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5myg

From Proteopedia

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Current revision

Crystal structure of the bromodomain of human BRPF1 in complex with NI-57 chemical probe

Structural highlights

5myg is a 4 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Method:	X-ray diffraction, Resolution 2.3Å
Ligands:
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

BRPF1_HUMAN Component of the MOZ/MORF complex which has a histone H3 acetyltransferase activity. Positively regulates the transcription of RUNX1 and RUNX2.^[1] ^[2]

Publication Abstract from PubMed

The bromodomain and PHD finger-containing (BRPF) family are scaffolding proteins important for the recruitment of histone acetyltransferases of the MYST family to chromatin. Here we describe NI-57 (16) as new pan-BRPF chemical probe of the bromodomain (BRD) of the BRPFs. Inhibitor 16 preferentially bound the BRD of BRPF1 and BRD1 over BRPF3, whereas binding to BRD9 was weaker. 16 has excellent selectivity over non-class IV BRD proteins. Target engagement of BRPF1B and BRD1 with 16 was demonstrated in nanoBRET and FRAP assays. The binding of 16 to BRPF1B was rationalized through an X-ray co-crystal structure determination which showed a flipped binding orientation when compared to previous structures. We report studies that show 16 has functional activity in cellular assays by modulation of the phenotype at low mumolar concentrations in both cancer and inflammatory models. Pharmacokinetic data for 16 was generated in mouse with single dose administration showing favourable oral bioavailability.

Design of a chemical probe for the Bromodomain and Plant Homeodomain Finger-containing (BRPF) family of proteins.,Igoe N, Bayle ED, Tallant C, Fedorov O, Meier JC, Savitsky P, Rogers C, Morias Y, Scholze S, Boyd H, Cunoosamy D, Andrews DM, Cheasty A, Brennan PE, Muller S, Knapp S, Fish PV J Med Chem. 2017 Jul 17. doi: 10.1021/acs.jmedchem.7b00611. PMID:28714688^[3]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

References

↑ Doyon Y, Cayrou C, Ullah M, Landry AJ, Cote V, Selleck W, Lane WS, Tan S, Yang XJ, Cote J. ING tumor suppressor proteins are critical regulators of chromatin acetylation required for genome expression and perpetuation. Mol Cell. 2006 Jan 6;21(1):51-64. PMID:16387653 doi:10.1016/j.molcel.2005.12.007
↑ Ullah M, Pelletier N, Xiao L, Zhao SP, Wang K, Degerny C, Tahmasebi S, Cayrou C, Doyon Y, Goh SL, Champagne N, Cote J, Yang XJ. Molecular architecture of quartet MOZ/MORF histone acetyltransferase complexes. Mol Cell Biol. 2008 Nov;28(22):6828-43. doi: 10.1128/MCB.01297-08. Epub 2008 Sep , 15. PMID:18794358 doi:10.1128/MCB.01297-08
↑ Igoe N, Bayle ED, Tallant C, Fedorov O, Meier JC, Savitsky P, Rogers C, Morias Y, Scholze S, Boyd H, Cunoosamy D, Andrews DM, Cheasty A, Brennan PE, Muller S, Knapp S, Fish PV. Design of a chemical probe for the Bromodomain and Plant Homeodomain Finger-containing (BRPF) family of proteins. J Med Chem. 2017 Jul 17. doi: 10.1021/acs.jmedchem.7b00611. PMID:28714688 doi:http://dx.doi.org/10.1021/acs.jmedchem.7b00611

1 Structural highlights
2 Function
3 Publication Abstract from PubMed
4 See Also
5 References

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/5myg"

@@ Line 3: / Line 3: @@
 <StructureSection load='5myg' size='340' side='right'caption='[[5myg]], [[Resolution|resolution]] 2.30&Aring;' scene=''>
 == Structural highlights ==
-<table><tr><td colspan='2'>[[5myg]] is a 4 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5MYG OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=5MYG FirstGlance]. <br>
+<table><tr><td colspan='2'>[[5myg]] is a 4 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=5MYG OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5MYG FirstGlance]. <br>
-</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=LS8:4-cyano-~{N}-(1,3-dimethyl-2-oxidanylidene-quinolin-6-yl)-2-methoxy-benzenesulfonamide'>LS8</scene></td></tr>
+</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.3&#8491;</td></tr>
-<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://proteopedia.org/fgij/fg.htm?mol=5myg FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5myg OCA], [http://pdbe.org/5myg PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5myg RCSB], [http://www.ebi.ac.uk/pdbsum/5myg PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5myg ProSAT]</span></td></tr>
+<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=LS8:4-cyano-~{N}-(1,3-dimethyl-2-oxidanylidene-quinolin-6-yl)-2-methoxy-benzenesulfonamide'>LS8</scene></td></tr>
+<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=5myg FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5myg OCA], [https://pdbe.org/5myg PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5myg RCSB], [https://www.ebi.ac.uk/pdbsum/5myg PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5myg ProSAT]</span></td></tr>
 </table>
 == Function ==
-[[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>
+[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>
 <div style="background-color:#fffaf0;">
 == Publication Abstract from PubMed ==
@@ Line 25: / Line 26: @@
 __TOC__
 </StructureSection>
+[[Category: Homo sapiens]]
 [[Category: Large Structures]]
-[[Category: Arrowsmith, C H]]
+[[Category: Arrowsmith CH]]
-[[Category: Bayle, E D]]
+[[Category: Bayle ED]]
-[[Category: Bountra, C]]
+[[Category: Bountra C]]
-[[Category: Brennan, P E]]
+[[Category: Brennan PE]]
-[[Category: Delft, F von]]
+[[Category: Edwards AM]]
-[[Category: Edwards, A M]]
+[[Category: Fedorov O]]
-[[Category: Fedorov, O]]
+[[Category: Fish P]]
-[[Category: Fish, P]]
+[[Category: Fitzpatrick F]]
-[[Category: Fitzpatrick, F]]
+[[Category: Igoe N]]
-[[Category: Igoe, N]]
+[[Category: Knapp S]]
-[[Category: Knapp, S]]
+[[Category: Kopec J]]
-[[Category: Kopec, J]]
+[[Category: Krojer T]]
-[[Category: Krojer, T]]
+[[Category: Muller S]]
-[[Category: Muller, S]]
+[[Category: Nunez-Alonso G]]
-[[Category: Nunez-Alonso, G]]
+[[Category: Savitsky P]]
-[[Category: Structural genomic]]
+[[Category: Tallant C]]
-[[Category: Savitsky, P]]
+[[Category: Von Delft F]]
-[[Category: Tallant, C]]
-[[Category: Sgc]]
-[[Category: Transcription]]

5myg

From Proteopedia

Current revision

Crystal structure of the bromodomain of human BRPF1 in complex with NI-57 chemical probe

Structural highlights

Function

Publication Abstract from PubMed

See Also

References

Contents

Proteopedia Page Contributors and Editors (what is this?)

Views

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