4mqu
From Proteopedia
(Difference between revisions)
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<StructureSection load='4mqu' size='340' side='right' caption='[[4mqu]], [[Resolution|resolution]] 2.22Å' scene=''> | <StructureSection load='4mqu' size='340' side='right' caption='[[4mqu]], [[Resolution|resolution]] 2.22Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>[[4mqu]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4MQU OCA]. <br> | + | <table><tr><td colspan='2'>[[4mqu]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4MQU OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4MQU FirstGlance]. <br> |
| - | </td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=IOD:IODIDE+ION'>IOD</scene>, <scene name='pdbligand=MG9:2-{4-[(2S)-4-[(6-AMINOPYRIDIN-3-YL)SULFONYL]-2-(PROP-1-YN-1-YL)PIPERAZIN-1-YL]PHENYL}-1,1,1,3,3,3-HEXAFLUOROPROPAN-2-OL'>MG9</scene>, <scene name='pdbligand=S6P:D-SORBITOL-6-PHOSPHATE'>S6P</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene>< | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=IOD:IODIDE+ION'>IOD</scene>, <scene name='pdbligand=MG9:2-{4-[(2S)-4-[(6-AMINOPYRIDIN-3-YL)SULFONYL]-2-(PROP-1-YN-1-YL)PIPERAZIN-1-YL]PHENYL}-1,1,1,3,3,3-HEXAFLUOROPROPAN-2-OL'>MG9</scene>, <scene name='pdbligand=S6P:D-SORBITOL-6-PHOSPHATE'>S6P</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene></td></tr> |
| - | <tr><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4mro|4mro]]</td></tr> | + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4mro|4mro]]</td></tr> |
| - | <tr | + | <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=4mqu FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4mqu OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4mqu RCSB], [http://www.ebi.ac.uk/pdbsum/4mqu PDBsum]</span></td></tr> |
| - | + | </table> | |
| - | <table> | + | == Function == |
| + | [[http://www.uniprot.org/uniprot/GCKR_HUMAN GCKR_HUMAN]] Inhibits glucokinase by forming an inactive complex with this enzyme. | ||
<div style="background-color:#fffaf0;"> | <div style="background-color:#fffaf0;"> | ||
== Publication Abstract from PubMed == | == Publication Abstract from PubMed == | ||
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Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles.,St Jean DJ Jr, Ashton KS, Bartberger MD, Chen J, Chmait S, Cupples R, Galbreath E, Helmering J, Hong FT, Jordan SR, Liu L, Kunz RK, Michelsen K, Nishimura N, Pennington LD, Poon SF, Reid D, Sivits G, Stec MM, Tadesse S, Tamayo N, Van G, Yang KC, Zhang J, Norman MH, Fotsch C, Lloyd DJ, Hale C J Med Chem. 2014 Jan 23;57(2):325-38. doi: 10.1021/jm4016747. Epub 2014 Jan 9. PMID:24405213<ref>PMID:24405213</ref> | Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 2. Leveraging structure-based drug design to identify analogues with improved pharmacokinetic profiles.,St Jean DJ Jr, Ashton KS, Bartberger MD, Chen J, Chmait S, Cupples R, Galbreath E, Helmering J, Hong FT, Jordan SR, Liu L, Kunz RK, Michelsen K, Nishimura N, Pennington LD, Poon SF, Reid D, Sivits G, Stec MM, Tadesse S, Tamayo N, Van G, Yang KC, Zhang J, Norman MH, Fotsch C, Lloyd DJ, Hale C J Med Chem. 2014 Jan 23;57(2):325-38. doi: 10.1021/jm4016747. Epub 2014 Jan 9. PMID:24405213<ref>PMID:24405213</ref> | ||
| - | From | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> |
</div> | </div> | ||
== References == | == References == | ||
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__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
| - | [[Category: Ashton, K S | + | [[Category: Ashton, K S]] |
| - | [[Category: Bartberger, M D | + | [[Category: Bartberger, M D]] |
| - | [[Category: Chen, J | + | [[Category: Chen, J]] |
| - | [[Category: Chmait, S | + | [[Category: Chmait, S]] |
| - | [[Category: Cupples, R | + | [[Category: Cupples, R]] |
| - | [[Category: Galbreath, E | + | [[Category: Galbreath, E]] |
| - | [[Category: Helmering, J | + | [[Category: Helmering, J]] |
| - | [[Category: Jean, D J.St | + | [[Category: Jean, D J.St]] |
| - | [[Category: Jordan, S R | + | [[Category: Jordan, S R]] |
| - | [[Category: Liu, L | + | [[Category: Liu, L]] |
[[Category: Binds fructose phosphates and glucokinase]] | [[Category: Binds fructose phosphates and glucokinase]] | ||
[[Category: Regulatory protein]] | [[Category: Regulatory protein]] | ||
[[Category: Sis domain]] | [[Category: Sis domain]] | ||
[[Category: Transferase inhibitor]] | [[Category: Transferase inhibitor]] | ||
Revision as of 15:42, 24 December 2014
Human GKRP complexed to AMG-3969 and S6P
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