期刊
ANNUAL REVIEW OF BIOCHEMISTRY, VOL 83
卷 83, 期 -, 页码 249-273出版社
ANNUAL REVIEWS
DOI: 10.1146/annurev-biochem-060713-035352
关键词
activity-based probes; proteomics; mass spectrometry; affinity handle; fluorescent imaging
资金
- NATIONAL INSTITUTE OF BIOMEDICAL IMAGING AND BIOENGINEERING [R01EB005011] Funding Source: NIH RePORTER
- NIBIB NIH HHS [R01-EB005011] Funding Source: Medline
Proteolytic enzymes are key signaling molecules in both normal physiological processes and various diseases. After synthesis, protease activity is tightly controlled. Consequently, levels of protease messenger RNA and protein often are not good indicators of total protease activity. To more accurately assign function to new proteases, investigators require methods that can be used to detect and quantify proteolysis. In this review, we describe basic principles, recent advances, and applications of biochemical methods to track protease activity, with an emphasis on the use of activity-based probes (ABPs) to detect protease activity. We describe ABP design principles and use case studies to illustrate the application of ABPs to protease enzymology, discovery and development of protease-targeted drugs, and detection and validation of proteases as biomarkers.
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