Loading
PDBj
メニューPDBj@FacebookPDBj@X(formerly Twitter)PDBj@BlueSkyPDBj@YouTubewwPDB FoundationwwPDBDonate
RCSB PDBPDBeBMRBAdv. SearchSearch help

1E7C

HUMAN SERUM ALBUMIN COMPLEXED WITH MYRISTIC ACID and the general anesthetic halothane

1E7C の概要
エントリーDOI10.2210/pdb1e7c/pdb
関連するPDBエントリー1AO6 1BJ5 1BKE 1BM0 1E78 1E7A 1E7B 1E7E 1E7F 1E7G 1E7H 1E7I 1UOR
分子名称SERUM ALBUMIN, MYRISTIC ACID, 2-BROMO-2-CHLORO-1,1,1-TRIFLUOROETHANE, ... (4 entities in total)
機能のキーワードplasma protein, metal-binding, lipid-binding, general anesthetic, halothane
由来する生物種HOMO SAPIENS (HUMAN)
細胞内の位置Secreted: P02768
タンパク質・核酸の鎖数1
化学式量合計69094.75
構造登録者
Bhattacharya, A.A.,Curry, S.,Franks, N.P. (登録日: 2000-08-26, 公開日: 2001-01-17, 最終更新日: 2024-10-23)
主引用文献Bhattacharya, A.A.,Curry, S.,Franks, N.P.
Binding of the General Anesthetics Propofol and Halothane to Human Serum Albumin. High Resolution Crystal Structures
J.Biol.Chem., 275:38731-, 2000
Cited by
PubMed Abstract: Human serum albumin (HSA) is one of the most abundant proteins in the circulatory system and plays a key role in the transport of fatty acids, metabolites, and drugs. For many drugs, binding to serum albumin is a critical determinant of their distribution and pharmacokinetics; however, there have as yet been no high resolution crystal structures published of drug-albumin complexes. Here we describe high resolution crystal structures of HSA with two of the most widely used general anesthetics, propofol and halothane. In addition, we describe a crystal structure of HSA complexed with both halothane and the fatty acid, myristate. We show that the intravenous anesthetic propofol binds at two discrete sites on HSA in preformed pockets that have been shown to accommodate fatty acids. Similarly we show that the inhalational agent halothane binds (at concentrations in the pharmacologically relevant range) at three sites that are also fatty acid binding loci. At much higher halothane concentrations, we have identified additional sites that are occupied. All of the higher affinity anesthetic binding sites are amphiphilic in nature, with both polar and apolar parts, and anesthetic binding causes only minor changes in local structure.
PubMed: 10940303
DOI: 10.1074/JBC.M005460200
主引用文献が同じPDBエントリー
実験手法
X-RAY DIFFRACTION (2.4 Å)
構造検証レポート
Validation report summary of 1e7c
検証レポート(詳細版)ダウンロードをダウンロード

237735

件を2025-06-18に公開中

PDB statisticsPDBj update infoContact PDBjnumon