Structural basis for the product specificity of histone lysine methyltransferases

Mol Cell. 2003 Jul;12(1):177-85. doi: 10.1016/s1097-2765(03)00224-7.

Abstract

DIM-5 is a SUV39-type histone H3 Lys9 methyltransferase that is essential for DNA methylation in N. crassa. We report the structure of a ternary complex including DIM-5, S-adenosyl-L-homocysteine, and a substrate H3 peptide. The histone tail inserts as a parallel strand between two DIM-5 strands, completing a hybrid sheet. Three post-SET cysteines coordinate a zinc atom together with Cys242 from the SET signature motif (NHXCXPN) near the active site. Consequently, a narrow channel is formed to accommodate the target Lys9 side chain. The sulfur atom of S-adenosyl-L-homocysteine, where the transferable methyl group is to be attached in S-adenosyl-L-methionine, lies at the opposite end of the channel, approximately 4 A away from the target Lys9 nitrogen. Structural comparison of the active sites of DIM-5, an H3 Lys9 trimethyltransferase, and SET7/9, an H3 Lys4 monomethyltransferase, allowed us to design substitutions in both enzymes that profoundly alter their product specificities without affecting their catalytic activities.

Publication types

  • Comparative Study
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Catalytic Domain / physiology
  • Cysteine / chemistry
  • Histone Methyltransferases
  • Histone-Lysine N-Methyltransferase*
  • Histones / chemistry*
  • Lysine / chemistry
  • Macromolecular Substances
  • Methyltransferases / chemistry*
  • Models, Molecular
  • Molecular Structure
  • Neurospora crassa / enzymology*
  • Peptides / chemistry
  • Protein Methyltransferases
  • Protein Structure, Tertiary / physiology
  • S-Adenosylhomocysteine / chemistry*
  • Sulfur / chemistry
  • Zinc / chemistry

Substances

  • Histones
  • Macromolecular Substances
  • Peptides
  • Sulfur
  • S-Adenosylhomocysteine
  • Histone Methyltransferases
  • Methyltransferases
  • Protein Methyltransferases
  • Histone-Lysine N-Methyltransferase
  • Zinc
  • Lysine
  • Cysteine

Associated data

  • PDB/1PEG