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纤溶酶原的AH位点及两个C末端片段。一个弱赖氨酸结合位点,偏好不带有游离羧基功能的配体。

The AH-site of plasminogen and two C-terminal fragments. A weak lysine-binding site preferring ligands not carrying a free carboxylate function.

作者信息

Christensen U

出版信息

Biochem J. 1984 Oct 15;223(2):413-21. doi: 10.1042/bj2230413.

Abstract

Glu-plasminogen [native plasminogen (Glu-1-Asn-790)], Lys-plasminogen [plasmin-cleaved fragment of plasminogen (Lys-77-Asn-790)] and miniplasminogen [fragment of plasminogen (Val-440-Asn-790)] were all found to interact specifically with immobilized 6-aminohexyl ligands. The interactions apparently are mediated by a single weak lysine-binding site, termed the AH-site, as seen from the patterns of inhibition obtained from frontal-quantitative-affinity-chromatography experiments with 6-aminohexanoic acid and alpha-N-acetyl-L-lysine methyl ester as competing ligands. The AH-site, in contrast with the strong lysine-binding site of Glu-plasminogen and Lys-plasminogen, may prefer ligands not carrying a free carboxylate function and therefore may interact with lysine side chains of proteins. In Glu-plasminogen the AH-site is present, but is apparently only partially free to react. It is suggested that it participates in an intramolecular complex and that an equilibrium state between two Glu-plasminogen forms exists. It is further suggested that binding of the plasminogens to fibrin is mainly determined by the AH-site.

摘要

已发现谷氨酸纤溶酶原[天然纤溶酶原(Glu-1-Asn-790)]、赖氨酸纤溶酶原[纤溶酶原的纤溶酶裂解片段(Lys-77-Asn-790)]和微型纤溶酶原[纤溶酶原片段(Val-440-Asn-790)]均能与固定化的6-氨基己基配体发生特异性相互作用。从以6-氨基己酸和α-N-乙酰-L-赖氨酸甲酯作为竞争配体的前沿定量亲和色谱实验所获得的抑制模式来看,这些相互作用显然是由一个单一的弱赖氨酸结合位点介导的,该位点称为AH位点。与谷氨酸纤溶酶原和赖氨酸纤溶酶原的强赖氨酸结合位点相比,AH位点可能更倾向于不带有游离羧酸盐功能的配体,因此可能与蛋白质的赖氨酸侧链相互作用。在谷氨酸纤溶酶原中存在AH位点,但显然只有部分能自由反应。有人认为它参与了分子内复合物的形成,并且谷氨酸纤溶酶原的两种形式之间存在平衡状态。进一步表明,纤溶酶原与纤维蛋白的结合主要由AH位点决定。

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Urokinase-catalysed plasminogen activation. Effects of ligands binding to the AH-site of plasminogen.
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Analysis of ligand-binding to the kringle 4 fragment from human plasminogen.
Eur Biophys J. 1987;14(6):359-68. doi: 10.1007/BF00262321.

本文引用的文献

1
INHIBITION OF FIBRINOLYTIC ACTIVITY OF PLASMIN BY VARIOUS SYNTHETIC INHIBITORS.
J Biochem. 1965 Mar;57:450-3. doi: 10.1093/oxfordjournals.jbchem.a128100.

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