Catalytic Lysine745 targeting strategy in fourth-generation EGFR tyrosine kinase inhibitors to address C797S mutation resistance

Overcoming resistance to third-generation tyrosine kinase inhibitors (TKIs) such as Osimertinib, particularly due to the emergence of the C797S mutation, remains a key challenge in non-small cell lung cancer (NSCLC) therapy. This review highlights recent advancements in the development of fourth-gen...

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Veröffentlicht in:	European journal of medicinal chemistry 2025-02, Vol.283, p.117140, Article 117140
Hauptverfasser:	Patil, Bhatu R., Patel, Harun M.
Format:	Artikel
Sprache:	eng
Schlagworte:	Antineoplastic Agents - chemical synthesis Antineoplastic Agents - chemistry Antineoplastic Agents - pharmacology Brigatinib C797S Carcinoma, Non-Small-Cell Lung - drug therapy Carcinoma, Non-Small-Cell Lung - genetics Catalytic Lys745 Drug Resistance, Neoplasm - drug effects ErbB Receptors - antagonists & inhibitors ErbB Receptors - genetics ErbB Receptors - metabolism Humans Lung Neoplasms - drug therapy Lung Neoplasms - pathology Lysine - chemistry Molecular Docking Simulation Molecular Structure Mutation Non-small cell lung cancer Osimertinib Protein Kinase Inhibitors - chemical synthesis Protein Kinase Inhibitors - chemistry Protein Kinase Inhibitors - pharmacology Structure-Activity Relationship Tyrosine Kinase Inhibitors
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