BAX activation is initiated at a novel interaction site

Nature. 2008 Oct 23;455(7216):1076-81. doi: 10.1038/nature07396.

Abstract

BAX is a pro-apoptotic protein of the BCL-2 family that is stationed in the cytosol until activated by a diversity of stress stimuli to induce cell death. Anti-apoptotic proteins such as BCL-2 counteract BAX-mediated cell death. Although an interaction site that confers survival functionality has been defined for anti-apoptotic proteins, an activation site has not been identified for BAX, rendering its explicit trigger mechanism unknown. We previously developed stabilized alpha-helix of BCL-2 domains (SAHBs) that directly initiate BAX-mediated mitochondrial apoptosis. Here we demonstrate by NMR analysis that BIM SAHB binds BAX at an interaction site that is distinct from the canonical binding groove characterized for anti-apoptotic proteins. The specificity of the human BIM-SAHB-BAX interaction is highlighted by point mutagenesis that disrupts functional activity, confirming that BAX activation is initiated at this novel structural location. Thus, we have now defined a BAX interaction site for direct activation, establishing a new target for therapeutic modulation of apoptosis.

Publication types

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

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Apoptosis
  • Apoptosis Regulatory Proteins / chemistry
  • Apoptosis Regulatory Proteins / metabolism
  • BH3 Interacting Domain Death Agonist Protein / metabolism
  • Bcl-2-Like Protein 11
  • Cell Line
  • Gene Expression Regulation*
  • Humans
  • Membrane Proteins / chemistry
  • Membrane Proteins / metabolism
  • Mice
  • Mutagenesis, Site-Directed
  • Mutation / genetics
  • Nuclear Magnetic Resonance, Biomolecular
  • Protein Binding
  • Proto-Oncogene Proteins / chemistry
  • Proto-Oncogene Proteins / metabolism
  • Sequence Alignment
  • bcl-2-Associated X Protein / chemistry
  • bcl-2-Associated X Protein / metabolism*

Substances

  • Apoptosis Regulatory Proteins
  • BAX protein, human
  • BCL2L11 protein, human
  • BH3 Interacting Domain Death Agonist Protein
  • BID protein, human
  • Bcl-2-Like Protein 11
  • Bcl2l11 protein, mouse
  • Membrane Proteins
  • Proto-Oncogene Proteins
  • bcl-2-Associated X Protein

Associated data

  • PDB/2K7W