Chemical Tools to Image the Activity of PAR-Cleaving Proteases

IF 3.8 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY ACS Bio & Med Chem Au Pub Date : 2023-05-27 DOI:10.1021/acsbiomedchemau.3c00019
Irene Y. Lee, Piyapa Tantisirivat and Laura E. Edgington-Mitchell*, 
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Abstract

Protease-activated receptors (PARs) comprise a family of four G protein-coupled receptors (GPCRs) that have broad functions in health and disease. Unlike most GPCRs, PARs are uniquely activated by proteolytic cleavage of their extracellular N termini. To fully understand PAR activation and function in vivo, it is critical to also study the proteases that activate them. As proteases are heavily regulated at the post-translational level, measures of total protease abundance have limited utility. Measures of protease activity are instead required to inform their function. This review will introduce several classes of chemical probes that have been developed to measure the activation of PAR-cleaving proteases. Their strengths, weaknesses, and applications will be discussed, especially as applied to image protease activity at the whole organism, tissue, and cellular level.

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化学工具成像par切割蛋白酶的活性
蛋白酶激活受体(PAR)包括一个由四个G蛋白偶联受体(GPCR)组成的家族,在健康和疾病中具有广泛的功能。与大多数GPCR不同,PAR通过蛋白水解裂解其细胞外N末端而被独特激活。为了充分了解标准杆数在体内的激活和功能,研究激活它们的蛋白酶也是至关重要的。由于蛋白酶在翻译后水平上受到严重调节,因此总蛋白酶丰度的测量作用有限。相反,需要蛋白酶活性的测量来告知它们的功能。这篇综述将介绍几类化学探针,这些探针已被开发用于测量PAR-离去蛋白酶的激活。将讨论它们的优点、缺点和应用,特别是应用于整个生物体、组织和细胞水平的图像蛋白酶活性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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来源期刊
ACS Bio & Med Chem Au
ACS Bio & Med Chem Au 药物、生物、化学-
CiteScore
4.10
自引率
0.00%
发文量
0
期刊介绍: ACS Bio & Med Chem Au is a broad scope open access journal which publishes short letters comprehensive articles reviews and perspectives in all aspects of biological and medicinal chemistry. Studies providing fundamental insights or describing novel syntheses as well as clinical or other applications-based work are welcomed.This broad scope includes experimental and theoretical studies on the chemical physical mechanistic and/or structural basis of biological or cell function in all domains of life. It encompasses the fields of chemical biology synthetic biology disease biology cell biology agriculture and food natural products research nucleic acid biology neuroscience structural biology and biophysics.The journal publishes studies that pertain to a broad range of medicinal chemistry including compound design and optimization biological evaluation molecular mechanistic understanding of drug delivery and drug delivery systems imaging agents and pharmacology and translational science of both small and large bioactive molecules. Novel computational cheminformatics and structural studies for the identification (or structure-activity relationship analysis) of bioactive molecules ligands and their targets are also welcome. The journal will consider computational studies applying established computational methods but only in combination with novel and original experimental data (e.g. in cases where new compounds have been designed and tested).Also included in the scope of the journal are articles relating to infectious diseases research on pathogens host-pathogen interactions therapeutics diagnostics vaccines drug-delivery systems and other biomedical technology development pertaining to infectious diseases.
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