Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

BRD2 (P25440) - Overview - Molecular Target Synopsis

Protein


BRD2, Bromodomain-containing protein 2
UniProt P25440

Also Known as BRD2_HUMAN, BRD2, KIAA9001, RING3

May play a role in spermatogenesis or folliculogenesis (By similarity). Binds hyperacetylated chromatin and plays a role in the regulation of transcription, probably by chromatin remodeling. Regulates transcription of the CCND1 gene. Plays a role in nucleosome assembly. Homodimer. Interacts with E2F1 and with histone H4 acetylated at 'Lys-13'.

6CUI
SOLUTION STRUCTURE OF THE EXTRATERMINAL (ET) DOMAIN OF BRD2
RCSB/PDB
Inspect Structure
See all 3D Structures for BRD2

Isoforms / Transcripts (Protein Coding)


Sub-cellular localization


UniProt: BRD2 is active in the following subcellular-locations: nucleus.
GO terms: BRD2 is active in the following subcellular-locations: cytoplasm, nuclear speck, nucleoplasm.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project BRD2 has gain in 0 cell-lines, loss in 0 cell-lines and no signal in 0 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: HOP_62, NCI_ADR_RES, HCT_15

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: NCI-H209, Hs 746T, SNU-398

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: SK-N-SH, K562, HSMM

(see details)

3D Structures


For BRD2 there are:
68 structures (135 chains) solved
56 are solved in complex with at least one small molecule ligand
1 are solved with an approved drug

BRD2 is solved in complex with the approved drug(s):

TYL/ACETAMINOPHEN (4A9J_A, 4A9J_B, 4A9J_C).

(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


BRD2 has been screened with 457 compounds (603 bioactivities), 161 compounds have bioactivities that show binding affinity of <= 500nM (200 bioactivities). (see details)