Clinical development of targeted and immune based anti-cancer therapies

NA Seebacher, AE Stacy, GM Porter… - Journal of Experimental & …, 2019 - Springer
Cancer is currently the second leading cause of death globally and is expected to be
responsible for approximately 9.6 million deaths in 2018. With an unprecedented …

EMT: A mechanism for escape from EGFR-targeted therapy in lung cancer

E Tulchinsky, O Demidov, M Kriajevska… - … et Biophysica Acta (BBA …, 2019 - Elsevier
Epithelial mesenchymal transition (EMT) is a reversible developmental genetic programme
of transdifferentiation of polarised epithelial cells to mesenchymal cells. In cancer, EMT is an …

Efficacy, safety, and genetic analysis of furmonertinib (AST2818) in patients with EGFR T790M mutated non-small-cell lung cancer: a phase 2b, multicentre, single-arm …

Y Shi, X Hu, S Zhang, D Lv, L Wu, Q Yu… - The Lancet …, 2021 - thelancet.com
Background Furmonertinib (AST2818) is a third-generation epidermal growth factor receptor
(EGFR) tyrosine kinase inhibitor (TKI) targeting both sensitising EGFR and EGFR Thr790Met …

Design, synthesis and anticancer evaluation of thieno [2, 3-d] pyrimidine derivatives as dual EGFR/HER2 inhibitors and apoptosis inducers

SA Elmetwally, KF Saied, IH Eissa, EB Elkaeed - Bioorganic chemistry, 2019 - Elsevier
Deregulation of many kinases is directly linked to cancer development and the tyrosine
kinase family is one of the most important targets in current cancer therapy regimens. In this …

Development of EGFR TKIs and options to manage resistance of third-generation EGFR TKI osimertinib: conventional ways and immune checkpoint inhibitors

L Wu, L Ke, Z Zhang, J Yu, X Meng - Frontiers in Oncology, 2020 - frontiersin.org
Epidermal growth factor receptor tyrosine kinase inhibitors (EGFR TKIs) have been first-line
therapy in the treatment of non-small cell lung cancer (NSCLC) harboring EGFR sensitive …

Mutant‐selective allosteric EGFR degraders are effective against a broad range of drug‐resistant mutations

J Jang, C To, DJH De Clercq, E Park… - Angewandte …, 2020 - Wiley Online Library
Targeting epidermal growth factor receptor (EGFR) through an allosteric mechanism
provides a potential therapeutic strategy to overcome drug‐resistant EGFR mutations that …

Start selective and rigidify: the discovery path toward a next generation of EGFR tyrosine kinase inhibitors

H Engelhardt, D Böse, M Petronczki… - Journal of medicinal …, 2019 - ACS Publications
The epidermal growth factor receptor (EGFR), when carrying an activating mutation like
del19 or L858R, acts as an oncogenic driver in a subset of lung tumors. While tumor …

mTOR/EGFR/iNOS/MAP2K1/FGFR/TGFB1 are druggable candidates for N-(2, 4-difluorophenyl)-2′, 4′-difluoro-4-hydroxybiphenyl-3-carboxamide (NSC765598) …

B Lawal, CY Lee, N Mokgautsi, MR Sumitra… - Frontiers in …, 2021 - frontiersin.org
Background The application of computational and multi-omics approaches has aided our
understanding of carcinogenesis and the development of therapeutic strategies …

[HTML][HTML] Inhibition of DCLK1 sensitizes resistant lung adenocarcinomas to EGFR-TKI through suppression of Wnt/β-Catenin activity and cancer stemness

R Yan, X Fan, Z Xiao, H Liu, X Huang, J Liu, S Zhang… - Cancer letters, 2022 - Elsevier
Lung adenocarcinoma is the most common form of lung cancer, accounting for 60% of non-
small cell lung cancer (NSCLC) cases in Asian patients. Importantly, nearly half of these …

Acquired resistance mechanisms to osimertinib: the constant battle

Z Zalaquett, MCR Hachem, Y Kassis, S Hachem… - Cancer Treatment …, 2023 - Elsevier
Lung cancer is the leading cause of cancer-related mortality worldwide. Detectable driver
mutations have now changed the course of lung cancer treatment with the emergence of …