spacer
spacer

PDBsum entry 2yek
Go to PDB code: 
protein ligands Protein-protein interface(s) links
Signaling protein PDB id
2yek

 

 

 

 

Loading ...

 
JSmol PyMol  
Contents
Protein chains
114 a.a.
107 a.a.
Ligands
EAM ×3
SO4
Waters ×397
PDB id:
2yek
Name: Signaling protein
Title: Crystal structure of the first bromodomain of human brd2 with the inhibitor gsk525762 (ibet)
Structure: Bromodomain-containing protein 2. Chain: a, b, c. Fragment: n-terminal bromodomain, residues 67-200. Synonym: o27.1.1, really interesting new gene 3 protein, human brd2. Engineered: yes
Source: Homo sapiens. Organism_taxid: 9606. Expressed in: escherichia coli. Expression_system_taxid: 562
Resolution:
1.98Å     R-factor:   0.158     R-free:   0.201
Authors: C.W.Chung
Key ref: C.W.Chung et al. (2011). Discovery and characterization of small molecule inhibitors of the BET family bromodomains. J Med Chem, 54, 3827-3838. PubMed id: 21568322
Date:
25-Mar-11     Release date:   15-Jun-11    
PROCHECK
Go to PROCHECK summary
 Headers
 References

Protein chain
Pfam   ArchSchema ?
P25440  (BRD2_HUMAN) -  Bromodomain-containing protein 2 from Homo sapiens
Seq:
Struc: 		 
Seq:
Struc: 		801 a.a.
114 a.a.
Protein chains
Pfam   ArchSchema ?
P25440  (BRD2_HUMAN) -  Bromodomain-containing protein 2 from Homo sapiens
Seq:
Struc: 		 
Seq:
Struc: 		801 a.a.
107 a.a.
Key:    PfamA domain  Secondary structure  CATH domain

 Enzyme reactions 
   Enzyme class: Chains A, B, C: E.C.?
[IntEnz]   [ExPASy]   [KEGG]   [BRENDA]

 

 
J Med Chem 54:3827-3838 (2011)
PubMed id: 21568322  
 
 
Discovery and characterization of small molecule inhibitors of the BET family bromodomains.
C.W.Chung, H.Coste, J.H.White, O.Mirguet, J.Wilde, R.L.Gosmini, C.Delves, S.M.Magny, R.Woodward, S.A.Hughes, E.V.Boursier, H.Flynn, A.M.Bouillot, P.Bamborough, J.M.Brusq, F.J.Gellibert, E.J.Jones, A.M.Riou, P.Homes, S.L.Martin, I.J.Uings, J.Toum, C.A.Clement, A.B.Boullay, R.L.Grimley, F.M.Blandel, R.K.Prinjha, K.Lee, J.Kirilovsky, E.Nicodeme.
 
  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.  
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
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.

 

spacer
spacer