Systematic study of the substituted active C-terminus of hirudin.
Hirudin, a potent clinical thrombin inhibitor from Hirudo medicinalis, consists of 65 amino acids in a single chain. In this paper, we systematically synthesize a series of C-terminal (desulfo hirudin45-65) peptides substituted by 20 natural L-amino acids via the Multipin method. The resulting peptide library is subsequently screened using an alpha-thrombin-mediated fibrinogen clotting assay and alpha-thrombin-induced amidolytic hydrolysis assay.
Liu
G
G
Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing, China. gangliu27@yahoo.com
Mu
S F
SF
Yun
L H
LH
Ding
Z K
ZK
Sun
M J
MJ
D000577:Amides / Q000378:metabolism; D000595:Amino Acid Sequence; D001665:Binding Sites; D001681:Biological Assay; D020134:Catalytic Domain; D020650:Combinatorial Chemistry Techniques; D005342:Fibrinolysis / Q000187:drug effects; D006629:Hirudins / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology; D006868:Hydrolysis; D008969:Molecular Sequence Data; D019151:Peptide Library
D000577:Amides; D006629:Hirudins; D019151:Peptide Library