„DON“ compounds

These potent molecules are side chain modified peptides. The electrophilic “DON” group replaces the substrate glutamine. The active site cysteinyl residue attacks the carbonyl group (1). The subsequent reaction leads to the release of nitrogen (2) and the concomitant irreversible alkylation at the active site of the transglutaminases (3).

DON comppound reaction mechanism

Zedira developed molecules frequently used in scientific literature.

  • Z-DON (Z006; Z-DON-Val-Pro-Leu-OMe) Z-DON is a very potent and specific blocker of tissue transglutaminase (IC50 about 0.02 μM) and membrane permeable.
  • Boc-DON (B003; Boc-DON-Gln-Ile-Val-OMe) Boc-DON is a potent and specific blocker of tissue transglutaminase (IC50 about 0.3 μM) and is not membrane permeable.
  • K9-DON (K003; Ac-LGPG-DON-SLVIG-NH2) K9-DON was developed to block coagulation factor XIIIa. The sequence is derived from a casein peptide. The IC50 is about 0.8 μM (Sabo et al. Biochemistry 2007, 46:10089-101).
  • TAMRA-DON (R002; N-(Tetramethylrhodaminyl)-DON-Val-Pro-Leu-OMe) TAMRA-DON is a fluorescent blocker of tissue transglutaminase with an IC50 of about 0.1 μM.


Art. No.
Name
Quantity
Price
B003 Boc-DON-Gln-Ile-Val-OMe, Boc-DON
10 mg
385 €
R002 TAMRA-DON
N-(Tetramethylrhodaminyl)-DON-Val-Pro-Leu-OMe
5 mg
10 mg
385 €
575 €
Z006 Z-DON-Val-Pro-Leu-OMe, "Z-DON"
10 mg
385 €
Z011 Z-(D)-DON-Val-Pro-Leu-OMe, Z-(D)-DON
10 mg
415 €

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News  

  • Zedira publication: Microbial Transglutaminase Used in Bread Preparation at Standard Bakery Concentrations Does Not Increase Immunodetectable Amounts of Deamidated Gliadin
  • Pressemitteilung: Dr. Falk Pharma und Zedira geben den Abschluss der Phase 1b-Studie für ZED1227 zur Zöliakie-Therapie bekannt und planen Start der Wirksamkeitsstudie
  • Press release: Dr. Falk Pharma and Zedira announce completion of phase 1b clinical trial of ZED1227 for the treatment of celiac disease and move on to proof of concept study
  • Press Release: Dr. Falk Pharma GmbH and Zedira enter a phase 1b clinical trial for a celiac disease drug
  • Zedira publication: Microbial transglutaminase has a lower deamidation preference than human tissue transglutaminase on a celiac disease relevant wheat gliadin T-cell epitope
  • Press release: Additional subsidy funding for clinical development of a celiac disease drug
  • Pressemitteilung: Zusätzliche Fördermittel für die klinische Entwicklung eines Zöliakie-Medikamentes
  • Press Release: Cooperation between Zedira and Cardiff University - Transglutaminase 6 is the focus of new research into ataxia
  • Press Release: Dr. Falk Pharma and Zedira enter phase I clinical trials for a celiac disease drug
  • Press release: Zedira receives further funding to develop Factor XIIIa-blockers for safe anticoagulation

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Events  

  • MEDICA

    13.11.2017 - 16.11.2017
    Düsseldorf, Germany

  • Gordon Research Conference on: Transglutaminases in Human Disease Processes

    16.06.2018 - 17.06.2018
    Les Diablerets, Switzerland