3.0
Summary
| Name |  BRD4View Modifications |
| Full Name | Bromodomain-containing protein 4 |
| Synonyms | Protein HUNK1 | HUNK1 |
| Primary ID | O60885 |
| Links |  -  -  |
| Type | protein |
| Relations | 20 |
| Inhibitors | JQ1; CID 132010322; CPI-0610 carboxylic acid; 2-[(9S)-7-(4-Chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]-N-[8-[[2-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]oxyacetyl]amino]octyl]acetamide; Tert-butyl 2-[(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]acetate; 2-[(4S)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide; CID 122201421 |
| Function | Chromatin reader protein that recognizes and binds acetylated histones and plays a key role in transmission of epigenetic memory across cell divisions and transcription regulation. Remains associated with acetylated chromatin throughout the entire cell cycle and provides epigenetic memory for postmitotic G1 gene transcription by preserving acetylated chromatin status and maintaining high-order chromatin structure (PubMed:23589332, PubMed:23317504, PubMed:22334664). During interphase, plays a key role in regulating the transcription of signal-inducible genes by associating with the P-TEFb complex and recruiting it to promoters. Also recruits P-TEFb complex to distal enhancers, so called anti-pause enhancers in collaboration with JMJD6. BRD4 and JMJD6 are required to form the transcriptionally active P-TEFb complex by displacing negative regulators such as HEXIM1 and 7SKsnRNA complex from P-TEFb, thereby transforming it into an active form that can then phosphorylate the C-terminal domain (CTD) of RNA polymerase II (PubMed:23589332, PubMed:19596240, PubMed:16109377, PubMed:16109376, PubMed:24360279). Promotes phosphorylation of 'Ser-2' of the C-terminal domain (CTD) of RNA polymerase II (PubMed:23086925). According to a report, directly acts as an atypical protein kinase and mediates phosphorylation of 'Ser-2' of the C-terminal domain (CTD) of RNA polymerase II; these data however need additional evidences in vivo (PubMed:22509028). In addition to acetylated histones, also recognizes and binds acetylated RELA, leading to further recruitment of the P-TEFb complex and subsequent activation of NF-kappa-B (PubMed:19103749). Also acts as a regulator of p53/TP53-mediated transcription |
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Modifications Tables
Relations
| Regulator | Mechanism | target | score ℹ | |
|---|---|---|---|---|
| + | BRD4 | up-regulates 
phosphorylation
|
POLR2A | 0.461 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | BRD4 | down-regulates quantity by destabilization 
phosphorylation
|
MYC | 0.58 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | JAK2 | up-regulates quantity by stabilization
phosphorylation
|
BRD4 | 0.331 |
| Publications: | 2 | Organism: | Homo Sapiens | |
| + | JQ1 | down-regulates activity
chemical inhibition
|
BRD4 | 0.8 |
| Publications: | 1 | Organism: | In Vitro | |
| + | CID 132010322 | down-regulates activity
chemical inhibition
|
BRD4 | 0.8 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | H4C1 | up-regulates activity
relocalization
|
BRD4 | 0.2 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | CPI-0610 carboxylic acid | down-regulates activity
chemical inhibition
|
BRD4 | 0.8 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | 2-[(9S)-7-(4-Chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]-N-[8-[[2-[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]oxyacetyl]amino]octyl]acetamide | down-regulates quantity
chemical inhibition
|
BRD4 | 0.8 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | BRD4 | up-regulates activity
binding
|
P-TEFb | 0.62 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | Tert-butyl 2-[(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]acetate | down-regulates activity
chemical inhibition
|
BRD4 | 0.8 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | BRD4 | up-regulates quantity by expression 
transcriptional regulation
|
KDM5C | 0.334 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | BRD4 | up-regulates activity
binding
|
EP300 | 0.436 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | ATAD5 | up-regulates
binding
|
BRD4 | 0.357 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | 2-[(4S)-6-(4-chlorophenyl)-8-methoxy-1-methyl-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepin-4-yl]-N-ethylacetamide | down-regulates activity
chemical inhibition
|
BRD4 | 0.8 |
| Publications: | 1 | Organism: | In Vitro | |
| + | YAP/TAZ | up-regulates activity
relocalization
|
BRD4 | 0.2 |
| Publications: | 1 | |||
| + | CID 122201421 | down-regulates activity
chemical inhibition
|
BRD4 | 0.8 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | MAPK3 | down-regulates activity
|
BRD4 | 0.317 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | ASXL3 | up-regulates activity
binding
|
BRD4 | 0.2 |
| Publications: | 1 | Organism: | Homo Sapiens | |
| + | MYC | down-regulates activity
|
BRD4 | 0.58 |
| Publications: | 1 | Organism: | Homo Sapiens | |