Design of a selective chemical probe for class I PDZ domains

Bioorg Med Chem Lett. 2007 Jan 15;17(2):546-8. doi: 10.1016/j.bmcl.2006.10.027. Epub 2006 Oct 17.

Abstract

Covalent labeling has been widely used for structural and functional analyses of proteins. To target a wide range of PDZ domains, we designed a chemical scaffold mimicking the E/D-T/S-XV peptide, which is a PDZ domain that binds ligands in higher occurrence. A chemical probe (2) that contained this moiety alkylated diverse PDZ domains, including NHERF-1 PDZ2, and differentially visualized the cellular proteome.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Alkylation
  • Carrier Proteins / drug effects*
  • Drug Design
  • Electrophoresis, Polyacrylamide Gel
  • Indicators and Reagents
  • Ligands
  • Membrane Proteins
  • Molecular Probes / chemical synthesis*
  • Molecular Probes / pharmacology*
  • Peptides / chemical synthesis
  • Peptides / pharmacology
  • Phosphoproteins / chemistry
  • Protein Binding
  • Proteome / drug effects
  • Sodium-Hydrogen Exchangers / chemistry

Substances

  • Carrier Proteins
  • Indicators and Reagents
  • Ligands
  • Membrane Proteins
  • Molecular Probes
  • PDZK1 protein, human
  • Peptides
  • Phosphoproteins
  • Proteome
  • Sodium-Hydrogen Exchangers
  • sodium-hydrogen exchanger regulatory factor