Bromodomain-containing protein

From Proteopedia

Revision as of 10:02, 3 April 2018

spinqualitylabelsall models Human bromodomain-containing protein 4 bromodomain 1 complex with inhibitor and ethylene glycol (PDB code 3p5o) Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image Function Bromodomain-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 Disease Dysfunction 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 [4].

3D Structures of bromodomain-containing protein

Updated on 03-April-2018 {{#tree:id=OrganizedByTopic|openlevels=0|

• Bromodomain-containing protein 1

• • 3lyi – hBRD1 PWWP domain residues 925-1049 - human
    
  • 2ku3 – hBRD1 PHD1 zinc finger domain residues 208-269 - NMR
    
  • 2lq6 – hBRD1 PHD2 zinc finger domain residues 317-394 (mutant) - NMR
    
  • 3l43 – histone H3.3 N-terminal/hBRD1 PHD1 zinc finger domain - NMR
    
  • 3rcw, 4z02 – hBRD1 bromodomain residues 555-688
    
  • 5pwb, 5pwa, 5pw9, 5pw8, 5pw7, 5pw6, 5pw5, 5pw4, 5pw3, 5pw2, 5pw1, 5pw0, 5pvz, 5pvy, 5pvx, 5pvw, 5pvv, 5pvu, 5pvt, 5pvs, 5pvr, 5pvq, 5pvp, 5pvo, 5pvn, 5pvm, 5pvl, 5pvk, 5pvj, 5pvi, 5pvh, 5pvg, 5pvf, 5pve, 5pvd, 5pvc, 5pvb, 5pva, 5pv9, 5pv8, 5pv7, 5pv6, 5pv5, 5pv4, 5pv3, 5pv2, 5pv1, 5pv0, 5puz, 5puy, 5pux, 5puw, 5puv, 5puu, 5put, 5pus, 5pur, 5puq, 5pup, 5pun, 5pum, 5puo, 5pul, 5puk, 5puj, 5pui, 5puh, 5pug, 5puf, 5pue, 5pud, 5puc, 5pub, 5pua, 5pu9, 5pu8, 5pu7, 5pu6, 5pu5, 5pu4, 5pu3, 5pu2, 5pu1, 5pu0, 5ptz, 5pty, 5ptx, 5ptw, 5ptv, 5ptu, 5pts, 5ptt, 5ptr, 5ptq, 5ptp, 5pto, 5ptn, 5ptm, 5ptl, 5ptk, 5ptj, 5pth, 5ptg, 5ptf, 5pte, 5ptd, 5ptc, 5ptb, 5pta, 5pt9, 5pt8, 5pt7 – 5pnx – hBRD1 bromodomain (mutant)
    
  • 5n49 – hBRD1 bromodomain + inhibitor
    
  • 5ame – hBRD1 bromodomain+PHD (mutant) + piperazine derivative
    
  • 5amf – hBRD1 bromodomain+PHD (mutant) + indazole derivative
    
  • 5fg6 – hBRD1 bromodomain+PHD + probe
    
  • 4z02 – hBRD1 PWWP domain + quinoline derivative
    

• Bromodomain-containing protein 2

• • 1x0j, 2dvv – hBRD2 bromodomain 1
    
  • 5hel, 5hem, 5hen, 5hfq – hBRD2 bromodomain 1 (mutant)
    
  • 2g4a – hBRD2 residues 1-116 - NMR
    
  • 5ibn – hBRD2 bromodomain 2
    
  • 4qeu, 5dfb – hBRD2 bromodomain 2 (mutant)
    

• Bromodomain-containing protein 2 complex

• • 2dvq, 2dvr, 2dvs, 2e3k – hBRD2 bromodomain 1 + 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, 5ig6, 5ek9, 5dw1, 5xhk, 5xhe, 5u6v, 5n2l – hBRD2 bromodomain 2 + inhibitor
    
  • 5o3i, 5o3h, 5o3g, 5o3f, 5o3e, 5o3d, 5o3c, 5o3b, 5o3a, 5o39, 5o38 – hBRD2 bromodomain 2 (mutant) + inhibitor
    
  • 5u5s – hBRD2 bromodomain 2 + STAT3 peptide - NMR
    
  • 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)
    
