Details of the Target

General Information of Target

Target ID LDTP11705
Target Name Bromodomain-containing protein 8 (BRD8)
Gene Name BRD8
Gene ID 10902
Synonyms
SMAP; SMAP2; Bromodomain-containing protein 8; Skeletal muscle abundant protein; Skeletal muscle abundant protein 2; Thyroid hormone receptor coactivating protein of 120 kDa; TrCP120; p120
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MLAMDTCKHVGQLQLAQDHSSLNPQKWHCVDCNTTESIWACLSCSHVACGRYIEEHALKH
FQESSHPVALEVNEMYVFCYLCDDYVLNDNTTGDLKLLRRTLSAIKSQNYHCTTRSGRFL
RSMGTGDDSYFLHDGAQSLLQSEDQLYTALWHRRRILMGKIFRTWFEQSPIGRKKQEEPF
QEKIVVKREVKKRRQELEYQVKAELESMPPRKSLRLQGLAQSTIIEIVSVQVPAQTPASP
AKDKVLSTSENEISQKVSDSSVKRRPIVTPGVTGLRNLGNTCYMNSVLQVLSHLLIFRQC
FLKLDLNQWLAMTASEKTRSCKHPPVTDTVVYQMNECQEKDTGFVCSRQSSLSSGLSGGA
SKGRKMELIQPKEPTSQYISLCHELHTLFQVMWSGKWALVSPFAMLHSVWRLIPAFRGYA
QQDAQEFLCELLDKIQRELETTGTSLPALIPTSQRKLIKQVLNVVNNIFHGQLLSQVTCL
ACDNKSNTIEPFWDLSLEFPERYQCSGKDIASQPCLVTEMLAKFTETEALEGKIYVCDQC
NSKRRRFSSKPVVLTEAQKQLMICHLPQVLRLHLKRFRWSGRNNREKIGVHVGFEEILNM
EPYCCRETLKSLRPECFIYDLSAVVMHHGKGFGSGHYTAYCYNSEGGFWVHCNDSKLSMC
TMDEVCKAQAYILFYTQRVTENGHSKLLPPELLLGSQHPNEDADTSSNEILS
Target Bioclass
Other
Subcellular location
Nucleus
Function
May act as a coactivator during transcriptional activation by hormone-activated nuclear receptors (NR). Isoform 2 stimulates transcriptional activation by AR/DHTR, ESR1/NR3A1, RXRA/NR2B1 and THRB/ERBA2. At least isoform 1 and isoform 2 are components of the NuA4 histone acetyltransferase (HAT) complex which is involved in transcriptional activation of select genes principally by acetylation of nucleosomal histones H4 and H2A. This modification may both alter nucleosome - DNA interactions and promote interaction of the modified histones with other proteins which positively regulate transcription. This complex may be required for the activation of transcriptional programs associated with oncogene and proto-oncogene mediated growth induction, tumor suppressor mediated growth arrest and replicative senescence, apoptosis, and DNA repair. NuA4 may also play a direct role in DNA repair when recruited to sites of DNA damage. Component of a SWR1-like complex that specifically mediates the removal of histone H2A.Z/H2AZ1 from the nucleosome.
Uniprot ID
Q9H0E9
Ensemble ID
ENST00000230901.9
HGNC ID
HGNC:19874
ChEMBL ID
CHEMBL3588731

