Site-Selective Sensing of Histone Methylation Enzyme Activity via an Arrayed Supramolecular Tandem Assay

J Am Chem Soc. 2017 Aug 16;139(32):10964-10967. doi: 10.1021/jacs.7b05002. Epub 2017 Aug 8.

Abstract

Arrayed deep cavitands can be coupled to a fluorescence-based supramolecular tandem assay that allows site-selective in situ monitoring of post-translational modifications catalyzed by the lysine methyltransferase PRDM9 or the lysine demethylase JMJD2E. An arrayed sensor system containing only three cavitand components can detect the specific substrates of enzyme modification, in the presence of other histone peptides in the enzyme assay, enabling investigation of cross-reactivity over multiple methylation sites and interference from nonsubstrate peptides.

Publication types

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

MeSH terms

  • Animals
  • Enzyme Assays / instrumentation
  • Enzyme Assays / methods*
  • Equipment Design
  • Histone-Lysine N-Methyltransferase / metabolism*
  • Histones / chemistry
  • Histones / metabolism*
  • Humans
  • Jumonji Domain-Containing Histone Demethylases / metabolism*
  • Methylation
  • Protein Processing, Post-Translational*

Substances

  • Histones
  • Jumonji Domain-Containing Histone Demethylases
  • Histone-Lysine N-Methyltransferase