Botulinum neurotoxin is shielded by NTNHA in an interlocked complex

Science. 2012 Feb 24;335(6071):977-81. doi: 10.1126/science.1214270.

Abstract

Botulinum neurotoxins (BoNTs) are highly poisonous substances that are also effective medicines. Accidental BoNT poisoning often occurs through ingestion of Clostridium botulinum-contaminated food. Here, we present the crystal structure of a BoNT in complex with a clostridial nontoxic nonhemagglutinin (NTNHA) protein at 2.7 angstroms. Biochemical and functional studies show that NTNHA provides large and multivalent binding interfaces to protect BoNT from gastrointestinal degradation. Moreover, the structure highlights key residues in BoNT that regulate complex assembly in a pH-dependent manner. Collectively, our findings define the molecular mechanisms by which NTNHA shields BoNT in the hostile gastrointestinal environment and releases it upon entry into the circulation. These results will assist in the design of small molecules for inhibiting oral BoNT intoxication and of delivery vehicles for oral administration of biologics.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Bacterial Proteins / chemistry*
  • Bacterial Proteins / metabolism
  • Binding Sites
  • Botulinum Toxins, Type A / chemistry*
  • Botulinum Toxins, Type A / metabolism
  • Crystallography, X-Ray
  • Hydrogen-Ion Concentration
  • Models, Molecular
  • Molecular Sequence Data
  • Multiprotein Complexes / chemistry
  • Multiprotein Complexes / metabolism
  • Mutagenesis
  • Protein Binding
  • Protein Conformation
  • Protein Interaction Domains and Motifs
  • Protein Structure, Secondary

Substances

  • Bacterial Proteins
  • Multiprotein Complexes
  • Botulinum Toxins, Type A

Associated data

  • PDB/3V0A
  • PDB/3V0B
  • PDB/3V0C