Trivalent metal complex geometry of the substrate governs cathepsin B enzymatic cleavage rate

Chem Commun (Camb). 2020 Jul 2;56(53):7289-7292. doi: 10.1039/d0cc02862b.

Abstract

The lysosomal protease cathepsin B recognizes defined, short peptide sequences, providing means for effective, targeted drug release. Here, we show that the introduction of a coordination complex adjacent to the cleavage sequence allows us to tune enzymatic cleavage rate by varying the complexed, trivalent metal ion.

MeSH terms

  • Amino Acid Sequence
  • Cathepsin B / metabolism*
  • Cations / chemistry
  • Chelating Agents / chemistry
  • Coordination Complexes / chemistry*
  • Coordination Complexes / metabolism*
  • Enzyme Activation
  • Kinetics
  • Lysosomes / chemistry
  • Metals / chemistry
  • Molecular Conformation
  • Structure-Activity Relationship

Substances

  • Cations
  • Chelating Agents
  • Coordination Complexes
  • Metals
  • Cathepsin B