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PDBsum entry 3p5o
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protein ligands links
Signaling protein/inhibitor PDB id
3p5o

 

 

 

 

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Contents
Protein chain
127 a.a. *
Ligands
EAM
EDO ×4
Waters ×264
* Residue conservation analysis
PDB id:
3p5o
Name: Signaling protein/inhibitor
Title: Crystal structure of the first bromodomain of human brd4 in complex with ibet inhibitor
Structure: Bromodomain-containing protein 4. Chain: a. Fragment: bromo domain 1, unp residues 44-168. Synonym: protein hunk1. Engineered: yes
Source: Homo sapiens. Human. Organism_taxid: 9606. Gene: brd4, hunk1. Expressed in: escherichia coli. Expression_system_taxid: 562.
Resolution:
1.60Å     R-factor:   0.157     R-free:   0.185
Authors: C.Chung
Key ref: E.Nicodeme et al. (2010). Suppression of inflammation by a synthetic histone mimic. Nature, 468, 1119-1123. PubMed id: 21068722
Date:
09-Oct-10     Release date:   17-Nov-10    
PROCHECK
Go to PROCHECK summary
 Headers
 References

Protein chain
Pfam   ArchSchema ?
O60885  (BRD4_HUMAN) -  Bromodomain-containing protein 4 from Homo sapiens
Seq:
Struc: 		 
Seq:
Struc: 		 
Seq:
Struc: 		1362 a.a.
127 a.a.*
Key:    PfamA domain  Secondary structure  CATH domain
* PDB and UniProt seqs differ at 1 residue position (black cross)

 Enzyme reactions 
   Enzyme class: E.C.?
[IntEnz]   [ExPASy]   [KEGG]   [BRENDA]

 

 
Nature 468:1119-1123 (2010)
PubMed id: 21068722  
 
 
Suppression of inflammation by a synthetic histone mimic.
E.Nicodeme, K.L.Jeffrey, U.Schaefer, S.Beinke, S.Dewell, C.W.Chung, R.Chandwani, I.Marazzi, P.Wilson, H.Coste, J.White, J.Kirilovsky, C.M.Rice, J.M.Lora, R.K.Prinjha, K.Lee, A.Tarakhovsky.
 
  ABSTRACT  
 
No abstract given.

 

Literature references that cite this PDB file's key reference

  PubMed id Reference
22722403 A.C.Belkina, and G.V.Denis (2012).
BET domain co-regulators in obesity, inflammation and cancer.
  Nat Rev Cancer, 12, 465-477.  
22498752 C.H.Arrowsmith, C.Bountra, P.V.Fish, K.Lee, and M.Schapira (2012).
Epigenetic protein families: a new frontier for drug discovery.
  Nat Rev Drug Discov, 11, 384-400.  
22419161 I.Marazzi, J.S.Ho, J.Kim, B.Manicassamy, S.Dewell, R.A.Albrecht, C.W.Seibert, U.Schaefer, K.L.Jeffrey, R.K.Prinjha, K.Lee, A.García-Sastre, R.G.Roeder, and A.Tarakhovsky (2012).
Suppression of the antiviral response by an influenza histone mimic.
  Nature, 483, 428-433.  
21358755 D.C.Hargreaves, and G.R.Crabtree (2011).
ATP-dependent chromatin remodeling: genetics, genomics and mechanisms.
  Cell Res, 21, 396-420.  
21814200 J.Zuber, J.Shi, E.Wang, A.R.Rappaport, H.Herrmann, E.A.Sison, D.Magoon, J.Qi, K.Blatt, M.Wunderlich, M.J.Taylor, C.Johns, A.Chicas, J.C.Mulloy, S.C.Kogan, P.Brown, P.Valent, J.E.Bradner, S.W.Lowe, and C.R.Vakoc (2011).
RNAi screen identifies Brd4 as a therapeutic target in acute myeloid leukaemia.
  Nature, 478, 524-528.  
21964340 M.A.Dawson, R.K.Prinjha, A.Dittmann, G.Giotopoulos, M.Bantscheff, W.I.Chan, S.C.Robson, C.W.Chung, C.Hopf, M.M.Savitski, C.Huthmacher, E.Gudgin, D.Lugo, S.Beinke, T.D.Chapman, E.J.Roberts, P.E.Soden, K.R.Auger, O.Mirguet, K.Doehner, R.Delwel, A.K.Burnett, P.Jeffrey, G.Drewes, K.Lee, B.J.Huntly, and T.Kouzarides (2011).
Inhibition of BET recruitment to chromatin as an effective treatment for MLL-fusion leukaemia.
  Nature, 478, 529-533.
PDB code: 3zyu
21366500 T.D.Heightman (2011).
Therapeutic prospects for epigenetic modulation.
  Expert Opin Ther Targets, 15, 729-740.  
21179160 S.D.Taverna, and P.A.Cole (2010).
Drug discovery: Reader's block.
  Nature, 468, 1050-1051.  
The most recent references are shown first. Citation data come partly from CiteXplore and partly from an automated harvesting procedure. Note that this is likely to be only a partial list as not all journals are covered by either method. However, we are continually building up the citation data so more and more references will be included with time. Where a reference describes a PDB structure, the PDB code is shown on the right.

 

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