A molecular warhead and its target: tissue transglutaminase and Celiac Sprue.
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.
Schuppan
Detlef
D
First Department of Medicine, University of Erlangen-Nuernberg, Ulmenweg 18, 91054 Erlangen, Germany.
Dieterich
Walburga
W
D002446:Celiac Disease / Q000188:drug therapy* / Q000201:enzymology; D003980:Diazooxonorleucine / Q000031:analogs & derivatives* / Q000138:chemical synthesis* / Q000494:pharmacology; D019204:GTP-Binding Proteins / Q000037:antagonists & inhibitors*; D005973:Glutamine / Q000737:chemistry; D005983:Glutens / Q000737:chemistry*; D006801:Humans; D010455:Peptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D000091345:Protein Glutamine gamma Glutamyltransferase 2; D011503:Transglutaminases / Q000037:antagonists & inhibitors*
D010455:Peptides; D003980:Diazooxonorleucine; D005973:Glutamine; D005983:Glutens; D000091345:Protein Glutamine gamma Glutamyltransferase 2; D011503:Transglutaminases; D019204:GTP-Binding Proteins