Advances in Activity-Based Sensing Probes for Isoform-Selective Imaging of Enzymatic Activity

Sarah H. Gardner, Christopher J. Reinhardt, Jefferson Chan

Research output: Contribution to journalReview articlepeer-review

Abstract

Until recently, there were no generalizable methods for assessing the effects of post-translational regulation on enzymatic activity. Activity-based 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.

Original languageEnglish (US)
JournalAngewandte Chemie - International Edition
DOIs
StateAccepted/In press - 2020

Keywords

  • activity-based sensing
  • fluorescence
  • molecular imaging
  • probe development
  • rational design

ASJC Scopus subject areas

  • Catalysis
  • Chemistry(all)

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