RGD Reference Report - The bromodomain: From epigenome reader to druggable target. - Rat Genome Database

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The bromodomain: From epigenome reader to druggable target.

Authors: Sanchez, R  Meslamani, J  Zhou, MM 
Citation: Sanchez R, etal., Biochim Biophys Acta. 2014 Aug;1839(8):676-685. doi: 10.1016/j.bbagrm.2014.03.011. Epub 2014 Mar 28.
RGD ID: 9479075
Pubmed: PMID:24686119   (View Abstract at PubMed)
PMCID: PMC4099289   (View Article at PubMed Central)
DOI: DOI:10.1016/j.bbagrm.2014.03.011   (Journal Full-text)

Lysine acetylation is a fundamental post-translational modification that plays an important role in the control of gene transcription in chromatin in an ordered fashion. The bromodomain, the conserved structural module present in transcription-associated proteins, functions exclusively to recognize acetyl-lysine on histones and non-histone proteins. The structural analyses of bromodomains' recognition of lysine-acetylated peptides derived from histones and cellular proteins provide detailed insights into the differences and unifying features of biological ligand binding selectivity by the bromodomains. Newly developed small-molecule inhibitors targeting bromodomain proteins further highlight the functional importance of bromodomain/acetyl-lysine binding as a key mechanism in orchestrating molecular interactions and regulation in chromatin biology and gene transcription. These new studies argue that modulating bromodomain/acetyl-lysine interactions with small-molecule chemicals offer new opportunities to control gene expression in a wide array of human diseases including cancer and inflammation. This article is part of a Special Issue entitled: Molecular mechanisms of histone modification function.



Molecular Pathway Annotations    Click to see Annotation Detail View

RGD Manual Annotations


  
Object SymbolSpeciesTermQualifierEvidenceWithNotesSourceOriginal Reference(s)
BPTFHumanhistone modification pathway   TAS  RGD 
BRD1Humanhistone modification pathway   TAS  RGD 
BRD2Humanhistone modification pathway   TAS  RGD 
BRD3Humanhistone modification pathway   TAS  RGD 
BRD4Humanhistone modification pathway   TAS  RGD 
BRD7Humanhistone modification pathway   TAS  RGD 
BRDTHumanhistone modification pathway   TAS  RGD 
BptfRathistone modification pathway   ISOBPTF (Homo sapiens) RGD 
BptfMousehistone modification pathway   ISOBPTF (Homo sapiens) RGD 
Brd1Rathistone modification pathway   ISOBRD1 (Homo sapiens) RGD 
Brd1Mousehistone modification pathway   ISOBRD1 (Homo sapiens) RGD 
Brd2Rathistone modification pathway   ISOBRD2 (Homo sapiens) RGD 
Brd2Mousehistone modification pathway   ISOBRD2 (Homo sapiens) RGD 
Brd3Rathistone modification pathway   ISOBRD3 (Homo sapiens) RGD 
Brd3Mousehistone modification pathway   ISOBRD3 (Homo sapiens) RGD 
Brd4Rathistone modification pathway   ISOBRD4 (Homo sapiens) RGD 
Brd4Mousehistone modification pathway   ISOBRD4 (Homo sapiens) RGD 
Brd7Rathistone modification pathway   ISOBRD7 (Homo sapiens) RGD 
Brd7Mousehistone modification pathway   ISOBRD7 (Homo sapiens) RGD 
BrdtRathistone modification pathway   ISOBRDT (Homo sapiens) RGD 
BrdtMousehistone modification pathway   ISOBRDT (Homo sapiens) RGD 
CREBBPHumanhistone modification pathway   TAS  RGD 
CrebbpRathistone modification pathway   ISOCREBBP (Homo sapiens) RGD 
CrebbpMousehistone modification pathway   ISOCREBBP (Homo sapiens) RGD 
PBRM1Humanhistone modification pathway   TAS  RGD 
Pbrm1Mousehistone modification pathway   ISOPBRM1 (Homo sapiens) RGD 
Pbrm1Rathistone modification pathway   ISOPBRM1 (Homo sapiens) RGD 
SMARCA2Humanhistone modification pathway   TAS  RGD 
SMARCA4Humanhistone modification pathway   TAS  RGD 
Smarca2Rathistone modification pathway   ISOSMARCA2 (Homo sapiens) RGD 
Smarca2Mousehistone modification pathway   ISOSMARCA2 (Homo sapiens) RGD 
Smarca4Rathistone modification pathway   ISOSMARCA4 (Homo sapiens) RGD 
Smarca4Mousehistone modification pathway   ISOSMARCA4 (Homo sapiens) RGD 
TAF1Humanhistone modification pathway   TAS  RGD 
TRIM33Humanhistone modification pathway   TAS  RGD 
Taf1Mousehistone modification pathway   ISOTAF1 (Homo sapiens) RGD 
Taf1Rathistone modification pathway   ISOTAF1 (Homo sapiens) RGD 
Trim33Rathistone modification pathway   ISOTRIM33 (Homo sapiens) RGD 
Trim33Mousehistone modification pathway   ISOTRIM33 (Homo sapiens) RGD 
Objects Annotated

Genes (Rattus norvegicus)
Bptf  (bromodomain PHD finger transcription factor)
Brd1  (bromodomain containing 1)
Brd2  (bromodomain containing 2)
Brd3  (bromodomain containing 3)
Brd4  (bromodomain containing 4)
Brd7  (bromodomain containing 7)
Brdt  (bromodomain testis associated)
Crebbp  (CREB binding protein)
Pbrm1  (polybromo 1)
Smarca2  (SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 2)
Smarca4  (SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 4)
Taf1  (TATA-box binding protein associated factor 1)
Trim33  (tripartite motif-containing 33)

Genes (Mus musculus)
Bptf  (bromodomain PHD finger transcription factor)
Brd1  (bromodomain containing 1)
Brd2  (bromodomain containing 2)
Brd3  (bromodomain containing 3)
Brd4  (bromodomain containing 4)
Brd7  (bromodomain containing 7)
Brdt  (bromodomain, testis-specific)
Crebbp  (CREB binding protein)
Pbrm1  (polybromo 1)
Smarca2  (SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 2)
Smarca4  (SWI/SNF related, matrix associated, actin dependent regulator of chromatin, subfamily a, member 4)
Taf1  (TATA-box binding protein associated factor 1)
Trim33  (tripartite motif-containing 33)

Genes (Homo sapiens)
BPTF  (bromodomain PHD finger transcription factor)
BRD1  (bromodomain containing 1)
BRD2  (bromodomain containing 2)
BRD3  (bromodomain containing 3)
BRD4  (bromodomain containing 4)
BRD7  (bromodomain containing 7)
BRDT  (bromodomain testis associated)
CREBBP  (CREB binding protein)
PBRM1  (polybromo 1)
SMARCA2  (SWI/SNF related BAF chromatin remodeling complex subunit ATPase 2)
SMARCA4  (SWI/SNF related BAF chromatin remodeling complex subunit ATPase 4)
TAF1  (TATA-box binding protein associated factor 1)
TRIM33  (tripartite motif containing 33)


Additional Information