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1ms7
From Proteopedia
(New page: 200px<br /><applet load="1ms7" size="450" color="white" frame="true" align="right" spinBox="true" caption="1ms7, resolution 1.97Å" /> '''X-ray structure of t...) |
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| - | [[Image:1ms7.gif|left|200px]]<br /><applet load="1ms7" size=" | + | [[Image:1ms7.gif|left|200px]]<br /><applet load="1ms7" size="350" color="white" frame="true" align="right" spinBox="true" |
caption="1ms7, resolution 1.97Å" /> | caption="1ms7, resolution 1.97Å" /> | ||
'''X-ray structure of the GluR2 ligand-binding core (S1S2J) in complex with (S)-Des-Me-AMPA at 1.97 A resolution, Crystallization in the presence of zinc acetate'''<br /> | '''X-ray structure of the GluR2 ligand-binding core (S1S2J) in complex with (S)-Des-Me-AMPA at 1.97 A resolution, Crystallization in the presence of zinc acetate'''<br /> | ||
==Overview== | ==Overview== | ||
| - | X-ray structures of the GluR2 ligand-binding core in complex with | + | X-ray structures of the GluR2 ligand-binding core in complex with (S)-Des-Me-AMPA and in the presence and absence of zinc ions have been determined. (S)-Des-Me-AMPA, which is devoid of a substituent in the 5-position of the isoxazolol ring, only has limited interactions with the partly hydrophobic pocket of the ligand-binding site, and adopts an AMPA-like binding mode. The structures, in comparison with other agonist complex structures, disclose the relative importance of the isoxazolol ring and of the substituent in the 5-position for the mode of binding. A relationship appears to exist between the extent of interaction of the ligand with the hydrophobic pocket and the affinity of the ligand. |
==About this Structure== | ==About this Structure== | ||
| - | 1MS7 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus] with ZN and SHI as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http:// | + | 1MS7 is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Rattus_norvegicus Rattus norvegicus] with <scene name='pdbligand=ZN:'>ZN</scene> and <scene name='pdbligand=SHI:'>SHI</scene> as [http://en.wikipedia.org/wiki/ligands ligands]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1MS7 OCA]. |
==Reference== | ==Reference== | ||
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[[Category: Gouaux, E.]] | [[Category: Gouaux, E.]] | ||
[[Category: Kasper, C.]] | [[Category: Kasper, C.]] | ||
| - | [[Category: Kastrup, J | + | [[Category: Kastrup, J S.]] |
[[Category: Liljefors, T.]] | [[Category: Liljefors, T.]] | ||
| - | [[Category: Lunn, M | + | [[Category: Lunn, M L.]] |
[[Category: SHI]] | [[Category: SHI]] | ||
[[Category: ZN]] | [[Category: ZN]] | ||
| Line 25: | Line 25: | ||
[[Category: ligand-binding core]] | [[Category: ligand-binding core]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 13:58:30 2008'' |
Revision as of 11:58, 21 February 2008
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X-ray structure of the GluR2 ligand-binding core (S1S2J) in complex with (S)-Des-Me-AMPA at 1.97 A resolution, Crystallization in the presence of zinc acetate
Overview
X-ray structures of the GluR2 ligand-binding core in complex with (S)-Des-Me-AMPA and in the presence and absence of zinc ions have been determined. (S)-Des-Me-AMPA, which is devoid of a substituent in the 5-position of the isoxazolol ring, only has limited interactions with the partly hydrophobic pocket of the ligand-binding site, and adopts an AMPA-like binding mode. The structures, in comparison with other agonist complex structures, disclose the relative importance of the isoxazolol ring and of the substituent in the 5-position for the mode of binding. A relationship appears to exist between the extent of interaction of the ligand with the hydrophobic pocket and the affinity of the ligand.
About this Structure
1MS7 is a Single protein structure of sequence from Rattus norvegicus with and as ligands. Full crystallographic information is available from OCA.
Reference
GluR2 ligand-binding core complexes: importance of the isoxazolol moiety and 5-substituent for the binding mode of AMPA-type agonists., Kasper C, Lunn ML, Liljefors T, Gouaux E, Egebjerg J, Kastrup JS, FEBS Lett. 2002 Nov 6;531(2):173-8. PMID:12417307
Page seeded by OCA on Thu Feb 21 13:58:30 2008
