Naturally occuring inhibitors

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 IC50 of about 10 nM for factor XIIIa, whereas Sicker (PhD thesis, 2008) measured an IC50 of 2.5 μM for the recombinant protein.

Using recombinant Tridegin we determined IC50 -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 IC50 -values in the micromolar range have been described, e.g. the antifungal antibiotic Cerulenin (Tymiak et al., J. Antibiot. 1993, 46:204-6).

Art. No.
Name
Quantity
Price
T087 Tridegin
(rec. produced in E. coli, gene derived from Haementeria ghilianii)
200 µg
480 €

Products

  • Zedira offers a huge portfolio of reliable specialist transglutaminase related products meant to catalyze research and development, both in academia and industry.

News  

  • DZG Aktuell: „Aufruf zur Teilnahme an einer weiteren Wirksamkeitsstudie mit dem Studienmedikament ZED1227“
  • imageDr. Falk Pharma and Zedira announce successful completion of the phase 2a proof-of-concept study of ZED1227 for the treatment of Celiac Disease
  • imageDr. Falk Pharma und Zedira verkünden den erfolgreichen Abschluss der Phase 2a-Studie mit ZED1227 zur Behandlung von Zöliakie
  • imageReversibly acting transglutaminase 2 inhibitors: drug candidates for the treatment of fibrosis
  • imagePress release: Zedira announces ISO 9001:2015 certification

Blog  

  • imageDesign of Oral FXIIIa Blockers as Safer Anticoagulants – Mission Impossible?
  • imageMicrobial transglutaminase (MTG) enables efficient and site-specific conjugation to native antibodies without the need of antibody engineering

Events  

  • Gordon Research Conference: Transglutaminases in Human Disease Processes

    12.06.2022 - 17.06.2022
    Mount Snow, USA

  • 19th International Celiac Disease Symposium

    19.10.2022 - 22.10.2022
    Sorrento, Italy