4mf3

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<StructureSection load='4mf3' size='340' side='right' caption='[[4mf3]], [[Resolution|resolution]] 3.00&Aring;' scene=''>
<StructureSection load='4mf3' size='340' side='right' caption='[[4mf3]], [[Resolution|resolution]] 3.00&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[4mf3]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4MF3 OCA]. <br>
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<table><tr><td colspan='2'>[[4mf3]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4MF3 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4MF3 FirstGlance]. <br>
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</td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=SXI:(3S,4AS,6S,8AR)-6-[3-CHLORO-2-(1H-TETRAZOL-5-YL)PHENOXY]DECAHYDROISOQUINOLINE-3-CARBOXYLIC+ACID'>SXI</scene><br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=SXI:(3S,4AS,6S,8AR)-6-[3-CHLORO-2-(1H-TETRAZOL-5-YL)PHENOXY]DECAHYDROISOQUINOLINE-3-CARBOXYLIC+ACID'>SXI</scene></td></tr>
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<tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Glucokinase Glucokinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.2 2.7.1.2] </span></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4mf3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4mf3 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4mf3 RCSB], [http://www.ebi.ac.uk/pdbsum/4mf3 PDBsum]</span></td></tr>
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<tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4mf3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4mf3 OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4mf3 RCSB], [http://www.ebi.ac.uk/pdbsum/4mf3 PDBsum]</span></td></tr>
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</table>
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<table>
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== Function ==
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[[http://www.uniprot.org/uniprot/GRIK1_HUMAN GRIK1_HUMAN]] Ionotropic glutamate receptor. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. Binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, and thereby converts the chemical signal to an electrical impulse. The receptor then desensitizes rapidly and enters a transient inactive state, characterized by the presence of bound agonist. May be involved in the transmission of light information from the retina to the hypothalamus.
<div style="background-color:#fffaf0;">
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
== Publication Abstract from PubMed ==
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GluK1 antagonists from 6-(tetrazolyl)phenyl decahydroisoquinoline derivatives: in vitro profile and in vivo analgesic efficacy.,Martinez-Perez JA, Iyengar S, Shannon HE, Bleakman D, Alt A, Clawson DK, Arnold BM, Bell MG, Bleisch TJ, Castano AM, Del Prado M, Dominguez E, Escribano AM, Filla SA, Ho KH, Hudziak KJ, Jones CK, Mateo A, Mathes BM, Mattiuz EL, Ogden AM, Simmons RM, Stack DR, Stratford RE, Winter MA, Wu Z, Ornstein PL Bioorg Med Chem Lett. 2013 Dec 1;23(23):6463-6. doi: 10.1016/j.bmcl.2013.09.045. , Epub 2013 Sep 24. PMID:24140446<ref>PMID:24140446</ref>
GluK1 antagonists from 6-(tetrazolyl)phenyl decahydroisoquinoline derivatives: in vitro profile and in vivo analgesic efficacy.,Martinez-Perez JA, Iyengar S, Shannon HE, Bleakman D, Alt A, Clawson DK, Arnold BM, Bell MG, Bleisch TJ, Castano AM, Del Prado M, Dominguez E, Escribano AM, Filla SA, Ho KH, Hudziak KJ, Jones CK, Mateo A, Mathes BM, Mattiuz EL, Ogden AM, Simmons RM, Stack DR, Stratford RE, Winter MA, Wu Z, Ornstein PL Bioorg Med Chem Lett. 2013 Dec 1;23(23):6463-6. doi: 10.1016/j.bmcl.2013.09.045. , Epub 2013 Sep 24. PMID:24140446<ref>PMID:24140446</ref>
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
</div>
</div>
== References ==
== References ==
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__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Alt, A.]]
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[[Category: Alt, A]]
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[[Category: Arnold, B M.]]
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[[Category: Arnold, B M]]
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[[Category: Bell, M G.]]
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[[Category: Bell, M G]]
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[[Category: Bleakman, D.]]
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[[Category: Bleakman, D]]
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[[Category: Bleisch, T J.]]
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[[Category: Bleisch, T J]]
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[[Category: Castano, A M.]]
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[[Category: Castano, A M]]
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[[Category: Clawson, D K.]]
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[[Category: Clawson, D K]]
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[[Category: Dominguez, E.]]
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[[Category: Dominguez, E]]
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[[Category: Escribano, A M.]]
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[[Category: Escribano, A M]]
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[[Category: Filla, S A.]]
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[[Category: Filla, S A]]
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[[Category: Ho, K H.]]
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[[Category: Ho, K H]]
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[[Category: Hudziak, K J.]]
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[[Category: Hudziak, K J]]
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[[Category: Iyengar, S.]]
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[[Category: Iyengar, S]]
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[[Category: Jones, C K.]]
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[[Category: Jones, C K]]
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[[Category: Katofiasc, M A.]]
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[[Category: Katofiasc, M A]]
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[[Category: Martinez-Perez, J A.]]
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[[Category: Martinez-Perez, J A]]
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[[Category: Mateo, A.]]
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[[Category: Mateo, A]]
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[[Category: Mathes, B M.]]
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[[Category: Mathes, B M]]
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[[Category: Mattiuz, E L.]]
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[[Category: Mattiuz, E L]]
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[[Category: Ogden, A M.L.]]
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[[Category: Ogden, A M.L]]
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[[Category: Ornstein, P L.]]
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[[Category: Ornstein, P L]]
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[[Category: Phebus, L A.]]
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[[Category: Phebus, L A]]
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[[Category: Prado, M Del.]]
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[[Category: Prado, M Del]]
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[[Category: Shannon, H E.]]
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[[Category: Shannon, H E]]
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[[Category: Simmons, R M.A.]]
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[[Category: Simmons, R M.A]]
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[[Category: Stack, D R.]]
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[[Category: Stack, D R]]
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[[Category: Stratford, R E.]]
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[[Category: Stratford, R E]]
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[[Category: Winter, M A.]]
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[[Category: Winter, M A]]
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[[Category: Wu, Z.]]
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[[Category: Wu, Z]]
[[Category: Glutamate binding]]
[[Category: Glutamate binding]]
[[Category: Glutamate receptor]]
[[Category: Glutamate receptor]]

Revision as of 14:04, 24 December 2014

Crystal Structure of Human GRIK1 complexed with a 6-(tetrazolyl)aryl decahydroisoquinoline antagonist

4mf3, resolution 3.00Å

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