FXIIIa-blocker Tridegin is a 66 amino acid polypeptide present in the saliva of the giant Amazon leech
Haementeria ghilianii. Tridegin is neither a competitive inhibitor nor an unspecific thiol-group blocking agent. The inhibition mechanism is unknown so far. Finney et al. (Biochem. J.1997, 324:797-805) reported an IC
50 of about 10 nM for factor XIIIa, whereas Sicker (PhD thesis, 2008) measured an IC
50 of 2.5 μM for the recombinant protein.
Using recombinant Tridegin we determined IC
50 -values against FXIIIa of 0.4 μM (
T036) and 1.8 μM (
F001) depending on the assay used (Product No. indicated in brackets). Human TG2 isn’t inhibited by recombinant Tridegin at concentrations up to 10 μM.
Further some microorganism derived unspecific “factor XIIIblockers” with IC
50 -values in the micromolar range have been described, e.g. the antifungal antibiotic Cerulenin (Tymiak et al., J. Antibiot. 1993, 46:204-6).
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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
Reversibly acting transglutaminase 2 inhibitors: drug candidates for the treatment of fibrosis
Press release: Zedira announces ISO 9001:2015 certification
Design of Oral FXIIIa Blockers as Safer Anticoagulants – Mission Impossible?
Microbial transglutaminase (MTG) enables efficient and site-specific conjugation to native antibodies without the need of antibody engineering