Enzyme-activated probes in optical imaging: a focus on atherosclerosis

Enzyme-activated probes enable complex biological processes to be studied in real-time. A wide range of enzymes are modulated in diseases, including cancer, inflammatory diseases and cardiovascular disease, and have the potential to act as vital diagnostic and prognostic biomarkers to monitor and report on disease progression. In this perspective article, we discuss suitable design characteristics of enzyme-activated fluorescent probes for ex vivo and in vivo optical imaging applications. With a particular focus on atherosclerosis imaging, we highlight recent approaches to report on the activity of cathepsins (K and B), matrix metalloproteinases (MMP-2 and MMP-9), thrombin, heme oxygenase-1 (HO-1) and myeloperoxidase (MPO).
This perspective provides an overview of the design requirements and fluorogenic mechanisms of enzyme-activatable probes in optical imaging, focusing particularly on detecting enzymatic targets overexpressed in vulnerable atherosclerotic plaque.