Abstract

A small-molecule ligand-directed caging strategy enables the localized modulation of endogenous enzyme activity with high temporal precision without genetic engineering, as reported by Yiyun Chen and co-workers in their Research Article (e202115472). The small-molecule ligands deactivate the endogenous DNA alkyltransferase by caging the enzyme's active site inside live cells. Light irradiation on demand releases the enzyme's active site to restore activity.

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