C-prenylated flavonoids possess notable pharmaceutical potential, but their production is hindered by the challenging selective prenylation of their unstable polyphenolic cores. Here, the authors present a directed evolution strategy to reshape the active pocket of the prenyltransferase AtaPT, uncovering an aromatic cage that governs both regioselectivity and donor specificity, and achieve efficient and scalable synthesis of 27 C-prenylated flavonoids.
- Ruiying Qiu
- Huisi Huang
- Jian-bo Wang
