Inhibitors to degraders: Changing paradigm in drug discovery,iScience

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Inhibitors to degraders: Changing paradigm in drug discovery
iScience ( IF 4.6 ) Pub Date : 2024-03-26 , DOI: 10.1016/j.isci.2024.109574
V Haridas _{1,

2} , Souvik Dutta ₁ , Akshay Munjal ₃ , Shailja Singh ₃

Affiliation

The chemical understanding of biological processes provides not only a deeper insight but also a solution to abnormal biological functioning. Protein degradation, a natural biological process for debris removal in the cell, has been studied for years. The recent finding that natural degradation pathways can be utilized for therapeutic purposes is a paradigm shift in the drug discovery approach. Methods such as Proteolysis Targeting Chimera (PROTAC), lysosomal targeting chimera, hydrophobic tagging, AUtophagy TArgeting Chimera, AUTOphagy TArgeting Chimera and several other variants of these methods have made a considerable impact on the way of drug design. Few selected examples testify that a huge wave of change is on the way. The drug design based on the targeted protein degradation is a powerful tool in our arsenal. More molecules will be invented that will uncover the hidden secrets of biological functioning and provide enduring solutions to several unmet medical needs.

中文翻译：

降解剂抑制剂：改变药物发现的范式

对生物过程的化学理解不仅提供了更深入的见解，而且为异常的生物功能提供了解决方案。蛋白质降解是细胞中去除碎片的一种自然生物过程，已经研究了多年。最近发现自然降解途径可用于治疗目的，这是药物发现方法的范式转变。诸如蛋白水解靶向嵌合体（PROTAC）、溶酶体靶向嵌合体、疏水标记、AUtophagy TArgeting Chimera、AUTOphagy TArgeting Chimera 等方法以及这些方法的其他几种变体对药物设计方式产生了相当大的影响。很少有选定的例子证明，一场巨大的变革浪潮正在到来。基于靶向蛋白质降解的药物设计是我们武器库中的强大工具。将发明更多分子，揭开生物功能的隐藏秘密，并为一些未满足的医疗需求提供持久的解决方案。

更新日期：2024-03-26

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