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5t4v

From Proteopedia

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Current revision (15:36, 6 March 2024) (edit) (undo)
 
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<StructureSection load='5t4v' size='340' side='right'caption='[[5t4v]], [[Resolution|resolution]] 1.65&Aring;' scene=''>
<StructureSection load='5t4v' size='340' side='right'caption='[[5t4v]], [[Resolution|resolution]] 1.65&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[5t4v]] 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=5T4V OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=5T4V FirstGlance]. <br>
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<table><tr><td colspan='2'>[[5t4v]] 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=5T4V OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5T4V FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=FMT:FORMIC+ACID'>FMT</scene>, <scene name='pdbligand=N48:4-CYANO-N-(7-METHOXY-1,4-DIMETHYL-2-OXO-1,2-DIHYDROQUINOLIN-6-YL)BENZENE-1-SULFONAMIDE'>N48</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]] 1.65&#8491;</td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">BRPF1, BR140 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</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=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=FMT:FORMIC+ACID'>FMT</scene>, <scene name='pdbligand=N48:4-CYANO-N-(7-METHOXY-1,4-DIMETHYL-2-OXO-1,2-DIHYDROQUINOLIN-6-YL)BENZENE-1-SULFONAMIDE'>N48</scene></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=5t4v FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5t4v OCA], [http://pdbe.org/5t4v PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5t4v RCSB], [http://www.ebi.ac.uk/pdbsum/5t4v PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5t4v 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=5t4v FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5t4v OCA], [https://pdbe.org/5t4v PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5t4v RCSB], [https://www.ebi.ac.uk/pdbsum/5t4v PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5t4v ProSAT]</span></td></tr>
</table>
</table>
== Function ==
== Function ==
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[[http://www.uniprot.org/uniprot/BRPF1_HUMAN BRPF1_HUMAN]] Component of the MOZ/MORF complex which has a histone H3 acetyltransferase activity. Positively regulates the transcription of RUNX1 and RUNX2.<ref>PMID:16387653</ref> <ref>PMID:18794358</ref>
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[https://www.uniprot.org/uniprot/BRPF1_HUMAN BRPF1_HUMAN] Component of the MOZ/MORF complex which has a histone H3 acetyltransferase activity. Positively regulates the transcription of RUNX1 and RUNX2.<ref>PMID:16387653</ref> <ref>PMID:18794358</ref>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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The BRPF (bromodomain and PHD finger-containing) family are scaffolding proteins important for the recruitment of histone acetyltransferases of the MYST family to chromatin. Evaluation of the BRPF family as a potential drug target is at an early stage although there is an emerging understanding of a role in acute myeloid leukemia (AML). We report the optimization of fragment hit 5b to 13-d as a biased, potent inhibitor of the BRD of the BRPFs with excellent selectivity over nonclass IV BRD proteins. Evaluation of 13-d in a panel of cancer cell lines showed a selective inhibition of proliferation of a subset of AML lines. Pharmacokinetic studies established that 13-d had properties compatible with oral dosing in mouse models of disease (Fpo 49%). We propose that NI-42 (13-d) is a new chemical probe for the BRPFs suitable for cellular and in vivo studies to explore the fundamental biology of these proteins.
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Design of a Biased Potent Small Molecule Inhibitor of the Bromodomain and PHD Finger-Containing (BRPF) Proteins Suitable for Cellular and in Vivo Studies.,Igoe N, Bayle ED, Fedorov O, Tallant C, Savitsky P, Rogers C, Owen DR, Deb G, Somervaille TC, Andrews DM, Jones N, Cheasty A, Ryder H, Brennan PE, Muller S, Knapp S, Fish PV J Med Chem. 2017 Jan 26;60(2):668-680. doi: 10.1021/acs.jmedchem.6b01583. Epub, 2017 Jan 9. PMID:28068087<ref>PMID:28068087</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 5t4v" style="background-color:#fffaf0;"></div>
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==See Also==
==See Also==
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__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Human]]
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[[Category: Homo sapiens]]
[[Category: Large Structures]]
[[Category: Large Structures]]
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[[Category: Arrowsmith, C H]]
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[[Category: Arrowsmith CH]]
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[[Category: Bayle, E D]]
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[[Category: Bayle ED]]
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[[Category: Bountra, C]]
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[[Category: Bountra C]]
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[[Category: Brennan, P E]]
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[[Category: Brennan PE]]
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[[Category: Delft, F von]]
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[[Category: Edwards AM]]
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[[Category: Edwards, A M]]
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[[Category: Fedorov O]]
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[[Category: Fedorov, O]]
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[[Category: Fish P]]
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[[Category: Fish, P]]
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[[Category: Igoe N]]
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[[Category: Igoe, N]]
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[[Category: Knapp S]]
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[[Category: Knapp, S]]
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[[Category: Mathea S]]
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[[Category: Mathea, S]]
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[[Category: Muller S]]
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[[Category: Muller, S]]
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[[Category: Newman JA]]
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[[Category: Newman, J A]]
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[[Category: Nunez-Alonso G]]
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[[Category: Nunez-Alonso, G]]
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[[Category: Savitsky P]]
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[[Category: Structural genomic]]
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[[Category: Tallant C]]
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[[Category: Savitsky, P]]
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[[Category: Von Delft F]]
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[[Category: Tallant, C]]
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[[Category: Sgc]]
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[[Category: Transcription]]
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Current revision

Crystal structure of the bromodomain of human BRPF1 in complex with NI-48 ligand

PDB ID 5t4v

Drag the structure with the mouse to rotate

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