5cpr

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==The novel SUV4-20 inhibitor A-196 verifies a role for epigenetics in genomic integrity==
==The novel SUV4-20 inhibitor A-196 verifies a role for epigenetics in genomic integrity==
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<StructureSection load='5cpr' size='340' side='right' caption='[[5cpr]], [[Resolution|resolution]] 2.22&Aring;' scene=''>
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<StructureSection load='5cpr' size='340' side='right'caption='[[5cpr]], [[Resolution|resolution]] 2.22&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[5cpr]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5CPR OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5CPR FirstGlance]. <br>
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<table><tr><td colspan='2'>[[5cpr]] 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=5CPR OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5CPR 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=539:6,7-DICHLORO-N-CYCLOPENTYL-4-(PYRIDIN-4-YL)PHTHALAZIN-1-AMINE'>539</scene>, <scene name='pdbligand=SAM:S-ADENOSYLMETHIONINE'>SAM</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]] 2.22&#8491;</td></tr>
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<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Histone-lysine_N-methyltransferase Histone-lysine N-methyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.1.1.43 2.1.1.43] </span></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=539:6,7-DICHLORO-N-CYCLOPENTYL-4-(PYRIDIN-4-YL)PHTHALAZIN-1-AMINE'>539</scene>, <scene name='pdbligand=SAM:S-ADENOSYLMETHIONINE'>SAM</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=5cpr FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5cpr OCA], [http://pdbe.org/5cpr PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5cpr RCSB], [http://www.ebi.ac.uk/pdbsum/5cpr PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5cpr 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=5cpr FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5cpr OCA], [https://pdbe.org/5cpr PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5cpr RCSB], [https://www.ebi.ac.uk/pdbsum/5cpr PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5cpr ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
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[[http://www.uniprot.org/uniprot/SV421_HUMAN SV421_HUMAN]] Histone methyltransferase that specifically trimethylates 'Lys-20' of histone H4. H4 'Lys-20' trimethylation represents a specific tag for epigenetic transcriptional repression. Mainly functions in pericentric heterochromatin regions, thereby playing a central role in the establishment of constitutive heterochromatin in these regions. SUV420H1 is targeted to histone H3 via its interaction with RB1 family proteins (RB1, RBL1 and RBL2) (By similarity).
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[https://www.uniprot.org/uniprot/KMT5B_HUMAN KMT5B_HUMAN] Histone methyltransferase that specifically trimethylates 'Lys-20' of histone H4. H4 'Lys-20' trimethylation represents a specific tag for epigenetic transcriptional repression. Mainly functions in pericentric heterochromatin regions, thereby playing a central role in the establishment of constitutive heterochromatin in these regions. KMT5B is targeted to histone H3 via its interaction with RB1 family proteins (RB1, RBL1 and RBL2) (By similarity). Plays a role in myogenesis by regulating the expression of target genes, such as EID3.<ref>PMID:23720823</ref>
<div style="background-color:#fffaf0;">
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
== Publication Abstract from PubMed ==
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</div>
</div>
<div class="pdbe-citations 5cpr" style="background-color:#fffaf0;"></div>
<div class="pdbe-citations 5cpr" style="background-color:#fffaf0;"></div>
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==See Also==
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*[[Histone methyltransferase 3D structures|Histone methyltransferase 3D structures]]
== References ==
== References ==
<references/>
<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Histone-lysine N-methyltransferase]]
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[[Category: Homo sapiens]]
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[[Category: Jakob, C G]]
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[[Category: Large Structures]]
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[[Category: Sun, C]]
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[[Category: Jakob CG]]
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[[Category: Upadhyay, A K]]
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[[Category: Sun C]]
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[[Category: H4k20]]
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[[Category: Upadhyay AK]]
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[[Category: Non-homologous end joining]]
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[[Category: Protein lysine transferase]]
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[[Category: Transferase]]
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Current revision

The novel SUV4-20 inhibitor A-196 verifies a role for epigenetics in genomic integrity

PDB ID 5cpr

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