1A7C

HUMAN PLASMINOGEN ACTIVATOR INHIBITOR TYPE-1 IN COMPLEX WITH A PENTAPEPTIDE

1A7C の概要

• エントリーDOI: 10.2210/pdb1a7c/pdb
• 分子名称: PLASMINOGEN ACTIVATOR INHIBITOR TYPE 1, PENTAPEPTIDE, 2-acetamido-2-deoxy-beta-D-glucopyranose-(1-4)-[beta-D-ribopyranose-(1-6)]2-acetamido-2-deoxy-beta-D-glucopyranose, ... (5 entities in total)
• 機能のキーワード: serine protease inhibitor, pai-1, carbohydrate, inhibitor complex, protease inhibitor-peptide complex, hydrolase inhibitor-peptide complex, hydrolase inhibitor/peptide
• 由来する生物種: Homo sapiens (human)
• タンパク質・核酸の鎖数: 3
• 化学式量合計: 44629.88

構造登録者

Xue, Y.,Inghardt, T.,Sjolin, L.,Deinum, J. (登録日: 1998-03-12, 公開日: 1999-03-23, 最終更新日: 2024-10-30)

主引用文献

Xue, Y.,Bjorquist, P.,Inghardt, T.,Linschoten, M.,Musil, D.,Sjolin, L.,Deinum, J.
Interfering with the inhibitory mechanism of serpins: crystal structure of a complex formed between cleaved plasminogen activator inhibitor type 1 and a reactive-centre loop peptide
Structure, 6:627-636, 1998

PubMed Abstract: Plasminogen activator inhibitor type 1 (PAI-1) is an important endogenous regulator of the fibrinolytic system. Reduction of PAI-1 activity has been shown to enhance dissolution of blood clots. Like other serpins, PAI-1 binds covalently to a target serine protease, thereby irreversibly inactivating the enzyme. During this process the exposed reactive-centre loop of PAI-1 is believed to undergo a conformational change becoming inserted into beta sheet A of the serpin. Incubation with peptides from the reactive-centre loop transform serpins into a substrate for their target protease. It has been hypothesised that these peptides bind to beta sheet A, thereby hindering the conformational rearrangement leading to loop insertion and formation of the stable serpin-protease complex.

PubMed: 9634700
DOI: 10.1016/S0969-2126(98)00064-1

実験手法

X-RAY DIFFRACTION (1.95 Å)