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2gyd
From Proteopedia
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[[Image:2gyd.gif|left|200px]] | [[Image:2gyd.gif|left|200px]] | ||
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'''Complex of equine apoferritin with the H-diaziflurane photolabeling reagent''' | '''Complex of equine apoferritin with the H-diaziflurane photolabeling reagent''' | ||
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[[Category: Loll, P J.]] | [[Category: Loll, P J.]] | ||
[[Category: Rossi, M J.]] | [[Category: Rossi, M J.]] | ||
| - | [[Category: | + | [[Category: Anesthetic]] |
| - | [[Category: | + | [[Category: Helical bundle]] |
| - | [[Category: | + | [[Category: Isoflurane]] |
| - | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 05:39:25 2008'' | |
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | |
Revision as of 02:39, 4 May 2008
Complex of equine apoferritin with the H-diaziflurane photolabeling reagent
Overview
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.
About this Structure
2GYD is a Single protein structure of sequence from Equus caballus. Full crystallographic information is available from OCA.
Reference
Photoactive analogues of the haloether anesthetics provide high-resolution features from low-affinity interactions., Xi J, Liu R, Rossi MJ, Yang J, Loll PJ, Dailey WP, Eckenhoff RG, ACS Chem Biol. 2006 Jul 21;1(6):377-84. PMID:17163775 Page seeded by OCA on Sun May 4 05:39:25 2008
