1ms7

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(New page: 200px<br /><applet load="1ms7" size="450" color="white" frame="true" align="right" spinBox="true" caption="1ms7, resolution 1.97&Aring;" /> '''X-ray structure of t...)
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[[Image:1ms7.gif|left|200px]]<br /><applet load="1ms7" size="450" color="white" frame="true" align="right" spinBox="true"
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[[Image:1ms7.gif|left|200px]]<br /><applet load="1ms7" size="350" color="white" frame="true" align="right" spinBox="true"
caption="1ms7, resolution 1.97&Aring;" />
caption="1ms7, resolution 1.97&Aring;" />
'''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==
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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.
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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==
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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://ispc.weizmann.ac.il/oca-bin/ocashort?id=1MS7 OCA].
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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.]]
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[[Category: Kastrup, J.S.]]
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[[Category: Kastrup, J S.]]
[[Category: Liljefors, T.]]
[[Category: Liljefors, T.]]
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[[Category: Lunn, M.L.]]
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[[Category: Lunn, M L.]]
[[Category: SHI]]
[[Category: SHI]]
[[Category: ZN]]
[[Category: ZN]]
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[[Category: ligand-binding core]]
[[Category: ligand-binding core]]
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''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Nov 20 21:39:49 2007''
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''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


1ms7, resolution 1.97Å

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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

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