Structures of human plasma β-factor XIIa cocrystallized with potent inhibitors.

ABSTRACT: Activated factor XIIa (FXIIa) is a serine protease that has received a great deal of interest in recent years as a potential target for the development of new antithrombotics. Despite the strong interest in obtaining structural information, only the structure of the FXIIa catalytic domain in its zymogen conformation is available. In this work, reproducible experimental conditions found for the crystallization of human plasma β-FXIIa and crystal growth optimization have led to determination of the first structure of the active form of the enzyme. Two crystal structures of human plasma β-FXIIa complexed with small molecule inhibitors are presented herein. The first is the noncovalent inhibitor benzamidine. The second is an aminoisoquinoline containing a boronic acid-reactive group that targe

SUBMITTER: Dementiev A 

PROVIDER: S-EPMC5851424 | biostudies-literature | 2018 Mar

REPOSITORIES: biostudies-literature