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Human blood coagulation factor XI (FXI) is a key enzyme in the amplification phase of blood coagulation cascade,and is recognized as an important target for anti-coagulant deve-lopment in recent years.We designed a new mutant form of FXIa catalytic domain rhFXI 370～607 (N73Q-N113Q-C123S),and report here the facile preparation,protein crystallization,and crystal structure of this protein.We highlight a few unique structural features of FXIa after comparison with the trypsin family serine proteases at sequence and structural levels.This work provides a foundation to develop new small molecular FXIa inhibitors with increased potency and specificity.
Human blood coagulation factor XI (FXI) is a key enzyme in the amplification phase of blood coagulation cascade, and is recognized as an important target for anti-coagulant deve-lopment in recent years. We designed a new mutant form of FXIa catalytic domain rhFXI 370 ~ 607 (N73Q-N113Q-C123S), and report here the facile preparation, protein crystallization, and crystal structure of this protein. We highlight a few unique structural features of FXIa after comparison with the trypsin family serine proteases at sequence and structural levels .This work provides a foundation to develop new small molecular FXIa inhibitors with increased potency and specificity.