Scholarlink

<p>Kinase inhibitors are commonly used in research and clinical practice. Among them, irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs), such as afatinib and osimertinib, constitute an important subclass. The aim of this study was to create an irreversible covalent EGFR TKI exhibiting endogenous fluorescence, i.e., intrinsic fluorescence without the need for additional fluorochromes. These compounds, designated SQI-2, SLT40, and SLT41, were successfully developed and shown to effectively inhibit the EGFR, EGFR<sup>L858R/T790M</sup>, and EGFR<sup>vIII</sup> kinases. The developed compounds are suitable for a range of cytochemical analyses, including real-time assays. The proposed TKIs may serve as research and diagnostic tools and represent precursors of new types of therapeutic compounds.</p>

错误：搜索内容不能为空，请输入英文关键词
错误：关键词超出字数限制，请精简
高级检索

Novel EGFR tyrosine kinase inhibitors exhibiting intrinsic fluorescence

  • 期刊论文

  • 出版模式：

    开放获取

  • 发表日期：

    2026年7月23日

查看全文
  • Amelia Kierasińska-Kałka,
  • Adrianna Rutkowska,
  • Jacek Mularski,
  • Marcin Pacholczyk,
  • Tadeusz Strózik,
  • Joanna Pęciak,
  • Cezary Tręda,
  • Klaudia Waszczykowska,
  • Marta Orlikowska,
  • Dominika Wyrzykowska,
  • Kamil Filiks,
  • Maria Jaskólska,
  • Jakub Bartkowiak,
  • Ewelina Stoczyńska-Fidelus,
  • Piotr Rieske

摘要

Kinase inhibitors are commonly used in research and clinical practice. Among them, irreversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors (TKIs), such as afatinib and osimertinib, constitute an important subclass. The aim of this study was to create an irreversible covalent EGFR TKI exhibiting endogenous fluorescence, i.e., intrinsic fluorescence without the need for additional fluorochromes. These compounds, designated SQI-2, SLT40, and SLT41, were successfully developed and shown to effectively inhibit the EGFR, EGFRL858R/T790M, and EGFRvIII kinases. The developed compounds are suitable for a range of cytochemical analyses, including real-time assays. The proposed TKIs may serve as research and diagnostic tools and represent precursors of new types of therapeutic compounds.