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1
Peptide inhibitors of C3 breakdown.C3分解的肽类抑制剂。
Clin Exp Immunol. 1990 Mar;79(3):454-8. doi: 10.1111/j.1365-2249.1990.tb08111.x.
2
Inhibition of the alternative C3 convertase and classical C5 convertase of complement by group A streptococcal M protein.A组链球菌M蛋白对补体替代途径C3转化酶和经典途径C5转化酶的抑制作用。
Infect Immun. 1990 Aug;58(8):2535-41. doi: 10.1128/iai.58.8.2535-2541.1990.
3
Regulation of C5 convertase activity by properdin, factors B and H.备解素、B因子和H因子对C5转化酶活性的调节
Immunol Res. 1989;8(4):305-15. doi: 10.1007/BF02935515.
4
A circulating inhibitor of fluid-phase amplification. C3 convertase formation in systemic lupus erythematosus.液相放大的循环抑制剂。系统性红斑狼疮中C3转化酶的形成。
J Clin Invest. 1985 Jun;75(6):1786-95. doi: 10.1172/JCI111891.
5
Purification and functional analysis of the polymorphic variants of the C3b/C4b receptor (CR1) and comparison with H, C4b-binding protein (C4bp), and decay accelerating factor (DAF).C3b/C4b受体（CR1）多态性变体的纯化与功能分析及其与H、C4b结合蛋白（C4bp）和衰变加速因子（DAF）的比较。
J Immunol. 1985 Oct;135(4):2661-7.
6
Regulation of the amplification C3 convertase of human complement by an inhibitory protein isolated from human erythrocyte membrane.从人红细胞膜分离出的一种抑制性蛋白对人补体C3转化酶扩增的调节作用。
Proc Natl Acad Sci U S A. 1979 Nov;76(11):5867-71. doi: 10.1073/pnas.76.11.5867.
7
Inhibition of classical C5 convertase in the complement system by factor H.补体系统中H因子对经典C5转化酶的抑制作用。
Immunology. 1983 Dec;50(4):631-5.
8
Inhibition of complement activation on the surface of cells after incorporation of decay-accelerating factor (DAF) into their membranes.衰变加速因子（DAF）整合到细胞膜后对细胞表面补体激活的抑制作用。
J Exp Med. 1984 Nov 1;160(5):1558-78. doi: 10.1084/jem.160.5.1558.
9
Inhibition of human complement by a C3-binding peptide isolated from a phage-displayed random peptide library.从噬菌体展示随机肽库中分离出的一种C3结合肽对人补体的抑制作用。
J Immunol. 1996 Jul 15;157(2):884-91.
10
Formation of the initial C3 convertase of the alternative complement pathway. Acquisition of C3b-like activities by spontaneous hydrolysis of the putative thioester in native C3.替代补体途径初始C3转化酶的形成。通过天然C3中假定硫酯的自发水解获得C3b样活性。
J Exp Med. 1981 Sep 1;154(3):856-67. doi: 10.1084/jem.154.3.856.

本文引用的文献

1
Potent new inhibitors of human renin.新型强效人肾素抑制剂
Nature. 1982 Oct 7;299(5883):555-7. doi: 10.1038/299555a0.
2
Cleavage of structural proteins during the assembly of the head of bacteriophage T4.在噬菌体T4头部组装过程中结构蛋白的切割
Nature. 1970 Aug 15;227(5259):680-5. doi: 10.1038/227680a0.
3
The labelling of proteins to high specific radioactivities by conjugation to a 125I-containing acylating agent.通过与含¹²⁵I的酰化剂结合将蛋白质标记至高比放射性。
Biochem J. 1973 Jul;133(3):529-39. doi: 10.1042/bj1330529.
4
Synthetic peptide inhibitors of complement serine proteases--II. Effects on hemolytic activity and production of C3a and C4a.
Mol Immunol. 1988 Dec;25(12):1269-75. doi: 10.1016/0161-5890(88)90041-7.
5
Protein and cell membrane iodinations with a sparingly soluble chloroamide, 1,3,4,6-tetrachloro-3a,6a-diphrenylglycoluril.使用微溶性氯酰胺1,3,4,6-四氯-3a,6a-二苯基甘脲进行蛋白质和细胞膜碘化
Biochem Biophys Res Commun. 1978 Feb 28;80(4):849-57. doi: 10.1016/0006-291x(78)91322-0.
6
Surface-associated heparin inhibits zymosan-induced activation of the human alternative complement pathway by augmenting the regulatory action of the control proteins on particle-bound C3b.表面相关肝素通过增强控制蛋白对颗粒结合C3b的调节作用，抑制酵母聚糖诱导的人替代补体途径的激活。
J Exp Med. 1979 Nov 1;150(5):1202-15. doi: 10.1084/jem.150.5.1202.

C3分解的肽类抑制剂。

Peptide inhibitors of C3 breakdown.

作者信息

Peake P, Szelke M, Jones D M, Singleton A, Sueiras-Diaz J, Lachmann P J

机构信息

Prince Henry Hospital, Little Bay, NSW, Australia.

出版信息

Clin Exp Immunol. 1990 Mar;79(3):454-8. doi: 10.1111/j.1365-2249.1990.tb08111.x.

DOI:10.1111/j.1365-2249.1990.tb08111.x
PMID:2138528
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1534956/
Abstract

We have investigated the development of substrate-based inhibitors of complement enzymes. Sequences around the scissile Arg77-Ser78 bond of C3 have been synthesized and tested as inhibitors of C3 convertase. The best inhibition was found with the tetrapeptide Ac-Arg-Ser-Asn-Leu-OH (H-576); extending this sequence in either direction reduced inhibitory activity. Preliminary experiments with peptides in which the scissile bond--CO--NH--was replaced with non-hydrolysable moieties such as--CO--CH2--(H-497) and--CH2--NH--(H-336) failed to show enhanced inhibition. One of the longer chain inhibitors H-416 containing DArg77-Ser78 was unexpectedly found to potentiate iC3 cleavage by factors I and H but did not inhibit the intact alternative pathway. The same peptide also bound to factor H. It is concluded that the binding requirements of the C3 convertase are more sophisticated than can be satisfactorily imitated simply by linear sequences around the scissile bond of C3.

摘要

我们研究了基于底物的补体酶抑制剂的开发。已合成了C3中可裂解的Arg77-Ser78键周围的序列，并将其作为C3转化酶的抑制剂进行了测试。发现四肽Ac-Arg-Ser-Asn-Leu-OH（H-576）具有最佳抑制作用；向任一方向延长该序列都会降低抑制活性。用其中可裂解键（-CO-NH-）被不可水解部分如-CO-CH2-（H-497）和-CH2-NH-（H-336）取代的肽进行的初步实验未能显示出增强的抑制作用。意外地发现，一种含有DArg77-Ser78的较长链抑制剂H-416可增强因子I和H对iC3的裂解作用，但不抑制完整的替代途径。同一肽也与因子H结合。得出的结论是，C3转化酶的结合要求比仅通过C3可裂解键周围的线性序列就能令人满意地模拟的情况更为复杂。