Structure of p300 in complex with acyl-CoA variants

Nat Chem Biol. 2017 Jan;13(1):21-29. doi: 10.1038/nchembio.2217. Epub 2016 Oct 31.

Abstract

Histone acetylation plays an important role in transcriptional activation. Histones are also modified by chemically diverse acylations that are frequently deposited by p300, a transcriptional coactivator that uses a number of different acyl-CoA cofactors. Here we report that while p300 is a robust acetylase, its activity gets weaker with increasing acyl-CoA chain length. Crystal structures of p300 in complex with propionyl-, crotonyl-, or butyryl-CoA show that the aliphatic portions of these cofactors are bound in the lysine substrate-binding tunnel in a conformation that is incompatible with substrate transfer. Lysine substrate binding is predicted to remodel the acyl-CoA ligands into a conformation compatible with acyl-chain transfer. This remodeling requires that the aliphatic portion of acyl-CoA be accommodated in a hydrophobic pocket in the enzymes active site. The size of the pocket and its aliphatic nature exclude long-chain and charged acyl-CoA variants, presumably explaining the cofactor preference for p300.

MeSH terms

  • Coenzyme A / chemistry*
  • Coenzyme A / metabolism
  • E1A-Associated p300 Protein / chemistry*
  • E1A-Associated p300 Protein / metabolism
  • Humans
  • Ligands
  • Models, Molecular
  • Protein Conformation

Substances

  • Ligands
  • E1A-Associated p300 Protein
  • EP300 protein, human
  • Coenzyme A