title: Inhibition of the protein C activator Protac, a serine proteinase from the venom of the southern copperhead snake Agkistrodon contortrix contortrix.
abstract: ProtacR, the single chain glycoprotein in the venom of Agkistrodon contortrix snake subspecies and related pit vipers has found broad application as a protein C activator in blood coagulation research and diagnosis. Inhibition studies were performed to further elucidate the nature of this serine proteinase. Benzamidine derivatives are poor inhibitors of ProtacR. Only a few 4-amidinoanilides of N alpha-substituted omega-phenyl-alpha-aminoalkylcarboxylic acids exert potent inhibitory activities. The active site of ProtacR appears to be accessible only for inhibitors with well-fitting structural features.
authors.affiliation: Institute of Pharmacology and Toxicology, Medical Academy Erfurt, G.D.R.
authors.forename: J
authors.initials: J
authors.lastname: Stürzebecher
authors.forename: U
authors.initials: U
authors.lastname: Neumann
authors.forename: J
authors.initials: J
authors.lastname: Meier
mesh_terms: D000813:Anilides / Q000494:pharmacology; D000818:Animals; D001550:Benzamidines / Q000494:pharmacology; D003435:Crotalid Venoms / Q000037:antagonists & inhibitors*; D036341:Intercellular Signaling Peptides and Proteins; D015394:Molecular Structure; D010455:Peptides / Q000037:antagonists & inhibitors* / Q000494:pharmacology; D011486:Protein C / Q000187:drug effects / Q000378:metabolism*; D015842:Serine Proteinase Inhibitors / Q000494:pharmacology*; D012911:Snakes; D013917:Thrombin / Q000037:antagonists & inhibitors; D014361:Trypsin Inhibitors / Q000494:pharmacology
chemical_list: D000813:Anilides; D001550:Benzamidines; D003435:Crotalid Venoms; D036341:Intercellular Signaling Peptides and Proteins; D010455:Peptides; D011486:Protein C; D015842:Serine Proteinase Inhibitors; D014361:Trypsin Inhibitors; C049647:snake venom protein C activator; D013917:Thrombin