2gyd

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(New page: 200px<br /><applet load="2gyd" size="450" color="white" frame="true" align="right" spinBox="true" caption="2gyd, resolution 1.720&Aring;" /> '''Complex of equine a...)
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[[Image:2gyd.gif|left|200px]]<br /><applet load="2gyd" size="450" color="white" frame="true" align="right" spinBox="true"
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[[Image:2gyd.gif|left|200px]]<br /><applet load="2gyd" size="350" color="white" frame="true" align="right" spinBox="true"
caption="2gyd, resolution 1.720&Aring;" />
caption="2gyd, resolution 1.720&Aring;" />
'''Complex of equine apoferritin with the H-diaziflurane photolabeling reagent'''<br />
'''Complex of equine apoferritin with the H-diaziflurane photolabeling reagent'''<br />
==Overview==
==Overview==
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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.
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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==
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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://ispc.weizmann.ac.il/oca-bin/ocashort?id=2GYD OCA].
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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.]]
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[[Category: Loll, P.J.]]
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[[Category: Loll, P J.]]
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[[Category: Rossi, M.J.]]
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[[Category: Rossi, M J.]]
[[Category: CD]]
[[Category: CD]]
[[Category: DFE]]
[[Category: DFE]]
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[[Category: isoflurane]]
[[Category: isoflurane]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Wed Nov 21 11:27:36 2007''
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''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

Image:2gyd.gif

2gyd, resolution 1.720Å

Drag the structure with the mouse to rotate

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

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