Chemical Tools to Image the Activity of PAR-Cleaving Proteases

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