2024
DOI: 10.1021/acsomega.4c04518
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Discovery of Heparin Mimetic, Potent, and Selective Inhibitors of Human Clotting Factor XIIIa

Kayla T. Vu,
Srabani Kar,
Navneet Goyal
et al.

Abstract: Factor XIIIa (FXIIIa) is a cysteine transglutaminase that catalyzes the last step in the coagulation process. An anionbinding site inhibition of FXIIIa is a paradigm-shifting strategy that may offer key advantages of controlled inhibition. Such an approach is likely to lead to novel FXIIIa inhibitors that do not carry bleeding risks. We previously reported a flavonoid trimer-based allosteric inhibitor of FXIIIa with moderate potency and selectivity. To further advance this approach, we evaluated a series of 27… Show more

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