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Product criteria
Product criteria
| Substance |
|---|
| Michael acceptor 3 |
Michael acceptor
peptidomimetics
Zedira designed peptidomimetic blockers bearing a Michael acceptor warhead.
The electrophilic α,β-unsaturated carbonyl compounds are attacked by the active site cysteine residue (1) to form an irreversible complex (2,3).
The peptidic lead compound Z013 (ZED754) was co-crystallized with tissue transglutaminase. The picture shows the binding mode to the active site. The scaffold was subsequently optimized using medicinal chemistry.
Our clinical candidate ZED1227 is the first TG inhibitor in the clinics.
Compound ZED1301 (A108) is a potent factor XIII inhibitor.
Structure of inhibited tissue transglutaminase.
The inhibitor (shown in cyan) is covalently bound by a Michael addition reaction to the active site Cys 277 (yellow surface), which is located in the catalytic tunnel. It mimics the peptide substrate. The main part of the inhibitor fits onto the protein surface, forming several hydrogen bonds and stabilizing the open conformation
(Lindemann et al., poster presentation at XX Int. Med. Chem. Symp. 2008).
The electrophilic α,β-unsaturated carbonyl compounds are attacked by the active site cysteine residue (1) to form an irreversible complex (2,3).
The peptidic lead compound Z013 (ZED754) was co-crystallized with tissue transglutaminase. The picture shows the binding mode to the active site. The scaffold was subsequently optimized using medicinal chemistry.
Our clinical candidate ZED1227 is the first TG inhibitor in the clinics.
Compound ZED1301 (A108) is a potent factor XIII inhibitor.
Structure of inhibited tissue transglutaminase.
The inhibitor (shown in cyan) is covalently bound by a Michael addition reaction to the active site Cys 277 (yellow surface), which is located in the catalytic tunnel. It mimics the peptide substrate. The main part of the inhibitor fits onto the protein surface, forming several hydrogen bonds and stabilizing the open conformation
(Lindemann et al., poster presentation at XX Int. Med. Chem. Symp. 2008).
| Art. No. | Name | Unit | Price |
|---|---|---|---|
| A108 | Ac-(D)-Asp-MA-Nle-Nle-Leu-Pro-Trp-Pro-OH, "ZED1301" | 5 mg | 550 € |
| B015 | Biotin-Ahx-MA-QPL-OMe | 10 mg | 495 € |
| Z013 | Z-MA-QPL-OMe | 10 mg | 495 € |
Besuch des Bundesministers für Wirtschaft und Klimaschutz Dr. Robert Habeck bei der Zedira 
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Dr. Falk Pharma and Zedira announce successful completion of the phase 2a proof-of-concept study of ZED1227 for the treatment of Celiac Disease 
Dr. Falk Pharma und Zedira verkünden den erfolgreichen Abschluss der Phase 2a-Studie mit ZED1227 zur Behandlung von Zöliakie 
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