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Activatable covalent labeling probes: design, mechanism, and biological applications

Yinxing Miao, Yuyang Tian, Deju Ye

2025Chemical Society Reviews12 citationsDOI

Abstract

imaging. This review provides a comprehensive overview of the design principles, activation strategies focusing on enzymatic and photochemical triggers, and key biomedical applications, while critically assessing challenges related to stability, pharmacokinetics, and clinical translation. By integrating chemical probe engineering with translational research, we highlight the transformative potential of stimuli-activatable covalent labeling probes for protein profiling, disease diagnosis, therapeutic monitoring, and real-time visualization of biological processes.

Topics & Concepts

Covalent bondChemistryBiomoleculeCombinatorial chemistryNanotechnologyChemical biologyPosttranslational modificationClick chemistryBiophysicsBiosensorBiochemistryMolecular probeMechanism (biology)Target proteinComputational biologyEnzymeBiocompatible materialCovalent bindingBioorthogonal chemistrySurface modificationClick Chemistry and ApplicationsAdvanced Polymer Synthesis and CharacterizationBiotin and Related Studies
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