The L3MBTL3 Methyl-Lysine Reader Domain Functions As a Dimer

ACS Chem Biol. 2016 Mar 18;11(3):722-8. doi: 10.1021/acschembio.5b00632. Epub 2015 Sep 2.

Abstract

L3MBTL3 recognizes mono- and dimethylated lysine residues on histone tails. The recently reported X-ray cocrystal structures of the chemical probe UNC1215 and inhibitor UNC2533 bound to the methyl-lysine reading MBT domains of L3MBTL3 demonstrate a unique and flexible 2:2 dimer mode of recognition. In this study, we describe our in vitro analysis of L3MBTL3 dimerization via its MBT domains and additionally show that this dimerization occurs within a cellular context in the absence of small molecule ligands. Furthermore, mutations to the first and second MBT domains abrogated L3MBTL3 dimerization both in vitro and in cells. These observations are consistent with the hypothesis that L3MBTL3 engages methylated histone tails as a dimer while carrying out its normal function and provides an explanation for the presence of repeated MBT domains within L3MBTL3.

Publication types

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

MeSH terms

  • Benzamides
  • Biotin
  • Cell-Free System
  • DNA-Binding Proteins / genetics
  • DNA-Binding Proteins / metabolism*
  • HeLa Cells
  • Histones
  • Humans
  • Ligands
  • Molecular Structure
  • Mutation
  • Piperidines
  • Protein Domains
  • Protein Multimerization

Substances

  • Benzamides
  • DNA-Binding Proteins
  • Histones
  • L3MBTL3 protein, human
  • Ligands
  • Piperidines
  • UNC1215
  • Biotin