5fp3

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==Cell penetrant inhibitors of the JMJD2 (KDM4) and JARID1 (KDM5) families of histone lysine demethylases==
==Cell penetrant inhibitors of the JMJD2 (KDM4) and JARID1 (KDM5) families of histone lysine demethylases==
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<StructureSection load='5fp3' size='340' side='right' caption='[[5fp3]], [[Resolution|resolution]] 2.05&Aring;' scene=''>
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<StructureSection load='5fp3' size='340' side='right'caption='[[5fp3]], [[Resolution|resolution]] 2.05&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[5fp3]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5FP3 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5FP3 FirstGlance]. <br>
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<table><tr><td colspan='2'>[[5fp3]] 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=5FP3 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5FP3 FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=3JI:3-(4-PHENYLBUTANAMIDO)PYRIDINE-4-CARBOXYLIC+ACID'>3JI</scene>, <scene name='pdbligand=BCN:BICINE'>BCN</scene>, <scene name='pdbligand=CO:COBALT+(II)+ION'>CO</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.05&#8491;</td></tr>
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<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[5fp4|5fp4]], [[5fp7|5fp7]], [[5fp8|5fp8]], [[5fp9|5fp9]], [[5fpa|5fpa]], [[5fpb|5fpb]]</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=BCN:BICINE'>BCN</scene>, <scene name='pdbligand=CO:COBALT+(II)+ION'>CO</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=YC8:3-(4-PHENYLBUTANOYLAMINO)PYRIDINE-4-CARBOXYLIC+ACID'>YC8</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
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<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=5fp3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5fp3 OCA], [http://pdbe.org/5fp3 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5fp3 RCSB], [http://www.ebi.ac.uk/pdbsum/5fp3 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5fp3 ProSAT]</span></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=5fp3 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5fp3 OCA], [https://pdbe.org/5fp3 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5fp3 RCSB], [https://www.ebi.ac.uk/pdbsum/5fp3 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5fp3 ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
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[[http://www.uniprot.org/uniprot/KDM6B_HUMAN KDM6B_HUMAN]] Histone demethylase that specifically demethylates 'Lys-27' of histone H3, thereby playing a central role in histone code. Demethylates trimethylated and dimethylated H3 'Lys-27'. Plays a central role in regulation of posterior development, by regulating HOX gene expression. Involved in inflammatory response by participating in macrophage differentiation in case of inflammation by regulating gene expression and macrophage differentiation.<ref>PMID:17825402</ref> <ref>PMID:17851529</ref>
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[https://www.uniprot.org/uniprot/KDM6B_HUMAN KDM6B_HUMAN] Histone demethylase that specifically demethylates 'Lys-27' of histone H3, thereby playing a central role in histone code. Demethylates trimethylated and dimethylated H3 'Lys-27'. Plays a central role in regulation of posterior development, by regulating HOX gene expression. Involved in inflammatory response by participating in macrophage differentiation in case of inflammation by regulating gene expression and macrophage differentiation.<ref>PMID:17825402</ref> <ref>PMID:17851529</ref>
<div style="background-color:#fffaf0;">
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
== Publication Abstract from PubMed ==
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==See Also==
==See Also==
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*[[Jumonji domain-containing protein|Jumonji domain-containing protein]]
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*[[Jumonji domain-containing protein 3D structures|Jumonji domain-containing protein 3D structures]]
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Human]]
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[[Category: Homo sapiens]]
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[[Category: Chung, C]]
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[[Category: Large Structures]]
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[[Category: Inhibitor]]
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[[Category: Chung C]]
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[[Category: Jmjd3]]
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[[Category: Jumonji]]
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[[Category: Kdm6b]]
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[[Category: Oxidoreductase]]
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Current revision

Cell penetrant inhibitors of the JMJD2 (KDM4) and JARID1 (KDM5) families of histone lysine demethylases

PDB ID 5fp3

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