Takuya Machida; Som Dutt; Nicolas Winssinger
Angew. Chem. Int. Ed. Engl., 2016, 55, 8595-8598
https://doi.org/10.1002/anie.201602751

Abstract

The importance of spatial organization in short peptide catalysts is well recognized. We synthesized and screened a library of peptides flanked by peptide nucleic acids (PNAs) such that the peptide would be constrained in a hairpin loop upon hybridization. A screen for phosphatase activity led to the discovery of a catalyst with >25‐fold rate acceleration over the linear peptide. We demonstrated that the hybridization‐enforced folding of the peptide is necessary for activity, and designed a catalyst that is allosterically controlled using a complementary PNA sequence.