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 …

The next generation of EGFR inhibitors: a patenting perspective of PROTACs based EGFR degraders

P Li, B Li, N Yang, T Xu, Z Zheng - Expert Opinion on Therapeutic …, 2023 - Taylor & Francis
Introduction Abnormal expression of epidermal growth factor receptor (EGFR) contributes to
tumor development, especially in non-small cell lung cancer (NSCLC). Although multiple …

A partial epithelial‐mesenchymal transition signature for highly aggressive colorectal cancer cells that survive under nutrient restriction

GA Pastorino, I Sheraj, K Huebner… - The Journal of …, 2024 - Wiley Online Library
Partial epithelial‐mesenchymal transition (p‐EMT) has recently been identified as a hybrid
state consisting of cells with both epithelial and mesenchymal characteristics and is …

[HTML][HTML] Targeted Strategies for Degradation of Key Transmembrane Proteins in Cancer

V Sakanyan, N Iradyan, R Alves de Sousa - BioTech, 2023 - mdpi.com
Targeted protein degradation is an attractive technology for cancer treatment due to its
ability to overcome the unpredictability of the small molecule inhibitors that cause resistance …

Design, Synthesis, and Biological Evaluation of Novel EGFR PROTACs Targeting C797S Mutation

Y Zhu, X Ye, Y Wu, H Shen, Z Cai, F Xia… - Journal of Medicinal …, 2024 - ACS Publications
The epidermal growth factor receptor (EGFR) tertiary C797S mutation is an important cause
of resistance to Osimertinib, which seriously hinders the clinical application of Osimertinib …

Discovery of Potent SOS1 PROTACs with Effective Antitumor Activities against NCI-H358 Tumor Cells In Vitro/In Vivo

X Pang, D Cui, B Lv, CY Wang - Journal of Medicinal Chemistry, 2024 - ACS Publications
Directly targeted KRAS inhibitors are now facing resistance problems, which might be
partially solved by the combination of SOS1 inhibitors with KRAS inhibitors. However, this …

Exploring the structural activity relationship of the osimertinib: A covalent inhibitor of double mutant EGFRL858R/T790M tyrosine kinase for the treatment of Non-Small …

BR Patil, KV Bhadane, I Ahmad, YJ Agrawal… - Bioorganic & Medicinal …, 2024 - Elsevier
The USFDA granted regular approval to Osimertinib (AZD9291) on March 30, 2017, for
treating individuals with metastatic Non-Small Cell Lung Cancer having EGFR T790M …

Transforming Cancer Care: Immunotherapy with Advanced Drug Delivery

S Srivastava, TC Siang, D Kaliyappan… - Journal of Drug Delivery …, 2024 - Elsevier
This study investigates the integration of immunotherapeutic agents into various drug
delivery platforms for cancer treatment, emphasizing their efficacy in diverse cancer types …

Design, Synthesis, and Anticancer Evaluation of Hemithioindigos via Inhibition of Human Topoisomerases

M Kaur, P Suman, S Arora, T Singh, A Munshi… - …, 2023 - Wiley Online Library
Hemithioindigos were designed as topoisomerase inhibitors, synthesized, and evaluated for
their anticancer properties against lung (A549) and breast (MDA‐MB‐468 and MCF7) …

In silico construction and evaluation of anti-EGFR ScFv and IFN-β fusion protein as a novel immunocytokine for the treatment of HER1 positive breast cancer

MI Khan, M Hassan, A Sohail, N Ahmad, I Khan… - 2023 - researchsquare.com
Context Human epidermal growth factor receptor 1 (HER1) positive breast cancer is
characterized by overexpression of the HER1 receptor protein on cancer cells leading to …