerged as first-line drugs for non-small cell lung cancers (NSCLCs). However, the …