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| <StructureSection load='4bw2' size='340' side='right' caption='Human bromodomain-containing protein 4 bromodomain 1 complex with inhibitor (PDB code [[4bw2]])' scene=''> | | <StructureSection load='3p5o' size='340' side='right' caption='Human bromodomain-containing protein 4 bromodomain 1 complex with inhibitor (PDB code [[4bw2]])' scene=''> |
| == Function == | | == Function == |
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Revision as of 12:58, 10 February 2016
FunctionBromodomain-containing proteins (BRD) are active as histone acetyltransferase, chromatin remodeling and transcriptional mediation. The bromodomain is a ca. 110 amino acid long sequence which recognizes acetylated lysine residues which are found in the C-terminal of histones[1].
For detalis on BRD3 see Human bromodomain containing protein 3
DiseaseDysfunction of BRD is involved in cancer, inflammation, obesity and multiple sclerosis[2]. BRD4 translocations are detected in NUT midline carcinoma and a variety of BRD4 inhibitors are clinically tested at the present[3].
Structural highlights | |
3D Structures of bromodomain-containing protein3D Structures of bromodomain-containing protein
Updated on 10-February-2016
{"openlevels":0}
- Bromodomain-containing protein 1
- 3lyi – hBRD1 PWWP domain - human
- 2ku3 – hBRD1 PHD1 zinc finger domain - NMR
- 2lq6 – hBRD1 PHD2 zinc finger domain (mutant) - NMR
- 3l43 – histone H3.3 N-terminal/hBRD1 PHD1 zinc finger domain - NMR
- 3rcw – hBRD1 bromodomain
- 5ame – hBRD1 bromodomain+PHD (mutant) + piperazine derivative
- 5amf – hBRD1 bromodomain+PHD (mutant) + indazole derivative
- 5fg6 – hBRD1 bromodomain+PHD + probe
- 4z02 – hBRD1 residues 925-1049 + quinoline derivative
- Bromodomain-containing protein 2
- 1x0j, 2dvv – hBRD2 N-terminal bromodomain
- 5hel, 5hem, 5hen, 5hfq – hBRD2 N-terminal bromodomain (mutant)
- 2g4a – hBRD2 residues 1-116 - NMR
- 4qeu, 5dfb – hBRD2 bromodomain 2 (mutant)
- Bromodomain-containing protein 2 complex
- 2dvq, 2dvr, 2dvs, 2e3k – hBRD2 N-terminal bromodomain + histone H4 peptide
- 3oni – hBRD2 residues 224-335 + inhibitor
- 3aqa, 2ydw, 2yek, 4a9e, 4a9f, 4a9h, 4a9i, 4a9j, 4a9m, 4a9n, 4a9o, 4alh, 4akn, 4alg, 4uyf, 4uyg, 4uyh – hBRD2 N-terminal bromodomain + inhibitor
- 4mr5, 4mr6, 4j1p – hBRD2 bromodomain 2 + inhibitor
- 5bt5 – hBRD2 bromodomain 2 + probe
- 4qev, 4qew – hBRD2 bromodomain 2 (mutant) + probe
- 5dfc, 5dfd – hBRD2 bromodomain 2 (mutant) + ligand
- Bromodomain-containing protein 3
- 2nxb – hBRD3 bromodomain 1
- 2yw5 – hBRD3 bromodomain 1 - NMR
