A rationally-designed chimeric KDM1A/KDM1B histone demethylase tower domain deletion mutant retaining enzymatic activity

FEBS Lett. 2015 Aug 19;589(18):2340-6. doi: 10.1016/j.febslet.2015.07.028. Epub 2015 Jul 29.

Abstract

A target with therapeutic potential, lysine-specific demethylase 1A (KDM1A) is a regulator of gene expression whose tower domain is a protein-protein interaction motif. This domain facilitates the interaction of KDM1A with coregulators and multiprotein complexes that direct its activity to nucleosomes. We describe the design and characterization of a chimeric 'towerless' KDM1A, termed nΔ150 KDM1AΔTower KDM1B chimera (chKDM1AΔTower), which incorporates a region from the paralog lysine-specific demethylase 1B (KDM1B). This chimera copurifies with FAD and displays demethylase activity, but fails to bind the partner protein corepressor of the RE1-silencing transcription factor (CoREST). We conclude that KDM1A catalysis can be decoupled from tower-dependent interactions, lending chKDM1AΔTower useful for dissecting molecular contributions to KDM1A function.

Keywords: Chimera; CoREST; Deletion mutant; Enzyme engineering; KDM1A/LSD1; Tower domain.

Publication types

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

MeSH terms

  • Amino Acid Sequence
  • Histone Demethylases / chemistry*
  • Histone Demethylases / genetics
  • Histone Demethylases / isolation & purification
  • Histone Demethylases / metabolism*
  • Humans
  • Models, Molecular
  • Molecular Sequence Data
  • Protein Engineering*
  • Protein Structure, Tertiary
  • Recombinant Fusion Proteins / chemistry*
  • Recombinant Fusion Proteins / genetics
  • Recombinant Fusion Proteins / isolation & purification
  • Recombinant Fusion Proteins / metabolism*
  • Sequence Deletion*

Substances

  • Recombinant Fusion Proteins
  • Histone Demethylases
  • KDM1A protein, human