[HTML][HTML] Protein tyrosine kinase inhibitor resistance in malignant tumors: molecular mechanisms and future perspective

Y Yang, S Li, Y Wang, Y Zhao, Q Li - Signal transduction and targeted …, 2022 - nature.com
Protein tyrosine kinases (PTKs) are a class of proteins with tyrosine kinase activity that
phosphorylate tyrosine residues of critical molecules in signaling pathways. Their basal …

Small molecule inhibitors targeting the EGFR/ErbB family of protein-tyrosine kinases in human cancers

R Roskoski Jr - Pharmacological research, 2019 - Elsevier
The EGFR family is among the most investigated receptor protein-tyrosine kinase groups
owing to its general role in signal transduction and in oncogenesis. This family consists of …

[HTML][HTML] Intrinsic Resistance to EGFR-Tyrosine Kinase Inhibitors in EGFR-Mutant Non-Small Cell Lung Cancer: Differences and Similarities with Acquired Resistance

E Santoni-Rugiu, LC Melchior, EM Urbanska… - Cancers, 2019 - mdpi.com
Activating mutations in the epidermal growth factor receptor gene occur as early cancer-
driving clonal events in a subset of patients with non-small cell lung cancer (NSCLC) and …

The next tier of EGFR resistance mutations in lung cancer

HL Tumbrink, A Heimsoeth, ML Sos - Oncogene, 2021 - nature.com
EGFR mutations account for the majority of druggable targets in lung adenocarcinoma. Over
the past decades the optimization of EGFR inhibitors revolutionized the treatment options for …

[HTML][HTML] Overcoming EGFRG724S-mediated osimertinib resistance through unique binding characteristics of second-generation EGFR inhibitors

J Fassunke, F Müller, M Keul, S Michels… - Nature …, 2018 - nature.com
The emergence of acquired resistance against targeted drugs remains a major clinical
challenge in lung adenocarcinoma patients. In a subgroup of these patients we identified an …

[HTML][HTML] Sensitivity and resistance of MET exon 14 mutations in lung cancer to eight MET tyrosine kinase inhibitors in vitro

T Fujino, Y Kobayashi, K Suda, T Koga… - Journal of Thoracic …, 2019 - Elsevier
Background MNNG HOS transforming gene (MET) exon 14 mutations in lung cancer,
including exon 14 skipping and point mutations, have been attracting the attention of …

[HTML][HTML] BBT-176, a novel fourth-generation tyrosine kinase inhibitor for osimertinib-resistant EGFR mutations in non–small cell lung cancer

SM Lim, T Fujino, C Kim, G Lee, YH Lee, DW Kim… - Clinical Cancer …, 2023 - AACR
Purpose: Resistance to third-generation EGFR inhibitors including osimertinib arises in part
from the C797S mutation in EGFR. Currently, no targeted treatment option is available for …

Recent advances in the development of EGFR degraders: PROTACs and LYTACs

D Hong, B Zhou, B Zhang, H Ren, L Zhu… - European Journal of …, 2022 - Elsevier
Abstract Epidermal Growth Factor Receptor (EGFR), a transmembrane tyrosine kinase
receptor, belongs to the ErbB receptor family, also known as HER1 or ErbB1. Its abnormal …

Activity of a novel HER2 inhibitor, poziotinib, for HER2 exon 20 mutations in lung cancer and mechanism of acquired resistance: An in vitro study

T Koga, Y Kobayashi, K Tomizawa, K Suda, T Kosaka… - Lung Cancer, 2018 - Elsevier
Objectives Oncogenic HER2 mutations are present in 2–4% of lung adenocarcinomas, but
the relevant clinical trials are unsatisfactory. The novel HER2 inhibitor poziotinib was …

Epidermal growth factor receptor PROTACs as an effective strategy for cancer therapy: A review

C Wang, Y Zhang, W Chen, Y Wang, D Xing - Biochimica et Biophysica …, 2023 - Elsevier
Epidermal growth factor receptor (EGFR), a transmembrane glycoprotein that mediates
cellular signaling pathways involved in cell proliferation, angiogenesis, apoptosis, and …