Details of the Target

General Information of Target

Target ID LDTP06304
Target Name Bromodomain-containing protein 3 (BRD3)
Gene Name BRD3
Gene ID 8019
Synonyms
KIAA0043; RING3L; Bromodomain-containing protein 3; RING3-like protein
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSTATTVAPAGIPATPGPVNPPPPEVSNPSKPGRKTNQLQYMQNVVVKTLWKHQFAWPFY
QPVDAIKLNLPDYHKIIKNPMDMGTIKKRLENNYYWSASECMQDFNTMFTNCYIYNKPTD
DIVLMAQALEKIFLQKVAQMPQEEVELLPPAPKGKGRKPAAGAQSAGTQQVAAVSSVSPA
TPFQSVPPTVSQTPVIAATPVPTITANVTSVPVPPAAAPPPPATPIVPVVPPTPPVVKKK
GVKRKADTTTPTTSAITASRSESPPPLSDPKQAKVVARRESGGRPIKPPKKDLEDGEVPQ
HAGKKGKLSEHLRYCDSILREMLSKKHAAYAWPFYKPVDAEALELHDYHDIIKHPMDLST
VKRKMDGREYPDAQGFAADVRLMFSNCYKYNPPDHEVVAMARKLQDVFEMRFAKMPDEPV
EAPALPAPAAPMVSKGAESSRSSEESSSDSGSSDSEEERATRLAELQEQLKAVHEQLAAL
SQAPVNKPKKKKEKKEKEKKKKDKEKEKEKHKVKAEEEKKAKVAPPAKQAQQKKAPAKKA
NSTTTAGRQLKKGGKQASASYDSEEEEEGLPMSYDEKRQLSLDINRLPGEKLGRVVHIIQ
SREPSLRDSNPDEIEIDFETLKPTTLRELERYVKSCLQKKQRKPFSASGKKQAAKSKEEL
AQEKKKELEKRLQDVSGQLSSSKKPARKEKPGSAPSGGPSRLSSSSSSESGSSSSSGSSS
DSSDSE
Target Type
Clinical trial
Target Bioclass
Other
Subcellular location
Nucleus
Function
Chromatin reader that recognizes and binds acetylated histones, thereby controlling gene expression and remodeling chromatin structures. Recruits transcription factors and coactivators to target gene sites, and activates RNA polymerase II machinery for transcriptional elongation. In vitro, binds acetylated lysine residues on the N-terminus of histone H2A, H2B, H3 and H4. Involved in endoderm differentiation via its association with long non-coding RNA (lncRNA) DIGIT: BRD3 undergoes liquid-liquid phase separation upon binding to lncRNA DIGIT, promoting binding to histone H3 acetylated at 'Lys-18' (H3K18ac) to induce endoderm gene expression. Also binds non-histones acetylated proteins, such as GATA1 and GATA2: regulates transcription by promoting the binding of the transcription factor GATA1 to its targets.
TTD ID
T42048
Uniprot ID
Q15059
DrugMap ID
TTHE657
Ensemble ID
ENST00000303407.12
HGNC ID
HGNC:1104
ChEMBL ID
CHEMBL1795186

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
EFO27 SNV: p.G717R DBIA    Probe Info 
HCT15 SNV: p.P299S DBIA    Probe Info 
HEP3B217 SNV: p.S434N DBIA    Probe Info 
HT115 SNV: p.N37K DBIA    Probe Info 
JHH4 SNV: p.H327L DBIA    Probe Info 
KARPAS422 SNV: p.K497R; p.K534R DBIA    Probe Info 
KELLY SNV: p.P355Q .
KYSE30 SNV: p.E409K .
MEWO Substitution: p.P355L DBIA    Probe Info 
NCIH1048 SNV: p.K591R DBIA    Probe Info 
RL952 SNV: p.R284H DBIA    Probe Info 
SKMEL5 SNV: p.Q662Ter DBIA    Probe Info 
SW1783 SNV: p.R578H DBIA    Probe Info 
TE4 SNV: p.T544N DBIA    Probe Info 
TYKNU SNV: p.S715F DBIA    Probe Info 

