Department of Pharmacy and Biotechnology, Alma Mater Studiorum-University of Bologna, Via Belmeloro 6, 40126, Bologna, Italy.
ChemMedChem. 2023 Oct 17;18(20):e202300422. doi: 10.1002/cmdc.202300422. Epub 2023 Sep 14.
Click chemistry is universally recognized as a powerful strategy for the fast and precise assembly of diverse building blocks. Targeted Protein Degradation (TPD) is a new therapeutic modality based on heterobifunctional small-molecule degraders that provides new opportunities to medicinal chemists dealing with undruggable targets and incurable diseases. Here, we highlight how very recently the TPD field and that of click chemistry have merged, opening up the possibility for fine-tuning the properties of a degrader, chemically assembled through a "click" synthesis. By reviewing concrete examples, we want to provide the reader with the insight that the application of click and bioorthogonal chemistry in the TDP field may be a winning combination.
点击化学被普遍认为是一种快速、精确地组装各种构建块的强大策略。靶向蛋白降解（TPD）是一种基于杂双功能小分子降解剂的新型治疗模式，为药物化学家处理不可成药的靶点和不治之症提供了新的机会。在这里，我们强调了最近 TPD 领域和点击化学领域是如何融合的，为通过“点击”合成化学组装的降解剂的特性微调开辟了可能性。通过回顾具体的例子，我们希望让读者了解到，点击化学和生物正交化学在 TDP 领域的应用可能是一个成功的组合。
