7u9i: Difference between revisions
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New page: '''Unreleased structure''' The entry 7u9i is ON HOLD Authors: Zeng, H., Perveen, S., Dong, A., Hutchinson, A., Seitova, A., Gibson, E., Hajian, T., Li, Y., Gao, Y.D., Schneider, S., Sil... |
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==Co-crystal structure of human CARM1 in complex with MT556 inhibitor== | |||
<StructureSection load='7u9i' size='340' side='right'caption='[[7u9i]], [[Resolution|resolution]] 2.00Å' scene=''> | |||
== Structural highlights == | |||
<table><tr><td colspan='2'>[[7u9i]] 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=7U9I OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7U9I FirstGlance]. <br> | |||
</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2Å</td></tr> | |||
[[Category: | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=44T:7-[5-S-(4-{[(4-ethylpyridin-3-yl)methyl]amino}butyl)-5-thio-beta-D-ribofuranosyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine'>44T</scene>, <scene name='pdbligand=UNX:UNKNOWN+ATOM+OR+ION'>UNX</scene></td></tr> | ||
[[Category: | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=7u9i FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7u9i OCA], [https://pdbe.org/7u9i PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7u9i RCSB], [https://www.ebi.ac.uk/pdbsum/7u9i PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7u9i ProSAT]</span></td></tr> | ||
[[Category: Arrowsmith | </table> | ||
[[Category: | == Function == | ||
[[Category: | [https://www.uniprot.org/uniprot/CARM1_HUMAN CARM1_HUMAN] Methylates (mono- and asymmetric dimethylation) the guanidino nitrogens of arginyl residues in several proteins involved in DNA packaging, transcription regulation, pre-mRNA splicing, and mRNA stability. Recruited to promoters upon gene activation together with histone acetyltransferases from EP300/P300 and p160 families, methylates histone H3 at 'Arg-17' (H3R17me), forming mainly asymmetric dimethylarginine (H3R17me2a), leading to activate transcription via chromatin remodeling. During nuclear hormone receptor activation and TCF7L2/TCF4 activation, acts synergically with EP300/P300 and either one of the p160 histone acetyltransferases NCOA1/SRC1, NCOA2/GRIP1 and NCOA3/ACTR or CTNNB1/beta-catenin to activate transcription. During myogenic transcriptional activation, acts together with NCOA3/ACTR as a coactivator for MEF2C. During monocyte inflammatory stimulation, acts together with EP300/P300 as a coactivator for NF-kappa-B. Acts as coactivator for PPARG, promotes adipocyte differentiation and the accumulation of brown fat tissue. Plays a role in the regulation of pre-mRNA alternative splicing by methylation of splicing factors. Also seems to be involved in p53/TP53 transcriptional activation. Methylates EP300/P300, both at 'Arg-2142', which may loosen its interaction with NCOA2/GRIP1, and at 'Arg-580' and 'Arg-604' in the KIX domain, which impairs its interaction with CREB and inhibits CREB-dependent transcriptional activation. Also methylates arginine residues in RNA-binding proteins PABPC1, ELAVL1 and ELAV4, which may affect their mRNA-stabilizing properties and the half-life of their target mRNAs.<ref>PMID:16497732</ref> <ref>PMID:19405910</ref> | ||
[[Category: | == References == | ||
[[Category: | <references/> | ||
[[Category: | __TOC__ | ||
[[Category: | </StructureSection> | ||
[[Category: | [[Category: Homo sapiens]] | ||
[[Category: Halabelian | [[Category: Large Structures]] | ||
[[Category: | [[Category: Arrowsmith CH]] | ||
[[Category: | [[Category: Brown PJ]] | ||
[[Category: | [[Category: Dong A]] | ||
[[Category: | [[Category: Edwards AM]] | ||
[[Category: Perveen | [[Category: Fischer C]] | ||
[[Category: | [[Category: Gao YD]] | ||
[[Category: | [[Category: Gibson E]] | ||
[[Category: | [[Category: Hajian T]] | ||
[[Category: | [[Category: Halabelian L]] | ||
[[Category: | [[Category: Hicks J]] | ||
[[Category: | [[Category: Hutchinson A]] | ||
[[Category: Li Y]] | |||
[[Category: Nicholson B]] | |||
[[Category: Perveen S]] | |||
[[Category: Schneider S]] | |||
[[Category: Seitova A]] | |||
[[Category: Siliphaivanh P]] | |||
[[Category: Sloman D]] | |||
[[Category: Vedadi M]] | |||
[[Category: Zeng H]] | |||
Latest revision as of 09:50, 25 October 2023
Co-crystal structure of human CARM1 in complex with MT556 inhibitor
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