5de1: Difference between revisions
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''' | ==Crystal structure of human IDH1 in complex with GSK321A== | ||
<StructureSection load='5de1' size='340' side='right' caption='[[5de1]], [[Resolution|resolution]] 2.25Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[5de1]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5DE1 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5DE1 FirstGlance]. <br> | |||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=59D:(7R)-1-(4-FLUOROBENZYL)-N-{3-[(1S)-1-HYDROXYETHYL]PHENYL}-7-METHYL-5-(1H-PYRROL-2-YLCARBONYL)-4,5,6,7-TETRAHYDRO-1H-PYRAZOLO[4,3-C]PYRIDINE-3-CARBOXAMIDE'>59D</scene>, <scene name='pdbligand=NAP:NADP+NICOTINAMIDE-ADENINE-DINUCLEOTIDE+PHOSPHATE'>NAP</scene></td></tr> | |||
<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Isocitrate_dehydrogenase_(NADP(+)) Isocitrate dehydrogenase (NADP(+))], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=1.1.1.42 1.1.1.42] </span></td></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=5de1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5de1 OCA], [http://pdbe.org/5de1 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5de1 RCSB], [http://www.ebi.ac.uk/pdbsum/5de1 PDBsum]</span></td></tr> | |||
[[Category: | </table> | ||
== Disease == | |||
[[http://www.uniprot.org/uniprot/IDHC_HUMAN IDHC_HUMAN]] Defects in IDH1 are involved in the development of glioma (GLM) [MIM:[http://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. | |||
__TOC__ | |||
</StructureSection> | |||
[[Category: Concha, N O]] | |||
[[Category: Qi, H]] | |||
[[Category: Smallwood, A]] | [[Category: Smallwood, A]] | ||
[[Category: | [[Category: Allosteric inhibitor]] | ||
[[Category: | [[Category: Idh1]] | ||
[[Category: Nadp+]] | |||
[[Category: Oxidoreductase-oxidoreductase inhibitor complex]] | |||
Revision as of 13:53, 7 October 2015
Crystal structure of human IDH1 in complex with GSK321A
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