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FUT-175作为一种有效的C5/C3转化酶活性抑制剂,用于生成C5a和C3a。

FUT-175 as a potent inhibitor of C5/C3 convertase activity for production of C5a and C3a.

作者信息

Inagi R, Miyata T, Maeda K, Sugiyama S, Miyama A, Nakashima I

机构信息

Department of Immunology, Nagoya University School of Medicine, Japan.

出版信息

Immunol Lett. 1991 Jan;27(1):49-52. doi: 10.1016/0165-2478(91)90243-4.

DOI:10.1016/0165-2478(91)90243-4
PMID:2019419
Abstract

We examined the inhibitory effect of FUT-175 on the C3/C5 convertase activity of the cobra venom factor-derived enzyme CVF,Bb by measuring C5b6-mediated reactive lysis of unsensitized guinea pig erythrocytes and by measuring directly the released fragments C3-des-Arg and C5a-des-Arg. In this study, we showed that the concentration of 4.5 X 10(-6) M of FUT-175 caused 50% inhibition of C5 convertase activity of CVF,Bb in reactive hemolysis assays, and that 4.0 X 10(-6) M FUT-175 caused 50% inhibition of the production of C3a and C5a generated by the C3/C5 convertase activity of CVF,Bb.

摘要

我们通过检测C5b6介导的未致敏豚鼠红细胞反应性溶解以及直接检测释放的片段C3-des-Arg和C5a-des-Arg,研究了FUT-175对眼镜蛇毒因子衍生酶CVF,Bb的C3/C5转化酶活性的抑制作用。在本研究中,我们发现,在反应性溶血试验中,4.5×10(-6) M的FUT-175浓度可导致CVF,Bb的C5转化酶活性受到50%的抑制,并且4.0×10(-6) M的FUT-175可导致CVF,Bb的C3/C5转化酶活性所产生的C3a和C5a生成受到50%的抑制。

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