1pb7: Difference between revisions

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[[Image:1pb7.jpg|left|200px]]<br /><applet load="1pb7" size="~~450~~" color="white" frame="true" align="right" spinBox="true"

[[Image:1pb7.jpg|left|200px]]<br /><applet load="1pb7" size="350" color="white" frame="true" align="right" spinBox="true"

caption="1pb7, resolution 1.35Å" />

'''CRYSTAL STRUCTURE OF THE NR1 LIGAND BINDING CORE IN COMPLEX WITH GLYCINE AT 1.35 ANGSTROMS RESOLUTION'''<br />

==Overview==

Excitatory neurotransmission mediated by the N-methyl-D-aspartate subtype, of ionotropic glutamate receptors is fundamental to the development and, function of the mammalian central nervous system. NMDA receptors require, both glycine and glutamate for activation with NR1 and NR2 forming glycine, and glutamate sites, respectively. Mechanisms to describe agonist and, antagonist binding, and activation and desensitization of NMDA receptors, have been hampered by the lack of high-resolution structures. Here, we, describe the cocrystal structures of the NR1 S1S2 ligand-binding core with, the agonists glycine and D-serine (DS), the partial agonist D-cycloserine, (DCS) and the antagonist 5,7-dichlorokynurenic acid (DCKA). The cleft of, the S1S2 'clamshell' is open in the presence of the antagonist DCKA and, closed in the glycine, DS and DCS complexes. In addition, the NR1 S1S2, structure reveals the fold and interactions of loop 1, a cysteine-rich, region implicated in intersubunit allostery.

Excitatory neurotransmission mediated by the N-methyl-D-aspartate subtype of ionotropic glutamate receptors is fundamental to the development and function of the mammalian central nervous system. NMDA receptors require both glycine and glutamate for activation with NR1 and NR2 forming glycine and glutamate sites, respectively. Mechanisms to describe agonist and antagonist binding, and activation and desensitization of NMDA receptors have been hampered by the lack of high-resolution structures. Here, we describe the cocrystal structures of the NR1 S1S2 ligand-binding core with the agonists glycine and D-serine (DS), the partial agonist D-cycloserine (DCS) and the antagonist 5,7-dichlorokynurenic acid (DCKA). The cleft of the S1S2 'clamshell' is open in the presence of the antagonist DCKA and closed in the glycine, DS and DCS complexes. In addition, the NR1 S1S2 structure reveals the fold and interactions of loop 1, a cysteine-rich region implicated in intersubunit allostery.

==About this Structure==

1PB7 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 GLY as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://~~ispc~~.weizmann.ac.il/oca-bin/ocashort?id=1PB7 OCA].

1PB7 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=GLY:'>GLY</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1PB7 OCA].

==Reference==

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[[Category: ligand binding receptor; rat; nr1]]

''Page seeded by [http://~~ispc~~.weizmann.ac.il/oca OCA ] on ~~Tue Nov 20 23~~:39:~~19 2007~~''

''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:27:00 2008''

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@@ Line 1: / Line 1: @@
-[[Image:1pb7.jpg|left|200px]]<br /><applet load="1pb7" size="450" color="white" frame="true" align="right" spinBox="true"
+[[Image:1pb7.jpg|left|200px]]<br /><applet load="1pb7" size="350" color="white" frame="true" align="right" spinBox="true"
 caption="1pb7, resolution 1.35&Aring;" />
 '''CRYSTAL STRUCTURE OF THE NR1 LIGAND BINDING CORE IN COMPLEX WITH GLYCINE AT 1.35 ANGSTROMS RESOLUTION'''<br />
 ==Overview==
-Excitatory neurotransmission mediated by the N-methyl-D-aspartate subtype, of ionotropic glutamate receptors is fundamental to the development and, function of the mammalian central nervous system. NMDA receptors require, both glycine and glutamate for activation with NR1 and NR2 forming glycine, and glutamate sites, respectively. Mechanisms to describe agonist and, antagonist binding, and activation and desensitization of NMDA receptors, have been hampered by the lack of high-resolution structures. Here, we, describe the cocrystal structures of the NR1 S1S2 ligand-binding core with, the agonists glycine and D-serine (DS), the partial agonist D-cycloserine, (DCS) and the antagonist 5,7-dichlorokynurenic acid (DCKA). The cleft of, the S1S2 'clamshell' is open in the presence of the antagonist DCKA and, closed in the glycine, DS and DCS complexes. In addition, the NR1 S1S2, structure reveals the fold and interactions of loop 1, a cysteine-rich, region implicated in intersubunit allostery.
+Excitatory neurotransmission mediated by the N-methyl-D-aspartate subtype of ionotropic glutamate receptors is fundamental to the development and function of the mammalian central nervous system. NMDA receptors require both glycine and glutamate for activation with NR1 and NR2 forming glycine and glutamate sites, respectively. Mechanisms to describe agonist and antagonist binding, and activation and desensitization of NMDA receptors have been hampered by the lack of high-resolution structures. Here, we describe the cocrystal structures of the NR1 S1S2 ligand-binding core with the agonists glycine and D-serine (DS), the partial agonist D-cycloserine (DCS) and the antagonist 5,7-dichlorokynurenic acid (DCKA). The cleft of the S1S2 'clamshell' is open in the presence of the antagonist DCKA and closed in the glycine, DS and DCS complexes. In addition, the NR1 S1S2 structure reveals the fold and interactions of loop 1, a cysteine-rich region implicated in intersubunit allostery.
 ==About this Structure==
-PB7 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 GLY as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1PB7 OCA].
+PB7 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=GLY:'>GLY</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1PB7 OCA].
 ==Reference==
@@ Line 18: / Line 18: @@
 [[Category: ligand binding receptor; rat; nr1]]
-''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Nov 20 23:39:19 2007''
+''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 14:27:00 2008''