3EHX

Crystal structure of the catalytic domain of human MMP12 complexed with the inhibitor (R)-2-(biphenyl-4-ylsulfonamido)-4-methylpentanoic acid

3EHX の概要

• エントリーDOI: 10.2210/pdb3ehx/pdb
• 関連するPDBエントリー: 3EHY
• 分子名称: Macrophage metalloelastase, ZINC ION, CALCIUM ION, ... (5 entities in total)
• 機能のキーワード: matrix metalloproteinase, mmp12, elastase, complex (elastase-inhibitor), metallo elastase, calcium, extracellular matrix, glycoprotein, hydrolase, metal-binding, metalloprotease, polymorphism, protease, secreted, zinc, zymogen
• 由来する生物種: Homo sapiens (human)
• 細胞内の位置: Secreted, extracellular space, extracellular matrix (Probable): P39900
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 18082.96

構造登録者

Calderone, V. (登録日: 2008-09-15, 公開日: 2009-05-19, 最終更新日: 2023-11-01)

主引用文献

Dragoni, E.,Calderone, V.,Fragai, M.,Jaiswal, R.,Luchinat, C.,Nativi, C.
Biotin-tagged probes for MMP expression and activation: design, synthesis, and binding properties
Bioconjug.Chem., 20:719-727, 2009

PubMed Abstract: The design and synthesis of biotin chain-terminated inhibitors (BTI) showing high affinity for matrix metalloproteinases (MMPs) on one side and high affinity for avidin through the biotinylated tag on the other are reported. The affinity of the designed BTI toward five different MMPs has been evaluated and the simultaneous formation of a highly stable ternary system Avidin-BTI-MMP clearly assessed. This system will permit the development of new approaches to detect, quantify, or collect MMPs in biological samples, with potential applications in vivo.

PubMed: 19275207
DOI: 10.1021/bc8003827

実験手法

X-RAY DIFFRACTION (1.9 Å)