- 3s91, 3s92 – hBRD3 bromodomain 1 + inhibitor
- 2l5e – mBRD3 bromodomain 1 + GATA-1 C-terminal – mouse - NMR
- 2oo1 – hBRD3 bromodomain 2
- 2e7n – hBRD3 bromodomain 2 - NMR
- 5hfr – hBRD3 bromodomain 2 (mutant)
- Bromodomain-containing protein 4
- Bromodomain-containing protein 4 bromodomain 1 complex
- 3jvk, 3muk, 3mul – mBRD4 bromodomain 1 + histone H3.3 peptide
- 3uvw, 3uvy, 3uvx, 3uw9 – hBRD4 bromodomain 1 + histone H4 peptide
- 4kv1 – hBRD4 bromodomain 1 + Rel peptide
- 3mxf – mBRD4 bromodomain 1 + inhibitor
- 3p5o, 2yel, 3zyu, 3u5j, 3u5k, 4a9l, 4e96, 4f3i, 4hxk, 4hxl, 4hxm, 4hxn, 4hxo, 4hxp, 4hxr, 4hxs, 4lr6, 4lrg, 3svf, 3svg, 4gpj, 4hbv, 4hbw, 4hbx, 4hby, 4don, 4j0r, 4j0s, 4bw1, 4bw2, 4bw3, 4bw4, 4men, 4meo, 4mep, 4meq, 4bjx, 4c66, 4c67, 4ioo, 4ioq, 4ior, 4mr3, 4mr4, 4nqm, 4nr8, 4cfk, 4cfl, 4lyw, 4ogi, 4ogj, 4o70, 4o71, 4o72, 4o74, 4o75, 4o76, 4o77, 4o78, 4o7a, 4o7b, 4o7c, 4o7e, 4o7f, 4ps5, 4nuc, 4nue, 4nud, 4pce, 4pci, 4uyd, 4qzs, 4wiv, 4cl9, 4clb, 4xy9, 4xya, 4z1q, 4z1s, 4uix, 4uiy, 4uiz, 4qr3, 4qr4, 4qr5, 5bt4, 5a5s, 5a85, 5acy, 4x2i, 4zc9, 5fbx, 4yh3, 4yh4, 5coi, 5cp5, 5cpe, 5cqt, 5crm, 5crz, 5cs8, 5ctl, 5cy9, 5d0c, 5dx4, 4lzs, 5d24, 5d25, 5d26, 5d3h, 5d3j, 5d3l, 5d3n, 5d3p, 5d3r, 5d3s, 5d3t, 5egu, 5ei4, 5eis, 5hls, 5hm0 – hBRD4 bromodomain 1 + inhibitor
- 4lys, 4lzr – hBRD4 bromodomain 1 + colchiceine
- 4qb3 – hBRD4 bromodomain 1 + olinone
- 4whw – hBRD4 bromodomain 1 + probe
- Bromodomain-containing protein 4 bromodomain 2 complex
- 2yem, 4z93 – hBRD4 bromodomain 2 + inhibitor
- 2lsp – hBRD4 bromodomain 2 + Nf-Kb peptide
- 4kv4 – hBRD4 bromodomain 2 + Rel peptide
- 2mjv – hBRD4 bromodomain 2 + Twist peptide
- Bromodomain-containing protein 9
- 3hme – hBRD9 bromodomain
- 4nqn, 4xy8, 4z6h, 4z6i, 5e9v – hBRD9 bromodomain + inhibitor
- 4yy4 – hBRD9 bromodomain + DMSO
- 4yy6, 4yyd, 4yyg, 4yyh, 4yyj, 4yyk – hBRD9 bromodomain + histone H4 peptide
- 4uit, 4uiu, 4uiv, 4uiw – hBRD9 N-terminal bromodomain + inhibitor
ReferencesReferences
- ↑ Zeng L, Zhou MM. Bromodomain: an acetyl-lysine binding domain. FEBS Lett. 2002 Feb 20;513(1):124-8. PMID:11911891
- ↑ Belkina AC, Denis GV. BET domain co-regulators in obesity, inflammation and cancer. Nat Rev Cancer. 2012 Jun 22;12(7):465-77. doi: 10.1038/nrc3256. PMID:22722403 doi:http://dx.doi.org/10.1038/nrc3256
- ↑ French CA. Demystified molecular pathology of NUT midline carcinomas. J Clin Pathol. 2010 Jun;63(6):492-6. doi: 10.1136/jcp.2007.052902. Epub 2008 Jun , 13. PMID:18552174 doi:http://dx.doi.org/10.1136/jcp.2007.052902
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