Regulation of apoptosis by an intrinsically disordered region of Bcl-xL

Nat Chem Biol. 2018 May;14(5):458-465. doi: 10.1038/s41589-018-0011-x. Epub 2018 Mar 5.

Abstract

Intrinsically disordered regions (IDRs) of proteins often regulate function upon post-translational modification (PTM) through interactions with folded domains. An IDR linking two α-helices (α1-α2) of the antiapoptotic protein Bcl-xL experiences several PTMs that reduce antiapoptotic activity. Here, we report that PTMs within the α1-α2 IDR promote its interaction with the folded core of Bcl-xL that inhibits the proapoptotic activity of two types of regulatory targets, BH3-only proteins and p53. This autoregulation utilizes an allosteric pathway whereby, in one direction, the IDR induces a direct displacement of p53 from Bcl-xL coupled to allosteric displacement of simultaneously bound BH3-only partners. This pathway operates in the opposite direction when the BH3-only protein PUMA binds to the BH3 binding groove of Bcl-xL, directly displacing other bound BH3-only proteins, and allosterically remodels the distal site, displacing p53. Our findings show how an IDR enhances functional versatility through PTM-dependent allosteric regulation of a folded protein domain.

Publication types

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

MeSH terms

  • Allosteric Site
  • Apoptosis*
  • Binding Sites
  • Gene Expression Regulation*
  • Humans
  • Intrinsically Disordered Proteins / genetics
  • Intrinsically Disordered Proteins / metabolism*
  • Kinetics
  • Mutation
  • Protein Binding
  • Protein Domains
  • Protein Folding
  • Protein Processing, Post-Translational
  • Protein Structure, Secondary
  • Signal Transduction
  • Tumor Suppressor Protein p53 / metabolism*
  • bcl-X Protein / genetics
  • bcl-X Protein / metabolism*

Substances

  • BCL2L1 protein, human
  • Intrinsically Disordered Proteins
  • TP53 protein, human
  • Tumor Suppressor Protein p53
  • bcl-X Protein