1BUI

Structure of the ternary microplasmin-staphylokinase-microplasmin complex: a proteinase-cofactor-substrate complex in action

1BUI の概要

• エントリーDOI: 10.2210/pdb1bui/pdb
• 関連するBIRD辞書のPRD_ID: PRD_000288
• 分子名称: Plasminogen, Staphylokinase, L-alpha-glutamyl-N-{(1S)-4-{[amino(iminio)methyl]amino}-1-[(1S)-2-chloro-1-hydroxyethyl]butyl}glycinamide, ... (4 entities in total)
• 機能のキーワード: plasmin, staphylokinase, serine proteinase, fibrinolysis, cofactor, hydrolase-hydrolase inhibitor complex, hydrolase/hydrolase inhibitor
• 由来する生物種: Homo sapiens (human); 詳細
• 細胞内の位置: Secreted : P00747 P15240
• タンパク質・核酸の鎖数: 3
• 化学式量合計: 69665.31

構造登録者

Parry, M.A.A.,Fernandez-Catalan, C.,Bergner, A.,Huber, R.,Hopfner, K.,Schlott, B.,Guehrs, K.,Bode, W. (登録日: 1998-09-04, 公開日: 1999-09-02, 最終更新日: 2024-10-30)

主引用文献

Parry, M.A.,Fernandez-Catalan, C.,Bergner, A.,Huber, R.,Hopfner, K.P.,Schlott, B.,Guhrs, K.H.,Bode, W.
The ternary microplasmin-staphylokinase-microplasmin complex is a proteinase-cofactor-substrate complex in action.
Nat.Struct.Biol., 5:917-923, 1998

PubMed Abstract: The serine proteinase plasmin is the key fibrinolytic enzyme that dissolves blood clots and also promotes cell migration and tissue remodeling. Here, we report the 2.65 A crystal structure of a ternary complex of microplasmin-staphylokinase bound to a second microplasmin. The staphylokinase 'cofactor' does not affect the active-site geometry of the plasmin 'enzyme', but instead modifies its subsite specificity by providing additional docking sites for enhanced presentation of the plasminogen 'substrate' to the 'enzymes's' active site. The activation loop of the plasmin 'substrate', cleaved in these crystals, can be reconstructed to show how it runs across the active site of the plasmin 'enzyme' prior to activation cleavage. This is the first experimental structure of a productive proteinase-cofactor-macromolecular substrate complex. Furthermore, it provides a template for the design of improved plasminogen activators and plasmin inhibitors with considerable therapeutical potential.

PubMed: 9783753
DOI: 10.1038/2359

実験手法

X-RAY DIFFRACTION (2.65 Å)