4lyw: Difference between revisions

Revision as of 07:14, 5 August 2016

Crystal Structure of BRD4(1) bound to inhibitor XD14

Structural highlights

4lyw 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:	21Q
Related:	4lyi, 4lys, 4lzr, 4lzs
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

Bromodomains are acetyllysine epigenetic mark reader proteins. Small molecules inhibiting them have potential as anti-inflammatory, antiviral, and anticancer agents. A 4-acyl pyrrole derivative (see yellow structure in recognition pocket) has been identified that potently inhibits specific bromodomains and exhibits antiproliferative activity against leukemia cell lines.

4-acyl pyrroles: mimicking acetylated lysines in histone code reading.,Lucas X, Wohlwend D, Hugle M, Schmidtkunz K, Gerhardt S, Schule R, Jung M, Einsle O, Gunther S Angew Chem Int Ed Engl. 2013 Dec 23;52(52):14055-9. doi: 10.1002/anie.201307652. , Epub 2013 Nov 24. PMID:24272870^[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
↑ Lucas X, Wohlwend D, Hugle M, Schmidtkunz K, Gerhardt S, Schule R, Jung M, Einsle O, Gunther S. 4-acyl pyrroles: mimicking acetylated lysines in histone code reading. Angew Chem Int Ed Engl. 2013 Dec 23;52(52):14055-9. doi: 10.1002/anie.201307652. , Epub 2013 Nov 24. PMID:24272870 doi:https://dx.doi.org/10.1002/anie.201307652

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OCA

[1] 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

[2] 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

[3] Lucas X, Wohlwend D, Hugle M, Schmidtkunz K, Gerhardt S, Schule R, Jung M, Einsle O, Gunther S. 4-acyl pyrroles: mimicking acetylated lysines in histone code reading. Angew Chem Int Ed Engl. 2013 Dec 23;52(52):14055-9. doi: 10.1002/anie.201307652. , Epub 2013 Nov 24. PMID:24272870 doi:https://dx.doi.org/10.1002/anie.201307652

[1]

[2]

[3]

@@ Line 1: / Line 1: @@
 ==Crystal Structure of BRD4(1) bound to inhibitor XD14==
 <StructureSection load='4lyw' size='340' side='right' caption='[[4lyw]], [[Resolution|resolution]] 1.95&Aring;' scene=''>
@@ Line 6: / Line 7: @@
 <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4lyi|4lyi]], [[4lys|4lys]], [[4lzr|4lzr]], [[4lzs|4lzs]]</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://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4lyw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4lyw OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4lyw RCSB], [http://www.ebi.ac.uk/pdbsum/4lyw PDBsum]</span></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=4lyw FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4lyw OCA], [http://pdbe.org/4lyw PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4lyw RCSB], [http://www.ebi.ac.uk/pdbsum/4lyw PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4lyw ProSAT]</span></td></tr>
 </table>
 == Disease ==
@@ Line 20: / Line 21: @@
 From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
 </div>
+<div class="pdbe-citations 4lyw" style="background-color:#fffaf0;"></div>
+==See Also==
+*[[Bromodomain-containing protein|Bromodomain-containing protein]]
 == References ==
 <references/>

4lyw: Difference between revisions

Revision as of 07:14, 5 August 2016

Crystal Structure of BRD4(1) bound to inhibitor XD14

Structural highlights

Disease

Function

Publication Abstract from PubMed

See Also

References

Contents

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