Issue 28, 2021

Molecular probes for selective detection of cysteine cathepsins

Abstract

Cysteine cathepsins are proteases critical in physiopathological processes and show potential as targets or biomarkers for diseases and medical conditions. The 11 members of the cathepsin family are redundant in some cases but remarkably independent of others, demanding the development of both pan-cathepsin targeting tools as well as probes that are selective for specific cathepsins with little off-target activity. This review addresses the diverse design strategies that have been employed to accomplish this tailored selectivity among cysteine cathepsin targets and the imaging modalities incorporated. The power of these diverse tools is contextualized by briefly highlighting the nature of a few prominent cysteine cathepsins, their involvement in select diseases, and the application of cathepsin imaging probes in research spanning basic biochemical studies to clinical applications.

Graphical abstract: Molecular probes for selective detection of cysteine cathepsins

Supplementary files

Article information

Article type
Review Article
Submitted
05 Feb 2021
Accepted
19 Mar 2021
First published
29 Mar 2021

Org. Biomol. Chem., 2021,19, 6182-6205

Author version available

Molecular probes for selective detection of cysteine cathepsins

K. A. Schleyer and L. Cui, Org. Biomol. Chem., 2021, 19, 6182 DOI: 10.1039/D1OB00225B

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