@article{1960c8a9ca0346408b5e5d607527e968,
title = "Advances in Activity-Based Sensing Probes for Isoform-Selective Imaging of Enzymatic Activity",
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.",
keywords = "activity-based sensing, fluorescence, molecular imaging, probe development, rational design",
author = "Gardner, {Sarah H.} and Reinhardt, {Christopher J.} and Jefferson Chan",
note = "C.J.R. thanks the Chemistry‐Biology Interface Training Grant (T32 GM070421) and the Seemon Pines Graduate Fellowship for support. J.C. acknowledges the National Institutes of Health (R35GM133581) for funding. Molecular graphics and analyses were performed with UCSF Chimera, developed by the Resource for Biocomputing, Visualization, and Informatics at the University of California, San Francisco, with support from NIH P41‐GM103311. . Sarah Gardner graduated from the University of Iowa in 2017 with a BSc in Biochemistry. With financial support from the Fight for Sight organization, she performed research in the laboratory of Prof. Sheila Baker. She is currently pursuing a PhD in Biochemistry with Prof. Jeff Chan at UIUC. Her research interests include the development and evaluation of chemical tools to study the roles of reactive aldehydes in the context of cancer and aging C.J.R. thanks the Chemistry-Biology Interface Training Grant (T32 GM070421) and the Seemon Pines Graduate Fellowship for support. J.C. acknowledges the National Institutes of Health (R35GM133581) for funding. Molecular graphics and analyses were performed with UCSF Chimera, developed by the Resource for Biocomputing, Visualization, and Informatics at the University of California, San Francisco, with support from NIH P41-GM103311.[94]",
year = "2021",
month = mar,
day = "1",
doi = "10.1002/anie.202003687",
language = "English (US)",
volume = "60",
pages = "5000--5009",
journal = "Angewandte Chemie - International Edition",
issn = "1433-7851",
publisher = "John Wiley & Sons, Ltd.",
number = "10",
}