1 publication

1 publication

Intracellular Reactions Promoted by Bis(histidine) Miniproteins Stapled Using Palladium(II) Complexes

Mascareñas, J.L.

Angew. Chem. Int. Ed. 2020, 59, 9149-9154, 10.1002/anie.202002032

The generation of catalytically active metalloproteins inside living mammalian cells is a major research challenge at the interface between catalysis and cell biology. Herein we demonstrate that basic domains of bZIP transcription factors, mutated to include two histidine residues at i and i+4 positions, react with palladium(II) sources to generate catalytically active, stapled pallado-miniproteins. The resulting constrained peptides are efficiently internalized into living mammalian cells, where they perform palladium-promoted depropargylation reactions without cellular fixation. Control experiments confirm the requirement of the peptide scaffolding and the palladium staple for attaining the intracellular reactivity.

Metal: Pd
Ligand type: Amino acid
Anchoring strategy: Dative
Optimization: Genetic
Reaction: Depropargylation
Max TON: ---
ee: ---
PDB: ---
Notes: Whole cell catalysis