4DO3

Structure of FAAH with a non-steroidal anti-inflammatory drug

4DO3 の概要

• エントリーDOI: 10.2210/pdb4do3/pdb
• 関連するPDBエントリー: 1M5T 2VYA 3LJ7
• 分子名称: Fatty-acid amide hydrolase 1, CHLORIDE ION, CYCLOHEXANE AMINOCARBOXYLIC ACID, ... (5 entities in total)
• 機能のキーワード: amidase, hydrolase, anandamide, nsaid, drug, cox, inhibitor, inflammation, pain, hydrolase-hydrolase inhibitor complex, hydrolase/hydrolase inhibitor
• 由来する生物種: Rattus norvegicus (rat)
• 細胞内の位置: Endoplasmic reticulum membrane; Single-pass membrane protein: P97612
• タンパク質・核酸の鎖数: 2
• 化学式量合計: 126614.04

構造登録者

Garau, G. (登録日: 2012-02-09, 公開日: 2013-01-23, 最終更新日: 2024-11-06)

主引用文献

Bertolacci, L.,Romeo, E.,Veronesi, M.,Magotti, P.,Albani, C.,Dionisi, M.,Lambruschini, C.,Scarpelli, R.,Cavalli, A.,De Vivo, M.,Piomelli, D.,Garau, G.
A Binding Site for Nonsteroidal Anti-inflammatory Drugs in Fatty Acid Amide Hydrolase.
J.Am.Chem.Soc., 135:22-25, 2013

PubMed Abstract: In addition to inhibiting the cyclooxygenase (COX)-mediated biosynthesis of prostanoids, various widely used nonsteroidal anti-inflammatory drugs (NSAIDs) enhance endocannabinoid signaling by blocking the anandamide-degrading membrane enzyme fatty acid amide hydrolase (FAAH). The X-ray structure of FAAH in complex with the NSAID carprofen, along with site-directed mutagenesis, enzyme activity assays, and NMR analysis, has revealed the molecular details of this interaction, providing information that may guide the design of dual FAAH-COX inhibitors with superior analgesic efficacy.

PubMed: 23240907
DOI: 10.1021/ja308733u

実験手法

X-RAY DIFFRACTION (2.25 Å)