A molecular warhead and its target: tissue transglutaminase and Celiac Sprue

Chem Biol. 2003 Mar;10(3):199-201. doi: 10.1016/s1074-5521(03)00055-3.

Abstract

The substitution of a glutamine residue with 6-diazo-5-oxo-norleucine (DON) transforms an immunodominant gluten peptide into a potent inhibitor of tissue transglutaminase. DON-modified peptides could be useful for the study and therapy of celiac sprue.

Publication types

  • Research Support, Non-U.S. Gov't
  • Comment

MeSH terms

  • Celiac Disease / drug therapy*
  • Celiac Disease / enzymology
  • Diazooxonorleucine / analogs & derivatives*
  • Diazooxonorleucine / chemical synthesis*
  • Diazooxonorleucine / pharmacology
  • GTP-Binding Proteins / antagonists & inhibitors*
  • Glutamine / chemistry
  • Glutens / chemistry*
  • Humans
  • Peptides / chemical synthesis*
  • Peptides / chemistry
  • Peptides / pharmacology
  • Protein Glutamine gamma Glutamyltransferase 2
  • Transglutaminases / antagonists & inhibitors*

Substances

  • Peptides
  • Diazooxonorleucine
  • Glutamine
  • Glutens
  • Protein Glutamine gamma Glutamyltransferase 2
  • Transglutaminases
  • GTP-Binding Proteins