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 7 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
Probe 1
 Probe Info  		Y370(6.63)  LDD3495  [1]
DBIA
 Probe Info  		C429(2.51)  LDD3310  [2]
BTD
 Probe Info  		C387(2.10)  LDD2135  [3]
Acrolein
 Probe Info  		N.A.  LDD0223  [4]
4-Iodoacetamidophenylacetylene
 Probe Info  		N.A.  LDD0038  [5]
IA-alkyne
 Probe Info  		N.A.  LDD0032  [6]
Lodoacetamide azide
 Probe Info  		N.A.  LDD0037  [5]
PAL-AfBPP Probe
Click To Hide/Show 4 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
VE-P
 Probe Info  		N.A.  LDD0396  [7]
8df
 Probe Info  		5.70  LDD0250  [8]
8ef
 Probe Info  		6.73  LDD0251  [8]
photo_BS
 Probe Info  		2.35  LDD0412  [9]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0092  Amine 8 HL-60 5.70  LDD0250  [8]
 LDCM0160  Bromosprine HEK-293T 2.35  LDD0412  [9]
 LDCM0022  KB02 42-MG-BA C429(2.18)  LDD2244  [2]
 LDCM0023  KB03 42-MG-BA C429(2.78)  LDD2661  [2]
 LDCM0024  KB05 COLO792 C429(2.51)  LDD3310  [2]
 LDCM0109  NEM HeLa N.A.  LDD0223  [4]
 LDCM0542  Nucleophilic fragment 37 MDA-MB-231 C387(2.10)  LDD2135  [3]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Importin subunit alpha-4 (KPNA3) Importin alpha family O00505
Transcription factor
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Myc proto-oncogene protein (MYC) . P01106

The Drug(s) Related To This Target

Phase 1
Click To Hide/Show 1 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Abbv-744 . D05ICT
Investigative
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Gw841819x Small molecular drug D03LIP
I-bet151 Small molecular drug D0WU1S
Pmid24000170c36 Small molecular drug D0C2XT
Pmid24000170c38 Small molecular drug D0Q2GK
Xd14 Small molecular drug D07FGY
Patented
Click To Hide/Show 5 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid26924192-compound-102 Small molecular drug D03RPJ
Pmid26924192-compound-103 Small molecular drug D05XXS
Pmid26924192-compound-104 Small molecular drug D03NWT
Pmid26924192-compound-105 Small molecular drug D0NN4U
Pyrrolo-pyrrolone Derivative 1 Small molecular drug D0YM3G

References

1 An Azo Coupling-Based Chemoproteomic Approach to Systematically Profile the Tyrosine Reactivity in the Human Proteome. Anal Chem. 2021 Jul 27;93(29):10334-10342. doi: 10.1021/acs.analchem.1c01935. Epub 2021 Jul 12.
2 DrugMap: A quantitative pan-cancer analysis of cysteine ligandability. Cell. 2024 May 9;187(10):2536-2556.e30. doi: 10.1016/j.cell.2024.03.027. Epub 2024 Apr 22.
Mass spectrometry data entry: PXD047840
3 Nucleophilic covalent ligand discovery for the cysteine redoxome. Nat Chem Biol. 2023 Nov;19(11):1309-1319. doi: 10.1038/s41589-023-01330-5. Epub 2023 May 29.
Mass spectrometry data entry: PXD039908 , PXD029761
4 ACR-Based Probe for the Quantitative Profiling of Histidine Reactivity in the Human Proteome. J Am Chem Soc. 2023 Mar 8;145(9):5252-5260. doi: 10.1021/jacs.2c12653. Epub 2023 Feb 27.
5 Enhancing Cysteine Chemoproteomic Coverage through Systematic Assessment of Click Chemistry Product Fragmentation. Anal Chem. 2022 Mar 8;94(9):3800-3810. doi: 10.1021/acs.analchem.1c04402. Epub 2022 Feb 23.
Mass spectrometry data entry: PXD028853
6 SP3-FAIMS Chemoproteomics for High-Coverage Profiling of the Human Cysteinome*. Chembiochem. 2021 May 14;22(10):1841-1851. doi: 10.1002/cbic.202000870. Epub 2021 Feb 18.
Mass spectrometry data entry: PXD023056 , PXD023059 , PXD023058 , PXD023057 , PXD023060
7 Pharmacological Targeting of Vacuolar H(+)-ATPase via Subunit V1G Combats Multidrug-Resistant Cancer. Cell Chem Biol. 2020 Nov 19;27(11):1359-1370.e8. doi: 10.1016/j.chembiol.2020.06.011. Epub 2020 Jul 9.
8 One-Step Synthesis of Photoaffinity Probes for Live-Cell MS-Based Proteomics. Chemistry. 2021 Dec 20;27(71):17880-17888. doi: 10.1002/chem.202102036. Epub 2021 Sep 14.
9 Chemical Proteomic Profiling of Bromodomains Enables the Wide-Spectrum Evaluation of Bromodomain Inhibitors in Living Cells. J Am Chem Soc. 2019 Jul 24;141(29):11497-11505. doi: 10.1021/jacs.9b02738. Epub 2019 Jul 9.