NeissLock provides an inducible protein anhydride for covalent targeting of endogenous proteins

Nat Commun. 2021 Jan 29;12(1):717. doi: 10.1038/s41467-021-20963-5.

Abstract

The Neisseria meningitidis protein FrpC contains a self-processing module (SPM) undergoing autoproteolysis via an aspartic anhydride. Herein, we establish NeissLock, using a binding protein genetically fused to SPM. Upon calcium triggering of SPM, the anhydride at the C-terminus of the binding protein allows nucleophilic attack by its target protein, ligating the complex. We establish a computational tool to search the Protein Data Bank, assessing proximity of amines to C-termini. We optimize NeissLock using the Ornithine Decarboxylase/Antizyme complex. Various sites on the target (α-amine or ε-amines) react with the anhydride, but reaction is blocked if the partner does not dock. Ligation is efficient at pH 7.0, with half-time less than 2 min. We arm Transforming Growth Factor-α with SPM, enabling specific covalent coupling to Epidermal Growth Factor Receptor at the cell-surface. NeissLock harnesses distinctive protein chemistry for high-yield covalent targeting of endogenous proteins, advancing the possibilities for molecular engineering.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anhydrides / metabolism
  • Animals
  • Bacterial Proteins / genetics*
  • Membrane Proteins / genetics*
  • Molecular Imaging / methods
  • Molecular Probes / chemistry
  • Molecular Probes / genetics
  • Molecular Probes / metabolism*
  • Protein Engineering / methods*
  • Proteolysis
  • Recombinant Fusion Proteins / chemistry
  • Recombinant Fusion Proteins / genetics
  • Recombinant Fusion Proteins / metabolism*
  • Staining and Labeling / methods*

Substances

  • Anhydrides
  • Bacterial Proteins
  • Membrane Proteins
  • Molecular Probes
  • Recombinant Fusion Proteins
  • frpC protein, Neisseria meningitidis