5m7u
From Proteopedia
(Difference between revisions)
| (2 intermediate revisions not shown.) | |||
| Line 1: | Line 1: | ||
==Structure of human O-GlcNAc hydrolase with new iminocyclitol type inhibitor== | ==Structure of human O-GlcNAc hydrolase with new iminocyclitol type inhibitor== | ||
| - | <StructureSection load='5m7u' size='340' side='right' caption='[[5m7u]], [[Resolution|resolution]] 2.30Å' scene=''> | + | <StructureSection load='5m7u' size='340' side='right'caption='[[5m7u]], [[Resolution|resolution]] 2.30Å' scene=''> |
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>[[5m7u]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5M7U OCA]. For a <b>guided tour on the structure components</b> use [ | + | <table><tr><td colspan='2'>[[5m7u]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5M7U OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5M7U FirstGlance]. <br> |
| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=XHA:2-[(2~{R},3~{S},4~{R},5~{R})-5-(HYDROXYMETHYL)-3,4-BIS(OXIDANYL)-1-[3-[3-(TRIFLUOROMETHYL)PHENYL]PROPYL]PYRROLIDIN-2-YL]-~{N}-METHYL-ETHANAMIDE'>XHA</scene></td></tr> | + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.3Å</td></tr> |
| - | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=XHA:2-[(2~{R},3~{S},4~{R},5~{R})-5-(HYDROXYMETHYL)-3,4-BIS(OXIDANYL)-1-[3-[3-(TRIFLUOROMETHYL)PHENYL]PROPYL]PYRROLIDIN-2-YL]-~{N}-METHYL-ETHANAMIDE'>XHA</scene></td></tr> |
| + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=5m7u FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5m7u OCA], [https://pdbe.org/5m7u PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5m7u RCSB], [https://www.ebi.ac.uk/pdbsum/5m7u PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5m7u ProSAT]</span></td></tr> | ||
</table> | </table> | ||
== Function == | == Function == | ||
| - | [ | + | [https://www.uniprot.org/uniprot/OGA_HUMAN OGA_HUMAN] Isoform 1: Cleaves GlcNAc but not GalNAc from O-glycosylated proteins. Can use p-nitrophenyl-beta-GlcNAc and 4-methylumbelliferone-GlcNAc as substrates but not p-nitrophenyl-beta-GalNAc or p-nitrophenyl-alpha-GlcNAc (in vitro) (PubMed:11148210). Does not bind acetyl-CoA and does not have histone acetyltransferase activity (PubMed:24088714).<ref>PMID:11148210</ref> <ref>PMID:11788610</ref> <ref>PMID:20673219</ref> <ref>PMID:22365600</ref> <ref>PMID:24088714</ref> Isoform 3: Cleaves GlcNAc but not GalNAc from O-glycosylated proteins. Can use p-nitrophenyl-beta-GlcNAc as substrate but not p-nitrophenyl-beta-GalNAc or p-nitrophenyl-alpha-GlcNAc (in vitro), but has about six times lower specific activity than isoform 1.<ref>PMID:20673219</ref> |
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | O-GlcNAc hydrolase (OGA) removes O-linked N-acetylglucosamine (O-GlcNAc) from a myriad of nucleocytoplasmic proteins. Through co-expression and assembly of OGA fragments, we determined the three-dimensional structure of human OGA, revealing an unusual helix-exchanged dimer that lays a structural foundation for an improved understanding of substrate recognition and regulation of OGA. Structures of OGA in complex with a series of inhibitors define a precise blueprint for the design of inhibitors that have clinical value. | ||
| + | |||
| + | Structural and functional insight into human O-GlcNAcase.,Roth C, Chan S, Offen WA, Hemsworth GR, Willems LI, King DT, Varghese V, Britton R, Vocadlo DJ, Davies GJ Nat Chem Biol. 2017 Mar 27. doi: 10.1038/nchembio.2358. PMID:28346405<ref>PMID:28346405</ref> | ||
| + | |||
| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
| + | <div class="pdbe-citations 5m7u" style="background-color:#fffaf0;"></div> | ||
| + | |||
| + | ==See Also== | ||
| + | *[[O-GlcNAcase|O-GlcNAcase]] | ||
== References == | == References == | ||
<references/> | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
| - | [[Category: Britton | + | [[Category: Homo sapiens]] |
| - | [[Category: Chan | + | [[Category: Large Structures]] |
| - | [[Category: Davies | + | [[Category: Britton R]] |
| - | [[Category: Hemsworth | + | [[Category: Chan S]] |
| - | [[Category: King | + | [[Category: Davies GJ]] |
| - | [[Category: Offen | + | [[Category: Hemsworth GR]] |
| - | [[Category: Roth | + | [[Category: King D]] |
| - | [[Category: Varghese | + | [[Category: Offen WA]] |
| - | [[Category: Vocadlo | + | [[Category: Roth C]] |
| - | [[Category: Willems | + | [[Category: Varghese V]] |
| - | + | [[Category: Vocadlo DJ]] | |
| - | + | [[Category: Willems LI]] | |
| - | + | ||
Current revision
Structure of human O-GlcNAc hydrolase with new iminocyclitol type inhibitor
| |||||||||||
Categories: Homo sapiens | Large Structures | Britton R | Chan S | Davies GJ | Hemsworth GR | King D | Offen WA | Roth C | Varghese V | Vocadlo DJ | Willems LI
