New synthetic inhibitor to the alternative complement pathway.
New synthetic inhibitor to the alternative complement pathway.
复制标题
替代补体途径的新合成抑制剂。
作者：
N. Ikari;Y. Sakai;Y. Hitomi;S. Fujii
本文研究了6-脒基-2-萘基-4-胍基苯甲酸酯（FUT-175）对因子B、因子D和眼镜蛇毒因子（CVF）X B B b活性的抑制作用。FUT-175特异性结合因子B的B B片段或CVF X B B。FUT-175是一种非竞争性抑制因子B和CVF X B B对L-亮氨酰-L-丙氨酰-L-精氨酸萘酯的酯水解作用的抑制剂。FUT-175还抑制因子B的溶血活性、CVF X B B b的C3转化酶活性和因子D的因子B裂解活性。引起这些活性50%抑制的FUT-175浓度为10（-5）-10（-4）M。
The inhibitory effects of 6-amidino-2-naphthyl 4-guanidinobenzoate (FUT-175) on the activities of factor B, factor D and cobra venom factor (CVF) X Bb were examined. FUT-175 bound specifically to the Bb fragment of factor B or CVF X Bb. FUT-175 was a non-competitive inhibitor of the esterolysis of L-leucyl-L-alanyl-L-arginine naphthylester by factor B and CVF X Bb. FUT-175 also inhibited the haemolytic activity of factor B, the C3 convertase activity of CVF X Bb and the factor B-cleaving activity of factor D. The concentration of FUT-175 causing 50% inhibition of these activities was 10(-5) - 10(-4)M.