6nt2

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'''Unreleased structure'''
 
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The entry 6nt2 is ON HOLD until Paper Publication
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==type 1 PRMT in complex with the inhibitor GSK3368715==
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<StructureSection load='6nt2' size='340' side='right'caption='[[6nt2]], [[Resolution|resolution]] 2.48&Aring;' scene=''>
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Authors: Concha, N.O.
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== Structural highlights ==
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<table><tr><td colspan='2'>[[6nt2]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6NT2 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6NT2 FirstGlance]. <br>
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Description: type 1 PRMT in complex with the inhibitor GSK3368715
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=DTT:2,3-DIHYDROXY-1,4-DITHIOBUTANE'>DTT</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=KZS:N~1~-({5-[4,4-bis(ethoxymethyl)cyclohexyl]-1H-pyrazol-4-yl}methyl)-N~1~,N~2~-dimethylethane-1,2-diamine'>KZS</scene>, <scene name='pdbligand=SAH:S-ADENOSYL-L-HOMOCYSTEINE'>SAH</scene></td></tr>
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[[Category: Unreleased Structures]]
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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/Type_I_protein_arginine_methyltransferase Type I protein arginine methyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.1.1.319 2.1.1.319] </span></td></tr>
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[[Category: Concha, N.O]]
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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=6nt2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6nt2 OCA], [http://pdbe.org/6nt2 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6nt2 RCSB], [http://www.ebi.ac.uk/pdbsum/6nt2 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6nt2 ProSAT]</span></td></tr>
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</table>
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== Function ==
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[[http://www.uniprot.org/uniprot/ANM1_HUMAN ANM1_HUMAN]] Arginine methyltransferase that methylates (mono and asymmetric dimethylation) the guanidino nitrogens of arginyl residues present in proteins such as ESR1, histone H2, H3 and H4, ILF3, HNRNPA1, HNRNPD, NFATC2IP, SUPT5H, TAF15, EWS, HABP4 and SERBP1 (PubMed:10749851, PubMed:16879614, PubMed:26876602). Constitutes the main enzyme that mediates monomethylation and asymmetric dimethylation of histone H4 'Arg-4' (H4R3me1 and H4R3me2a, respectively), a specific tag for epigenetic transcriptional activation. May be involved in the regulation of TAF15 transcriptional activity, act as an activator of estrogen receptor (ER)-mediated transactivation, play a key role in neurite outgrowth and act as a negative regulator of megakaryocytic differentiation, by modulating p38 MAPK pathway. Methylates RBM15, promoting ubiquitination and degradation of RBM15 (PubMed:26575292). Methylates FOXO1 and retains it in the nucleus increasing its transcriptional activity. Methylates CHTOP and this methylation is critical for its 5-hydroxymethylcytosine (5hmC)-binding activity (PubMed:25284789). Methylates H4R3 in genes involved in glioblastomagenesis in a CHTOP- and/or TET1-dependent manner (PubMed:25284789).<ref>PMID:10749851</ref> <ref>PMID:11387442</ref> <ref>PMID:11448779</ref> <ref>PMID:12718890</ref> <ref>PMID:16879614</ref> <ref>PMID:18320585</ref> <ref>PMID:18657504</ref> <ref>PMID:18773938</ref> <ref>PMID:19124016</ref> <ref>PMID:19405910</ref> <ref>PMID:20442406</ref> <ref>PMID:25284789</ref> <ref>PMID:26575292</ref> <ref>PMID:26876602</ref> <ref>PMID:28040436</ref>
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== References ==
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<references/>
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__TOC__
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</StructureSection>
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[[Category: Large Structures]]
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[[Category: Type I protein arginine methyltransferase]]
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[[Category: Concha, N O]]
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[[Category: Antitumor protein]]
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[[Category: Arginine]]
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[[Category: Cmplex]]
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[[Category: Inhibitor]]
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[[Category: Methyl transferase]]

Revision as of 05:47, 10 July 2019

type 1 PRMT in complex with the inhibitor GSK3368715

PDB ID 6nt2

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