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6dtn

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'''Unreleased structure'''
 
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The entry 6dtn is ON HOLD until Paper Publication
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==The structure of NTMT1 in complex with compound DC100-1==
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<StructureSection load='6dtn' size='340' side='right'caption='[[6dtn]], [[Resolution|resolution]] 1.48&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[6dtn]] is a 2 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6DTN OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6DTN FirstGlance]. <br>
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</td></tr><tr id='NonStdRes'><td class="sblockLbl"><b>[[Non-Standard_Residue|NonStd Res:]]</b></td><td class="sblockDat"><scene name='pdbligand=6D6:5-{[(3S)-3-AMINO-3-CARBOXYPROPYL](3-AMINOPROPYL)AMINO}-5-DEOXYADENOSINE'>6D6</scene>, <scene name='pdbligand=NH2:AMINO+GROUP'>NH2</scene></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/Protein_N-terminal_methyltransferase Protein N-terminal methyltransferase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.1.1.244 2.1.1.244] </span></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=6dtn FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6dtn OCA], [http://pdbe.org/6dtn PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6dtn RCSB], [http://www.ebi.ac.uk/pdbsum/6dtn PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6dtn ProSAT]</span></td></tr>
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</table>
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== Function ==
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[[http://www.uniprot.org/uniprot/NTM1A_HUMAN NTM1A_HUMAN]] Distributive alpha-N-methyltransferase that methylates the N-terminus of target proteins containing the N-terminal motif [Ala/Pro/Ser]-Pro-Lys when the initiator Met is cleaved. Specifically catalyzes mono-, di- or tri-methylation of exposed alpha-amino group of Ala or Ser residue in the [Ala/Ser]-Pro-Lys motif and mono- or di-methylation of Pro in the Pro-Pro-Lys motif. Some of the substrates may be primed by METTL11B-mediated monomethylation. Responsible for the N-terminal methylation of KLHL31, MYL2, MYL3, RB1, RCC1, RPL23A and SET. Required during mitosis for normal bipolar spindle formation and chromosome segregation via its action on RCC1.<ref>PMID:20481588</ref> <ref>PMID:20668449</ref> <ref>PMID:24090352</ref>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Protein N-terminal methyltransferase 1 (NTMT1) plays an important role in regulating mitosis and DNA repair. Here, we describe the discovery of a potent NTMT1 bisubstrate inhibitor 4 (IC50 = 35 +/- 2 nM) that exhibits greater than 100-fold selectivity against a panel of methyltransferases. We also report the first crystal structure of NTMT1 in complex with an inhibitor, which revealed that 4 occupies substrate and cofactor binding sites of NTMT1.
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Authors:
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Discovery of Bisubstrate Inhibitors for Protein N-Terminal Methyltransferase 1.,Chen D, Dong G, Noinaj N, Huang R J Med Chem. 2019 Mar 27. doi: 10.1021/acs.jmedchem.9b00206. PMID:30883119<ref>PMID:30883119</ref>
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Description:
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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[[Category: Unreleased Structures]]
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</div>
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<div class="pdbe-citations 6dtn" style="background-color:#fffaf0;"></div>
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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: Protein N-terminal methyltransferase]]
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[[Category: Chen, D]]
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[[Category: Huang, R]]
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[[Category: Noinaj, N]]
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[[Category: Enzyme]]
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[[Category: Inhibitor complex]]
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[[Category: Methyltransferase]]
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[[Category: Transferase]]
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[[Category: Transferase-transferase inhibitor complex]]

Revision as of 06:53, 3 April 2019

The structure of NTMT1 in complex with compound DC100-1

PDB ID 6dtn

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