Interrogating Protein Phosphatases with Chemical Activity Probes

• Published in: Chemistry : a European journal 2018-06, Vol.24 (31), p.7810-7824
• Main Authors: Casey, Garrett R., Stains, Cliff I.
• Format: Article
• Language: English
• Subjects: Animals; Biomarkers - chemistry; Biomarkers - metabolism; biosensors; Chemical activity; Chemistry; Fluorescence; Fluorescent Dyes - chemistry; Fluorescent indicators; fluorescent probes; Humans; Kinetics; Molecular chains; Organic chemistry; Phosphatase; Phosphoprotein Phosphatases - chemistry; Phosphoprotein Phosphatases - metabolism; Probes; Proteins; Reviews; sensors; Signal Transduction
• ISSN: 0947-6539; 1521-3765
• DOI: 10.1002/chem.201705194

Protein phosphatases, while long overlooked, have recently become appreciated as drivers of both normal‐ and disease‐associated signaling events. As a result, the spotlight is now turning torwards this enzyme family and efforts geared towards the development of modern chemical tools for studying these enzymes are well underway. This Minireview focuses on the evolution of chemical activity probes, both optical and covalent, for the study of protein phosphatases. Small‐molecule probes, global monitoring of phosphatase activity through the use of covalent modifiers, and targeted fluorescence‐based activity probes are discussed. We conclude with an overview of open questions in the field and highlight the potential impact of chemical tools for studying protein phosphatases. Illuminating Protein Phosphatases: Protein phosphatases are becoming recognized as critical signaling enzymes in both normal and disease physiology. Chemical reporters of enzymatic activity are poised to provide insights into the chemical biology of these important signaling enzymes.