5l57
From Proteopedia
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| - | '''Unreleased structure''' | ||
| - | + | ==Crystal structure of Iso-citrate Dehydrogenase R132H in complex with a novel inhibitor (compound 13a)== | |
| + | <StructureSection load='5l57' size='340' side='right'caption='[[5l57]], [[Resolution|resolution]] 2.69Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[5l57]] is a 1 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=5L57 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5L57 FirstGlance]. <br> | ||
| + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.695Å</td></tr> | ||
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=6N3:(1~{R},5~{S})-3-[6-(3-METHYLBUTOXY)-5-[[(1~{R},3~{S})-5-OXIDANYL-2-ADAMANTYL]CARBAMOYL]PYRIDIN-2-YL]-3-AZABICYCLO[3.1.0]HEXANE-6-CARBOXYLIC+ACID'>6N3</scene>, <scene name='pdbligand=NDP:NADPH+DIHYDRO-NICOTINAMIDE-ADENINE-DINUCLEOTIDE+PHOSPHATE'>NDP</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=5l57 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5l57 OCA], [https://pdbe.org/5l57 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5l57 RCSB], [https://www.ebi.ac.uk/pdbsum/5l57 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5l57 ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Disease == | ||
| + | [https://www.uniprot.org/uniprot/IDHC_HUMAN IDHC_HUMAN] Defects in IDH1 are involved in the development of glioma (GLM) [MIM:[https://omim.org/entry/137800 137800]. Gliomas are central nervous system neoplasms derived from glial cells and comprise astrocytomas, glioblastoma multiforme, oligodendrogliomas, and ependymomas. Note=Mutations affecting Arg-132 are tissue-specific, and suggest that this residue plays a unique role in the development of high-grade gliomas. Mutations of Arg-132 to Cys, His, Leu or Ser abolish magnesium binding and abolish the conversion of isocitrate to alpha-ketoglutarate. Instead, alpha-ketoglutarate is converted to R(-)-2-hydroxyglutarate. Elevated levels of R(-)-2-hydroxyglutarate are correlated with an elevated risk of malignant brain tumors. | ||
| + | == Function == | ||
| + | [https://www.uniprot.org/uniprot/IDHC_HUMAN IDHC_HUMAN] | ||
| - | + | ==See Also== | |
| - | + | *[[Isocitrate dehydrogenase 3D structures|Isocitrate dehydrogenase 3D structures]] | |
| - | + | __TOC__ | |
| - | [[Category: | + | </StructureSection> |
| - | [[Category: Levy | + | [[Category: Homo sapiens]] |
| + | [[Category: Large Structures]] | ||
| + | [[Category: Levy C]] | ||
Current revision
Crystal structure of Iso-citrate Dehydrogenase R132H in complex with a novel inhibitor (compound 13a)
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