[Inhibitors] Michael acceptorpeptidomimetics_ZEDIRA - 코아사이언스

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Michael acceptorpeptidomimetics

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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.

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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).

 

Cat. No.	Name	Unit
A108	Ac-(D)-Asp-MA-Nle-Nle-Leu-Pro-Trp-Pro-OH, "ZED1301"	5 mg
B015	Biotin-Ahx-MA-QPL-OMe	10 mg
Z013	Z-MA-QPL-OMe	10 mg

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