A Structural Insight Into Two Important ErbB Receptors (EGFR and HER2) and Their Relevance to Non‐Small Cell Lung Cancer DOI Creative Commons

Edanur Topalan,

Ahmet Büyükgüngör,

Melih Çiğdem

и другие.

Archiv der Pharmazie, Год журнала: 2025, Номер 358(4)

Опубликована: Апрель 1, 2025

ABSTRACT The epidermal growth factor receptor (EGFR) family, comprising tyrosine kinases (RTK) such as EGFR and HER2, plays a critical role in various signaling pathways related to cell proliferation, differentiation, growth. overactivation due aberrant can lead cancers, including non‐small lung cancer (NSCLC). To develop treatment for EGFR‐related NSCLC, several kinase inhibitors (TKIs) were designed: gefitinib, erlotinib, first‐generation; neratinib, dacomitinib second‐generation; osimertinib, lazertinib third‐generation, examples. However, the acquired resistance by mutations T790M C797S together with exon 20 insertion mutations, these drugs do not provide promising results NSCLC patients. development of fourth‐generation like EAI045 further innovative overcome this problem is must cure NSCLC. Among these, pyrazoline‐thiazole scaffolds are found effective EGFR‐HER2 against making them drug candidates. Although structures obtained so far family meaningful insights into mechanisms, quality quantity insufficient elucidate complete functions This review evaluates investigates their relation

Язык: Английский

A Structural Insight Into Two Important ErbB Receptors (EGFR and HER2) and Their Relevance to Non‐Small Cell Lung Cancer DOI Creative Commons

Edanur Topalan,

Ahmet Büyükgüngör,

Melih Çiğdem

и другие.

Archiv der Pharmazie, Год журнала: 2025, Номер 358(4)

Опубликована: Апрель 1, 2025

ABSTRACT The epidermal growth factor receptor (EGFR) family, comprising tyrosine kinases (RTK) such as EGFR and HER2, plays a critical role in various signaling pathways related to cell proliferation, differentiation, growth. overactivation due aberrant can lead cancers, including non‐small lung cancer (NSCLC). To develop treatment for EGFR‐related NSCLC, several kinase inhibitors (TKIs) were designed: gefitinib, erlotinib, first‐generation; neratinib, dacomitinib second‐generation; osimertinib, lazertinib third‐generation, examples. However, the acquired resistance by mutations T790M C797S together with exon 20 insertion mutations, these drugs do not provide promising results NSCLC patients. development of fourth‐generation like EAI045 further innovative overcome this problem is must cure NSCLC. Among these, pyrazoline‐thiazole scaffolds are found effective EGFR‐HER2 against making them drug candidates. Although structures obtained so far family meaningful insights into mechanisms, quality quantity insufficient elucidate complete functions This review evaluates investigates their relation

Язык: Английский

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