This old version of Proteopedia is provided for student assignments while the new version is undergoing repairs. Content and edits done in this old version of Proteopedia after March 1, 2026 will eventually be lost when it is retired in about June of 2026.

Apply for new accounts at the new Proteopedia. Your logins will work in both the old and new versions.

5lj2

From Proteopedia

(Difference between revisions)

Jump to: navigation, search

Revision as of 10:39, 12 August 2020

N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH 5-(5-aminopyridin-3-yl)-8-(((3R,4R)-3-((1,1-dioxidotetrahydro-2H-thiopyran-4-yl)methoxy)piperidin-4-yl)amino)-3-methyl-1,7-naphthyridin-2(1H)-one

Structural highlights

5lj2 is a 1 chain structure with sequence from Human. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:	,
Gene:	BRD4, HUNK1 (HUMAN)
Resources:	FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Disease

[BRD4_HUMAN] Note=A chromosomal aberration involving BRD4 is found in a rare, aggressive, and lethal carcinoma arising in midline organs of young people. Translocation t(15;19)(q14;p13) with NUT which produces a BRD4-NUT fusion protein.^[1] ^[2]

Function

[BRD4_HUMAN] Plays a role in a process governing chromosomal dynamics during mitosis (By similarity).

Publication Abstract from PubMed

ATAD2 is a cancer-associated protein whose bromodomain has been described as among the least druggable of that target class. Starting from a potent lead, permeability and selectivity were improved through a dual approach: 1) using CF2 as a sulfone bio-isostere to exploit the unique properties of fluorine, and 2) using 1,3-interactions to control the conformation of a piperidine ring. This resulted in the first reported low-nanomolar, selective and cell permeable chemical probe for ATAD2.

A Chemical Probe for the ATAD2 Bromodomain.,Bamborough P, Chung CW, Demont EH, Furze RC, Bannister AJ, Che KH, Diallo H, Douault C, Grandi P, Kouzarides T, Michon AM, Mitchell DJ, Prinjha RK, Rau C, Robson S, Sheppard RJ, Upton R, Watson RJ Angew Chem Int Ed Engl. 2016 Sep 12;55(38):11382-6. doi: 10.1002/anie.201603928. , Epub 2016 Aug 17. PMID:27530368^[3]

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

References

↑ French CA, Miyoshi I, Kubonishi I, Grier HE, Perez-Atayde AR, Fletcher JA. BRD4-NUT fusion oncogene: a novel mechanism in aggressive carcinoma. Cancer Res. 2003 Jan 15;63(2):304-7. PMID:12543779
↑ French CA, Miyoshi I, Aster JC, Kubonishi I, Kroll TG, Dal Cin P, Vargas SO, Perez-Atayde AR, Fletcher JA. BRD4 bromodomain gene rearrangement in aggressive carcinoma with translocation t(15;19). Am J Pathol. 2001 Dec;159(6):1987-92. PMID:11733348 doi:10.1016/S0002-9440(10)63049-0
↑ Bamborough P, Chung CW, Demont EH, Furze RC, Bannister AJ, Che KH, Diallo H, Douault C, Grandi P, Kouzarides T, Michon AM, Mitchell DJ, Prinjha RK, Rau C, Robson S, Sheppard RJ, Upton R, Watson RJ. A Chemical Probe for the ATAD2 Bromodomain. Angew Chem Int Ed Engl. 2016 Sep 12;55(38):11382-6. doi: 10.1002/anie.201603928. , Epub 2016 Aug 17. PMID:27530368 doi:http://dx.doi.org/10.1002/anie.201603928

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

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/5lj2"

@@ Line 1: / Line 1: @@
 ==N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH 5-(5-aminopyridin-3-yl)-8-(((3R,4R)-3-((1,1-dioxidotetrahydro-2H-thiopyran-4-yl)methoxy)piperidin-4-yl)amino)-3-methyl-1,7-naphthyridin-2(1H)-one==
-<StructureSection load='5lj2' size='340' side='right' caption='[[5lj2]], [[Resolution|resolution]] 1.19&Aring;' scene=''>
+<StructureSection load='5lj2' size='340' side='right'caption='[[5lj2]], [[Resolution|resolution]] 1.19&Aring;' scene=''>
 == Structural highlights ==
-<table><tr><td colspan='2'>[[5lj2]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5LJ2 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=5LJ2 FirstGlance]. <br>
+<table><tr><td colspan='2'>[[5lj2]] 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=5LJ2 OCA]. For a <b>guided tour on the structure components</b> use [http://proteopedia.org/fgij/fg.htm?mol=5LJ2 FirstGlance]. <br>
-</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=6XW:5-(5-AMINOPYRIDIN-3-YL)-8-(((3R,4R)-3-((1,1-DIOXIDOTETRAHYDRO-2H-THIOPYRAN-4-YL)METHOXY)PIPERIDIN-4-YL)AMINO)-3-METHYL-1,7-NAPHTHYRIDIN-2(1H)-ONE'>6XW</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene></td></tr>
+</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=6XW:5-(5-AMINOPYRIDIN-3-YL)-8-(((3R,4R)-3-((1,1-DIOXIDOTETRAHYDRO-2H-THIOPYRAN-4-YL)METHOXY)PIPERIDIN-4-YL)AMINO)-3-METHYL-1,7-NAPHTHYRIDIN-2(1H)-ONE'>6XW</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene></td></tr>
-<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=5lj2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5lj2 OCA], [http://pdbe.org/5lj2 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5lj2 RCSB], [http://www.ebi.ac.uk/pdbsum/5lj2 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5lj2 ProSAT]</span></td></tr>
+<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">BRD4, HUNK1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</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=5lj2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5lj2 OCA], [http://pdbe.org/5lj2 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=5lj2 RCSB], [http://www.ebi.ac.uk/pdbsum/5lj2 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=5lj2 ProSAT]</span></td></tr>
 </table>
 == Disease ==
@@ Line 20: / Line 21: @@
 </div>
 <div class="pdbe-citations 5lj2" style="background-color:#fffaf0;"></div>
+==See Also==
+*[[ATPase family AAA domain-containing protein|ATPase family AAA domain-containing protein]]
+*[[Bromodomain-containing protein 3D structures|Bromodomain-containing protein 3D structures]]
 == References ==
 <references/>
 __TOC__
 </StructureSection>
+[[Category: Human]]
+[[Category: Large Structures]]
 [[Category: Bamborough, P]]
 [[Category: Chung, C]]

5lj2

From Proteopedia

Revision as of 10:39, 12 August 2020

N-TERMINAL BROMODOMAIN OF HUMAN BRD4 WITH 5-(5-aminopyridin-3-yl)-8-(((3R,4R)-3-((1,1-dioxidotetrahydro-2H-thiopyran-4-yl)methoxy)piperidin-4-yl)amino)-3-methyl-1,7-naphthyridin-2(1H)-one

Structural highlights

Disease

Function

Publication Abstract from PubMed

See Also

References

Contents

Proteopedia Page Contributors and Editors (what is this?)

Views

Personal tools

Navigation

Search

Toolbox