  • 5hjc – hBRD3 bromodomain 2+ histone H3.1 peptide
    
  • 5a7c – hBRD3 bromodomain 2 + inhibitor
    
  • 6bgh – hBRD3 ET domain + BRG1 peptide - NMR
    
  • 6bgg – hBRD3 ET domain + CHD4 peptide - NMR
    

• Bromodomain-containing protein 4

• • 2oss, 4j3i, 4lyi, 5hq7, 5hq6, 5hq5 – hBRD4 bromodomain 1
    
  • 2ouo – hBRD4 bromodomain 2
    
  • 2i8n – hBRD4 bromodomain 2 - NMR
    
  • 6bnh – hBRD4 ET domain + JMJD6 peptide - NMR
    
  • 3jvj – mBRD4 bromodomain 1
    
  • 2dww, 3jvl, 3jvm – mBRD4 bromodomain 2
    
  • 2jns – mBRD4 ET domain - NMR
    

• 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, 3u5l, 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, 5ku3, 5khm, 5i88, 5i80, 5f63, 5f62, 5f61, 5f60, 5e0r, 5dw2, 5dlz, 5dlx, 5cfw, 5ad3, 5ad2, 4zw1, 5u2f, 5u2e, 5u28, 5luu, 5lj2, 5lj1, 5y1y, 5wuu, 5vom, 5v67, 5uvw, 5ula, 5ti7, 5n2m, [[5mli], 5mkz], 5m3a, 5m39, 5lrq, 5kj0, 5kdh, 5h21, [[5f5z] – hBRD4 bromodomain 1 + inhibitor
    
  • 5z9c – hBRD4 bromodomain 1 + inhibitor - NMR
    
  • 5ti6, 5ti5, 5ti4, 5ti3, 5ti2 – hBRD4 bromodomain 1 (mutant) + inhibitor
    
  • 4lys, 4lzr – hBRD4 bromodomain 1 + colchiceine
    
  • 4qb3 – hBRD4 bromodomain 1 + olinone
    
  • 4whw – hBRD4 bromodomain 1 + probe
    
  • 5igk – hBRD4 bromodomain 1 + bromosporine
    
  • 5hcl – hBRD4 bromodomain 1 + drug
    

• Bromodomain-containing protein 4 bromodomain 2 complex

• • 2yem, 4z93, 5u2c, 5jwm, 5uvz, 5uvy, 5uvx, 5uvv, 5uvu, 5uvt, 5uvs, 5uoo, 5uf0, 5uez, 5uey, 5uex, 5uew, 5uev, 5ueu, 5uet, 5ues, 5uer, 5ueq, 5uep, 5ueo – hBRD4 bromodomain 2 + inhibitor
    
  • 2lsp – hBRD4 bromodomain 2 + Nf-Kb peptide
    
  • 4kv4 – hBRD4 bromodomain 2 + Rel peptide
    
  • 2mjv – hBRD4 bromodomain 2 + Twist peptide
    
  • 5t35 – hBRD4 bromodomain 2 + ELOB + ELOC + PVHL peptide
    

• Bromodomain-containing protein 7

• • 5mq1 – hBRD7 bromodomain + inhibitor
    

• Bromodomain-containing protein 9

• • 3hme – hBRD9 bromodomain
    
  • 5ji8 – hBRD9 JUS-SPRY domain
    
  • 5ign – hBRD9 bromodomain + L999
    
  • 5igm – hBRD9 bromodomain + bromosporine
    
  • 4nqn, 4xy8, 4z6h, 4z6i, 5e9v, 5f2p, 5f25, 5f1l, 5f1h, 5eu1, 5mky – hBRD9 bromodomain + inhibitor
    
  • 4yy4 – hBRD9 bromodomain + DMSO
    
  • 4yy6, 4yyd, 4yyg, 4yyh, 4yyj, 4yyk, 4yyi – hBRD9 bromodomain + histone H4 peptide
    
  • 4uit, 4uiu, 4uiv, 4uiw – hBRD9 JUS-SPRY domain + inhibitor
    
  • 5i7y, 5i7x, 5i40 – hBRD9 JUS-SPRY domain + inhibitor
    
  • 5twx – hBRD9 bromodomain residues 134-250 + heterobifunctional ligand
    

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References

1. ↑ Zeng L, Zhou MM. Bromodomain: an acetyl-lysine binding domain. FEBS Lett. 2002 Feb 20;513(1):124-8. PMID:11911891
2. ↑ 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
3. ↑ 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
4. ↑ 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