Design of a selective chemical probe for class I PDZ domains

Naoaki Fujii, Anang Shelat, Randy A. Hall, R. Kiplin Guy

Research output: Contribution to journalArticlepeer-review

12 Scopus citations


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.

Original languageEnglish
Pages (from-to)546-548
Number of pages3
JournalBioorganic and Medicinal Chemistry Letters
Issue number2
StatePublished - Jan 15 2007

Bibliographical note

Funding Information:
We thank Kathleen A. P. Novak for providing GST-MAGI3 PDZ2 protein and its H73A mutant; R. Mike Gage for providing HEK293 cells that express NHERF-1-HA; Amanda M. Castleberry for excellent technical assistance; and Angela McArthur for scientific editing of the manuscript. Financial support was provided in part by the American Lebanese Syrian Associated Charities (N.F., A.S., and R.K.G.).


  • Chemical probe
  • PDZ domain
  • Proteomics

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry


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