Advances in Activity-Based Sensing Probes for IsoformSelective Imaging of Enzymatic Activity

酶活性选择性成像的活性传感探针的研究进展

主讲人：唐丹丹

Angewandte Chemie International  | April 2021 | Volume 60, Issue 10 | Pasges5000-5009 | https://doi.org/10.1002/anie.202003687

Abstract：

      Until recently, there were no generalizable methods for assessing the effects of post-translational regulation on enzymatic activity. Activitybased sensing (ABS) has emerged as a powerful approach for monitoring small-molecule and enzyme activities within living systems. Initial examples of ABS were applied for measuring general enzymatic activity; however, a recent focus has been placed on increasing the selectivity to monitor a single enzyme or isoform. The highest degree of selectivity is required for differentiating between isoforms, where the targets display significant structural similarities as a result of a gene duplication or alternative splicing. This Minireview highlights key examples of small-molecule isoform-selective probes with a focus on the relevance of isoform differentiation, design strategies to achieve selectivity, and applications in basic biology or in the clinic.

摘要：

  直到最近，还没有一种可推广的方法来评估翻译后调节对酶活性的影响。基于活性的传感（ABS）已经成为监测生命系统中小分子和酶活性的强大方法。ABS的最初例子被用于测量一般的酶活性；然而，最近的重点放在提高监测单一酶或亚型的选择性上。区分不同的亚型需要最高程度的选择性，即由于基因重复或选择性剪接，目标显示出显著的结构相似性。这篇小型综述强调了小分子亚型选择性探针的关键例子，重点关注亚型分化的相关性、实现选择性的设计策略以及在基础生物学或临床中的应用。