Systematic study of the substituted active C-terminus of hirudin

Hirudin, a potent clinical thrombin inhibitor from Hirudo medicinalis, cons ists of 65 amino acids in a single chain. In this paper, we systematically synthesize a series of C-terminal (desulfo hirudin(45-65)) peptides substit uted by 20 natural L-amino acids via the Multipin method. The resulting pep tide library is subsequently screened using an alpha-thrombin-mediated fibr inogen clotting assay and alpha-thrombin-induced amidolytic hydrolysis assa y.