2GYD

Complex of equine apoferritin with the H-diaziflurane photolabeling reagent

2GYD の概要

• エントリーDOI: 10.2210/pdb2gyd/pdb
• 分子名称: ferritin L subunit, CADMIUM ION, 2-(1,1-DIFLUOROETHOXY)-1,1,1-TRIFLUOROETHANE, ... (4 entities in total)
• 機能のキーワード: helical bundles, anesthetic, isoflurane, metal binding protein
• 由来する生物種: Equus caballus (horse)
• タンパク質・核酸の鎖数: 1
• 化学式量合計: 20353.89

構造登録者

Loll, P.J.,Rossi, M.J.,Eckenhoff, R. (登録日: 2006-05-09, 公開日: 2006-06-13, 最終更新日: 2024-11-13)

主引用文献

Xi, J.,Liu, R.,Rossi, M.J.,Yang, J.,Loll, P.J.,Dailey, W.P.,Eckenhoff, R.G.
Photoactive analogues of the haloether anesthetics provide high-resolution features from low-affinity interactions.
Acs Chem.Biol., 1:377-384, 2006

PubMed Abstract: The difficulty in obtaining binding target and site information for low-affinity drugs, like the inhaled anesthetics, has limited identification of their molecular effectors. Because such information can be provided by photoactive analogues, we designed, synthesized, and characterized a novel diazirnyl haloether that closely mimics isoflurane, the most widely used clinical general anesthetic. This compound, H-diaziflurane, is a nontoxic, potent anesthetic that potentiates GABA-gated ion channels in primary cultures of hippocampal neurons. Calorimetric and structural characterizations show that H-diaziflurane binds a model anesthetic host protein with similar energetics as isoflurane and forms photoadducts with residues lining the isoflurane binding site. H-diaziflurane will be immediately useful for identifying targets and sites important for the molecular pharmacology of the inhaled haloether anesthetics.

PubMed: 17163775
DOI: 10.1021/cb600207d

実験手法

X-RAY DIFFRACTION (1.72 Å)