Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 66, Issue -, Pages 526-530Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.05.018
Keywords
Imidazolium warheads; Dialkylsulfonium; Peptidic inhibitors; Tissue transglutaminase (TG2); Coagulation factor XIIIa (FXIIIa)
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Funding
- TRANSCOM, FP7 [251506]
- TRACKS [MRTN-CT-2006-03032]
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New peptidic water-soluble inhibitors are reported. In addition to the carboxylate moiety, a new polar warhead was explored. Depending on the size of its substituents, the newly appended imidazolium scaffold designed to enhance the hydrophilic character of the inhibitors could induce a good inhibition for tissue transglutaminase (TG2) and blood coagulation factor XIIIa (EXIIIa). Correlated with the narrow tunnel that hosts the target catalytic cysteine residue, the various modulations suggest a bent conformation of the ligands as the binding pattern mode. Analogues in the dialkylsulfonium series were also tested and showed specificity for TG2 over FXIIIa. (c) 2013 Elsevier Masson SAS. All rights reserved.
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