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
FTC133 SNV: p.I495K .
HCT116 Deletion: p.R178GfsTer6 .
HEC1 SNV: p.A65T DBIA    Probe Info 
HEC1B SNV: p.A65T .
HSC3 Deletion: p.L1113QfsTer5 .
MFE296 Deletion: p.R178GfsTer6 DBIA    Probe Info 
NCIH3122 SNV: p.E657Ter DBIA    Probe Info 
PEO1 SNV: p.Y728H .
YSCCC SNV: p.S1158F .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 13 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
m-APA
 Probe Info  		15.00  LDD0402  [1]
P8
 Probe Info  		2.08  LDD0455  [2]
DBIA
 Probe Info  		C26(2.75)  LDD3310  [3]
Acrolein
 Probe Info  		N.A.  LDD0222  [4]
IA-alkyne
 Probe Info  		N.A.  LDD0036  [5]
Lodoacetamide azide
 Probe Info  		N.A.  LDD0037  [5]
IPM
 Probe Info  		C142(0.00); C64(0.00)  LDD0147  [6]
TFBX
 Probe Info  		N.A.  LDD0148  [6]
Phosphinate-6
 Probe Info  		N.A.  LDD0018  [7]
Methacrolein
 Probe Info  		N.A.  LDD0218  [4]
W1
 Probe Info  		N.A.  LDD0236  [8]
AOyne
 Probe Info  		15.00  LDD0443  [9]
NAIA_5
 Probe Info  		C64(0.00); C26(0.00)  LDD2223  [10]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0156  Aniline NCI-H1299 11.51  LDD0403  [1]
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [4]
 LDCM0632  CL-Sc Hep-G2 C64(1.13); C64(0.95)  LDD2227  [10]
 LDCM0022  KB02 22RV1 C26(2.46)  LDD2243  [3]
 LDCM0023  KB03 22RV1 C26(3.74)  LDD2660  [3]
 LDCM0024  KB05 COLO792 C26(2.75)  LDD3310  [3]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Fibronectin type III and SPRY domain-containing protein 2 (FSD2) . A1L4K1
Peptidyl-prolyl cis-trans isomerase NIMA-interacting 1 (PIN1) . Q13526
Other
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Enhancer of polycomb homolog 1 (EPC1) Enhancer of polycomb family Q9H2F5
Protein Mis18-alpha (MIS18A) Mis18 family Q9NYP9
Microspherule protein 1 (MCRS1) . Q96EZ8

References

1 Quantitative and Site-Specific Chemoproteomic Profiling of Targets of Acrolein. Chem Res Toxicol. 2019 Mar 18;32(3):467-473. doi: 10.1021/acs.chemrestox.8b00343. Epub 2019 Jan 15.
2 Comparison of Different Competitive Proteome Profiling Approaches in Target Identification of Covalent Inhibitors. Chembiochem. 2022 Dec 16;23(24):e202200389. doi: 10.1002/cbic.202200389. Epub 2022 Nov 22.
3 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
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 Chemoproteomic Profiling by Cysteine Fluoroalkylation Reveals Myrocin G as an Inhibitor of the Nonhomologous End Joining DNA Repair Pathway. J Am Chem Soc. 2021 Dec 8;143(48):20332-20342. doi: 10.1021/jacs.1c09724. Epub 2021 Nov 24.
Mass spectrometry data entry: PXD029255
7 DFT-Guided Discovery of Ethynyl-Triazolyl-Phosphinates as Modular Electrophiles for Chemoselective Cysteine Bioconjugation and Profiling. Angew Chem Int Ed Engl. 2022 Oct 10;61(41):e202205348. doi: 10.1002/anie.202205348. Epub 2022 Aug 22.
Mass spectrometry data entry: PXD033004
8 Oxidant-Induced Bioconjugation for Protein Labeling in Live Cells. ACS Chem Biol. 2023 Jan 20;18(1):112-122. doi: 10.1021/acschembio.2c00740. Epub 2022 Dec 21.
9 Chemoproteomic profiling of targets of lipid-derived electrophiles by bioorthogonal aminooxy probe. Redox Biol. 2017 Aug;12:712-718. doi: 10.1016/j.redox.2017.04.001. Epub 2017 Apr 5.
10 N-Acryloylindole-alkyne (NAIA) enables imaging and profiling new ligandable cysteines and oxidized thiols by chemoproteomics. Nat Commun. 2023 Jun 15;14(1):3564. doi: 10.1038/s41467-023-39268-w.
Mass spectrometry data entry: PXD041264