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2gyd
From Proteopedia
(New page: 200px<br /><applet load="2gyd" size="450" color="white" frame="true" align="right" spinBox="true" caption="2gyd, resolution 1.720Å" /> '''Complex of equine a...) |
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| - | [[Image:2gyd.gif|left|200px]]<br /><applet load="2gyd" size=" | + | [[Image:2gyd.gif|left|200px]]<br /><applet load="2gyd" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="2gyd, resolution 1.720Å" /> | caption="2gyd, resolution 1.720Å" /> | ||
'''Complex of equine apoferritin with the H-diaziflurane photolabeling reagent'''<br /> | '''Complex of equine apoferritin with the H-diaziflurane photolabeling reagent'''<br /> | ||
==Overview== | ==Overview== | ||
| - | The difficulty in obtaining binding target and site information for | + | 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== | ==About this Structure== | ||
| - | 2GYD is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Equus_caballus Equus caballus] with CD and DFE as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http:// | + | 2GYD is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Equus_caballus Equus caballus] with <scene name='pdbligand=CD:'>CD</scene> and <scene name='pdbligand=DFE:'>DFE</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2GYD OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Eckenhoff, R.]] | [[Category: Eckenhoff, R.]] | ||
| - | [[Category: Loll, P | + | [[Category: Loll, P J.]] |
| - | [[Category: Rossi, M | + | [[Category: Rossi, M J.]] |
[[Category: CD]] | [[Category: CD]] | ||
[[Category: DFE]] | [[Category: DFE]] | ||
| Line 22: | Line 22: | ||
[[Category: isoflurane]] | [[Category: isoflurane]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 17:36:25 2008'' |
Revision as of 15:36, 21 February 2008
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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 with and as ligands. 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 Thu Feb 21 17:36:25 2008
Categories: Equus caballus | Single protein | Eckenhoff, R. | Loll, P J. | Rossi, M J. | CD | DFE | Anesthetic | Helical bundles | Isoflurane
