2gyd: Difference between revisions
New page: left|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]] | ||
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[[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 CD and DFE 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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