5k4l
From Proteopedia
(Difference between revisions)
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| - | '''Unreleased structure''' | ||
| - | + | ==Crystal structure of KDM5A in complex with a naphthyridone inhibitor== | |
| - | + | <StructureSection load='5k4l' size='340' side='right' caption='[[5k4l]], [[Resolution|resolution]] 3.18Å' scene=''> | |
| - | + | == Structural highlights == | |
| - | + | <table><tr><td colspan='2'>[[5k4l]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5K4L OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5K4L FirstGlance]. <br> | |
| - | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=6QN:~{N}-ETHYL-4-OXIDANYL-2-OXIDANYLIDENE-1~{H}-1,7-NAPHTHYRIDINE-3-CARBOXAMIDE'>6QN</scene>, <scene name='pdbligand=NI:NICKEL+(II)+ION'>NI</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr> | |
| - | [ | + | <tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=UNK:UNKNOWN'>UNK</scene></td></tr> |
| - | [[Category: Kiefer, J | + | <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=5k4l FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5k4l OCA], [http://pdbe.org/5k4l PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5k4l RCSB], [http://www.ebi.ac.uk/pdbsum/5k4l PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5k4l ProSAT]</span></td></tr> |
| - | [[Category: Vinogradova, M | + | </table> |
| + | == Function == | ||
| + | [[http://www.uniprot.org/uniprot/KDM5A_HUMAN KDM5A_HUMAN]] Histone demethylase that specifically demethylates 'Lys-4' of histone H3, thereby playing a central role in histone code. Does not demethylate histone H3 'Lys-9', H3 'Lys-27', H3 'Lys-36', H3 'Lys-79' or H4 'Lys-20'. Demethylates trimethylated and dimethylated but not monomethylated H3 'Lys-4'. May stimulate transcription mediated by nuclear receptors. May be involved in transcriptional regulation of Hox proteins during cell differentiation. May participate in transcriptional repression of cytokines such as CXCL12. Plays a role in the regulation of the circadian rhythm and in maintaining the normal periodicity of the circadian clock. In a histone demethylase-independent manner, acts as a coactivator of the CLOCK-ARNTL/BMAL1-mediated transcriptional activation of PER1/2 and other clock-controlled genes and increases histone acetylation at PER1/2 promoters by inhibiting the activity of HDAC1 (By similarity).[UniProtKB:Q3UXZ9]<ref>PMID:11358960</ref> <ref>PMID:15949438</ref> <ref>PMID:17320160</ref> <ref>PMID:17320161</ref> <ref>PMID:17320163</ref> | ||
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Kiefer, J R]] | ||
| + | [[Category: Vinogradova, M V]] | ||
| + | [[Category: Cancer]] | ||
| + | [[Category: Demethylase]] | ||
| + | [[Category: Epigenetic]] | ||
| + | [[Category: Inhibitor]] | ||
| + | [[Category: Jumonji]] | ||
| + | [[Category: Oxidoreductase-inhibitor complex]] | ||
Revision as of 16:28, 10 August 2016
Crystal structure of KDM5A in complex with a naphthyridone inhibitor
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