 |
PDBsum entry 3mxf
|
|
|
|
|
 |
Contents |
 |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
* Residue conservation analysis
|
|
|
|
|
|
PDB id:
|
|
|
|
| Name: |
|
Cell cycle
|
|
|
Title:
|
|
Crystal structure of the first bromodomain of human brd4 in complex with the inhibitor jq1
|
|
Structure:
|
|
Bromodomain-containing protein 4. Chain: a. Synonym: protein hunk1. Engineered: yes
|
|
Source:
|
|
Homo sapiens. Human. Organism_taxid: 9606. Gene: brd4, hunk1, mcap. Expressed in: escherichia coli. Expression_system_taxid: 469008.
|
|
Resolution:
|
|
|
1.60Å
|
R-factor:
|
0.151
|
R-free:
|
0.184
|
|
|
Authors:
|
|
P.Filippakopoulos,S.Picaud,J.Qi,T.Keates,I.Felletar,O.Fedorov, J.Muniz,F.Von Delft,C.H.Arrowsmith,A.M.Edwards,J.Weigelt,C.Bountra, J.E.Bradner,S.Knapp,Structural Genomics Consortium (Sgc)
|
|
Key ref:
|
|
P.Filippakopoulos
et al.
(2010).
Selective inhibition of BET bromodomains.
Nature,
468,
1067-1073.
PubMed id:
|
|
|
Date:
|
|
|
07-May-10
|
Release date:
|
06-Oct-10
|
|
|
|
|
|
|
PROCHECK
|
|
|
|
|
|
Headers
|
|
|
|
References
|
|
|
|
|
|
|
|
O60885
(BRD4_HUMAN) -
Bromodomain-containing protein 4 from Homo sapiens
|
|
|
|
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)
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
 |
|
|
|
|
|
|
| |
|
|
Nature
468:1067-1073
(2010)
|
|
PubMed id:
|
|
|
|
|
|
| |
|
Selective inhibition of BET bromodomains.
|
|
P.Filippakopoulos,
J.Qi,
S.Picaud,
Y.Shen,
W.B.Smith,
O.Fedorov,
E.M.Morse,
T.Keates,
T.T.Hickman,
I.Felletar,
M.Philpott,
S.Munro,
M.R.McKeown,
Y.Wang,
A.L.Christie,
N.West,
M.J.Cameron,
B.Schwartz,
T.D.Heightman,
N.La Thangue,
C.A.French,
O.Wiest,
A.L.Kung,
S.Knapp,
J.E.Bradner.
|
|
|
|
|
| |
ABSTRACT
|
|
|
|
| |
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
 |
 |
 |
|
Literature references that cite this PDB file's key reference
|
|
|
| |
PubMed id
|
|
Reference
|
|
|
|
|
|
Y.Yang,
and
M.T.Bedford
(2013).
Protein arginine methyltransferases and cancer.
|
| |
Nat Rev Cancer,
13,
37-50.
|
|
|
|
|
|
|
A.C.Belkina,
and
G.V.Denis
(2012).
BET domain co-regulators in obesity, inflammation and cancer.
|
| |
Nat Rev Cancer,
12,
465-477.
|
|
|
|
|
|
|
C.A.Musselman,
M.E.Lalonde,
J.Côté,
and
T.G.Kutateladze
(2012).
Perceiving the epigenetic landscape through histone readers.
|
| |
Nat Struct Mol Biol,
19,
1218-1227.
|
|
|
|
|
|
|
H.Heyn,
and
M.Esteller
(2012).
DNA methylation profiling in the clinic: applications and challenges.
|
| |
Nat Rev Genet,
13,
679-692.
|
|
|
|
|
|
|
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.
|
|
|
|
|
|
|
M.N.Patel,
M.D.Halling-Brown,
J.E.Tym,
P.Workman,
and
B.Al-Lazikani
(2012).
Objective assessment of cancer genes for drug discovery.
|
| |
Nat Rev Drug Discov,
12,
35-50.
|
|
|
|
|
|
|
D.C.Hargreaves,
and
G.R.Crabtree
(2011).
ATP-dependent chromatin remodeling: genetics, genomics and mechanisms.
|
| |
Cell Res,
21,
396-420.
|
|
|
|
|
|
|
F.J.Dilworth,
and
A.Blais
(2011).
Epigenetic regulation of satellite cell activation during muscle regeneration.
|
| |
Stem Cell Res Ther,
2,
18.
|
|
|
|
|
|
|
J.Patel,
R.R.Pathak,
and
S.Mujtaba
(2011).
The biology of lysine acetylation integrates transcriptional programming and metabolism.
|
| |
Nutr Metab (Lond),
8,
12.
|
|
|
|
|
|
|
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.
|
|
|
|
|
|
|
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:
|
|
|
|
|
|
|
|
R.Zhao,
T.Nakamura,
Y.Fu,
Z.Lazar,
and
D.L.Spector
(2011).
Gene bookmarking accelerates the kinetics of post-mitotic transcriptional re-activation.
|
| |
Nat Cell Biol,
13,
1295-1304.
|
|
|
|
|
|
|
S.B.Baylin,
and
P.A.Jones
(2011).
A decade of exploring the cancer epigenome - biological and translational implications.
|
| |
Nat Rev Cancer,
11,
726-734.
|
|
|
|
|
|
|
S.Khochbin
(2011).
In the heart of a dynamic chromatin.
|
| |
Chem Biol,
18,
410-412.
|
|
|
|
|
|
|
S.M.Feller
(2011).
First Honorary Medal of the Signal Transduction Society (STS) and 'CELL COMMUNICATION AND SIGNALING' awarded to Professor Anthony J. (Tony) Pawson.
|
| |
Cell Commun Signal,
9,
3.
|
|
|
|
|
|
|
T.Ito,
T.Umehara,
K.Sasaki,
Y.Nakamura,
N.Nishino,
T.Terada,
M.Shirouzu,
B.Padmanabhan,
S.Yokoyama,
A.Ito,
and
M.Yoshida
(2011).
Real-time imaging of histone H4K12-specific acetylation determines the modes of action of histone deacetylase and bromodomain inhibitors.
|
| |
Chem Biol,
18,
495-507.
|
|
|
PDB code:
|
|
|
|
|
|
|
|
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.
|
|
Links
