Stürzebecher J, Neumann U, Meier J
Institute of Pharmacology and Toxicology, Medical Academy Erfurt, G.D.R.
Toxicon. 1991;29(2):151-5. doi: 10.1016/0041-0101(91)90099-d.
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.
ProtacR是蝮蛇属蛇亚种和相关蝰蛇毒液中的单链糖蛋白，已作为凝血研究和诊断中的蛋白C激活剂得到广泛应用。进行了抑制研究以进一步阐明这种丝氨酸蛋白酶的性质。苯甲脒衍生物是ProtacR的弱抑制剂。只有少数Nα-取代的ω-苯基-α-氨基烷基羧酸的4-脒基苯胺具有强大的抑制活性。ProtacR的活性位点似乎仅对具有结构特征匹配良好的抑制剂开放。
