Synthesis of potent water-soluble tissue transglutaminase inhibitors

Martin Griffin, Alexandre Mongeot, Russell Collighan, Robert E. Saint, Richard A. Jones, Ian G.C. Coutts, Daniel L. Rathbone

Research output: Contribution to journalArticlepeer-review


Dipeptide-based sulfonium peptidylmethylketones derived from 6-diazo-5-oxo-L-norleucine (DON) have been investigated as potential water-soluble inhibitors of extracellular transglutaminase. The lead compounds were prepared in four steps and exhibited potent activity against tissue transglutaminase.
Original languageEnglish
Pages (from-to)5559-5562
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Issue number20
Publication statusPublished - 15 Oct 2008


  • transglutaminase
  • inhibitors
  • dipeptide


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