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3vuz

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{{STRUCTURE_3vuz| PDB=3vuz | SCENE= }}
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==Crystal structure of histone methyltransferase SET7/9 in comlex with AAM-1==
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===Crystal structure of histone methyltransferase SET7/9 in comlex with AAM-1===
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<StructureSection load='3vuz' size='340' side='right' caption='[[3vuz]], [[Resolution|resolution]] 2.50&Aring;' scene=''>
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== Structural highlights ==
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[[3vuz]] is a 1 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=3VUZ OCA]. <br>
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<b>Related:</b> [[3vv0|3vv0]]<br>
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<b>Activity:</b> <span class='plainlinks'>[http://en.wikipedia.org/wiki/Glucokinase Glucokinase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.2 2.7.1.2] </span><br>
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== Publication Abstract from PubMed ==
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SET7/9 is a protein lysine methyltransferase that methylates histone H3 and nonhistone proteins such as p53, TAF10 and oestrogen receptor alpha. In previous work, novel inhibitors of SET7/9 that are amine analogues of the coenzyme S-(5'-adenosyl)-L-methionine (AdoMet) have been developed. Here, crystal structures of SET7/9 are reported in complexes with two AdoMet analogues, designated DAAM-3 and AAM-1, in which an n-hexylaminoethyl group or an n-hexyl group is attached to the N atom that replaces the S atom of AdoMet, respectively. In both structures, the inhibitors bind to the coenzyme-binding site and their additional alkyl chain binds in the lysine-access channel. The N atom in the azaalkyl chain of DAAM-3 is located at almost the same position as the N-methyl C atom of the methylated lysine side chain in the substrate-peptide complex structures and stabilizes complex formation by hydrogen bonding to the substrate-binding site residues of SET7/9. On the other hand, the alkyl chain of AAM-1, which is a weaker inhibitor than DAAM-3, binds in the lysine-access channel only through hydrophobic and van der Waals interactions. Unexpectedly, the substrate-binding site of SET7/9 complexed with AAM-1 specifically interacts with the artificial N-terminal sequence of an adjacent symmetry-related molecule, presumably stabilizing the alkyl chain of AAM-1.
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==Function==
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Structures of histone methyltransferase SET7/9 in complexes with adenosylmethionine derivatives.,Niwa H, Handa N, Tomabechi Y, Honda K, Toyama M, Ohsawa N, Shirouzu M, Kagechika H, Hirano T, Umehara T, Yokoyama S Acta Crystallogr D Biol Crystallogr. 2013 Apr;69(Pt 4):595-602. doi:, 10.1107/S0907444912052092. Epub 2013 Mar 14. PMID:23519668<ref>PMID:23519668</ref>
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[[http://www.uniprot.org/uniprot/SETD7_HUMAN SETD7_HUMAN]] Histone methyltransferase that specifically monomethylates 'Lys-4' of histone H3. H3 'Lys-4' methylation represents a specific tag for epigenetic transcriptional activation. Plays a central role in the transcriptional activation of genes such as collagenase or insulin. Recruited by IPF1/PDX-1 to the insulin promoter, leading to activate transcription. Has also methyltransferase activity toward non-histone proteins such as p53/TP53, TAF10, and possibly TAF7 by recognizing and binding the [KR]-[STA]-K in substrate proteins. Monomethylates 'Lys-189' of TAF10, leading to increase the affinity of TAF10 for RNA polymerase II. Monomethylates 'Lys-372' of p53/TP53, stabilizing p53/TP53 and increasing p53/TP53-mediated transcriptional activation.<ref>PMID:12588998</ref><ref>PMID:15099517</ref><ref>PMID:16141209</ref><ref>PMID:17108971</ref><ref>PMID:12540855</ref><ref>PMID:15525938</ref>
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==About this Structure==
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br>
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[[3vuz]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3VUZ OCA].
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== References ==
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<references/>
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==Reference==
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__TOC__
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<references group="xtra"/><references/>
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</StructureSection>
[[Category: Histone-lysine N-methyltransferase]]
[[Category: Histone-lysine N-methyltransferase]]
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[[Category: Homo sapiens]]
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[[Category: Human]]
[[Category: Handa, N.]]
[[Category: Handa, N.]]
[[Category: Hirano, T.]]
[[Category: Hirano, T.]]

Revision as of 05:22, 30 April 2014

Crystal structure of histone methyltransferase SET7/9 in comlex with AAM-1

3vuz, resolution 2.50Å

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