Scholarlink

This chapter provides an overview of PROTAC mechanisms, challenges, and the pivotal role of click chemistry in addressing these challenges. Key applications discussed include in-situ PROTAC assembly to enhance permeability, conjugation with targeting moieties for improved selectivity, and rapid library construction for efficient screening. Kinetic considerations in click reactions are emphasized, alongside extensions to related degradation strategies beyond PROTACs. Overall, the versatility of click chemistry is highlighted as a powerful tool for advancing PROTAC development and targeted protein degradation therapeutics.

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

Click Chemistry in the Development of PROTACs

  • 章节

  • 发表日期：

    2026年

查看全文
  • Ce Yang,
  • Hongliang Li,
  • Dongning Liu,
  • Yuancheng Li,
  • Binghe Wang

摘要

This chapter provides an overview of PROTAC mechanisms, challenges, and the pivotal role of click chemistry in addressing these challenges. Key applications discussed include in-situ PROTAC assembly to enhance permeability, conjugation with targeting moieties for improved selectivity, and rapid library construction for efficient screening. Kinetic considerations in click reactions are emphasized, alongside extensions to related degradation strategies beyond PROTACs. Overall, the versatility of click chemistry is highlighted as a powerful tool for advancing PROTAC development and targeted protein degradation therapeutics.