5a2s
From Proteopedia
(Difference between revisions)
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<StructureSection load='5a2s' size='340' side='right'caption='[[5a2s]], [[Resolution|resolution]] 2.65Å' scene=''> | <StructureSection load='5a2s' size='340' side='right'caption='[[5a2s]], [[Resolution|resolution]] 2.65Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>[[5a2s]] is a 2 chain structure with sequence from [ | + | <table><tr><td colspan='2'>[[5a2s]] 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=5A2S OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5A2S FirstGlance]. <br> |
| - | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=OTF:(1S,2S,3S)-1-FLUORANYL-2-[4-(5-FLUORANYLPYRIMIDIN-2-YL)PHENYL]-N-OXIDANYL-3-PHENYL-CYCLOPROPANE-1-CARBOXAMIDE'>OTF</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=OTF:(1S,2S,3S)-1-FLUORANYL-2-[4-(5-FLUORANYLPYRIMIDIN-2-YL)PHENYL]-N-OXIDANYL-3-PHENYL-CYCLOPROPANE-1-CARBOXAMIDE'>OTF</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</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=5a2s FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5a2s OCA], [https://pdbe.org/5a2s PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5a2s RCSB], [https://www.ebi.ac.uk/pdbsum/5a2s PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5a2s ProSAT]</span></td></tr> | |
| - | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | + | |
</table> | </table> | ||
== Disease == | == Disease == | ||
| - | [ | + | [https://www.uniprot.org/uniprot/HDAC4_HUMAN HDAC4_HUMAN] Defects in HDAC4 are the cause of brachydactyly-mental retardation syndrome (BDMR) [MIM:[https://omim.org/entry/600430 600430]. A syndrome resembling the physical anomalies found in Albright hereditary osteodystrophy. Common features are mild facial dysmorphism, congenital heart defects, distinct brachydactyly type E, mental retardation, developmental delay, seizures, autism spectrum disorder, and stocky build. Soft tissue ossification is absent, and there are no abnormalities in parathyroid hormone or calcium metabolism.<ref>PMID:20691407</ref> |
== Function == | == Function == | ||
| - | [ | + | [https://www.uniprot.org/uniprot/HDAC4_HUMAN HDAC4_HUMAN] Responsible for the deacetylation of lysine residues on the N-terminal part of the core histones (H2A, H2B, H3 and H4). Histone deacetylation gives a tag for epigenetic repression and plays an important role in transcriptional regulation, cell cycle progression and developmental events. Histone deacetylases act via the formation of large multiprotein complexes. Involved in muscle maturation via its interaction with the myocyte enhancer factors such as MEF2A, MEF2C and MEF2D.<ref>PMID:10523670</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== | ||
| - | *[[Histone deacetylase|Histone deacetylase]] | + | *[[Histone deacetylase 3D structures|Histone deacetylase 3D structures]] |
== References == | == References == | ||
<references/> | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
| - | [[Category: | + | [[Category: Homo sapiens]] |
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[[Category: Large Structures]] | [[Category: Large Structures]] | ||
| - | [[Category: Aziz | + | [[Category: Aziz O]] |
| - | [[Category: Birch | + | [[Category: Birch H]] |
| - | [[Category: Breccia | + | [[Category: Breccia P]] |
| - | [[Category: Burli | + | [[Category: Burli RW]] |
| - | [[Category: Dominguez | + | [[Category: Dominguez C]] |
| - | [[Category: Hughes | + | [[Category: Hughes S]] |
| - | [[Category: Jarvis | + | [[Category: Jarvis RE]] |
| - | [[Category: Lamers | + | [[Category: Lamers M]] |
| - | [[Category: Leonard | + | [[Category: Leonard P]] |
| - | [[Category: Luckhurst | + | [[Category: Luckhurst CA]] |
| - | [[Category: Matthews | + | [[Category: Matthews KL]] |
| - | [[Category: McAllister | + | [[Category: McAllister G]] |
| - | [[Category: Pollack | + | [[Category: Pollack S]] |
| - | [[Category: Saville-Stones | + | [[Category: Saville-Stones E]] |
| - | [[Category: Stott | + | [[Category: Stott AJ]] |
| - | [[Category: Wishart | + | [[Category: Wishart G]] |
| - | [[Category: Yates | + | [[Category: Yates D]] |
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Revision as of 04:35, 25 May 2023
Potent, selective and CNS-penetrant tetrasubstituted cyclopropane class IIa histone deacetylase (HDAC) inhibitors
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Categories: Homo sapiens | Large Structures | Aziz O | Birch H | Breccia P | Burli RW | Dominguez C | Hughes S | Jarvis RE | Lamers M | Leonard P | Luckhurst CA | Matthews KL | McAllister G | Pollack S | Saville-Stones E | Stott AJ | Wishart G | Yates D
