Details of the Target

General Information of Target

Target ID LDTP01653
Target Name Bromodomain-containing protein 1 (BRD1)
Gene Name BRD1
Gene ID 23774
Synonyms
BRL; BRPF2; Bromodomain-containing protein 1; BR140-like protein; Bromodomain and PHD finger-containing protein 2
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MRRKGRCHRGSAARHPSSPCSVKHSPTRETLTYAQAQRMVEIEIEGRLHRISIFDPLEII
LEDDLTAQEMSECNSNKENSERPPVCLRTKRHKNNRVKKKNEALPSAHGTPASASALPEP
KVRIVEYSPPSAPRRPPVYYKFIEKSAEELDNEVEYDMDEEDYAWLEIVNEKRKGDCVPA
VSQSMFEFLMDRFEKESHCENQKQGEQQSLIDEDAVCCICMDGECQNSNVILFCDMCNLA
VHQECYGVPYIPEGQWLCRHCLQSRARPADCVLCPNKGGAFKKTDDDRWGHVVCALWIPE
VGFANTVFIEPIDGVRNIPPARWKLTCYLCKQKGVGACIQCHKANCYTAFHVTCAQKAGL
YMKMEPVKELTGGGTTFSVRKTAYCDVHTPPGCTRRPLNIYGDVEMKNGVCRKESSVKTV
RSTSKVRKKAKKAKKALAEPCAVLPTVCAPYIPPQRLNRIANQVAIQRKKQFVERAHSYW
LLKRLSRNGAPLLRRLQSSLQSQRSSQQRENDEEMKAAKEKLKYWQRLRHDLERARLLIE
LLRKREKLKREQVKVEQVAMELRLTPLTVLLRSVLDQLQDKDPARIFAQPVSLKEVPDYL
DHIKHPMDFATMRKRLEAQGYKNLHEFEEDFDLIIDNCMKYNARDTVFYRAAVRLRDQGG
VVLRQARREVDSIGLEEASGMHLPERPAAAPRRPFSWEDVDRLLDPANRAHLGLEEQLRE
LLDMLDLTCAMKSSGSRSKRAKLLKKEIALLRNKLSQQHSQPLPTGPGLEGFEEDGAALG
PEAGEEVLPRLETLLQPRKRSRSTCGDSEVEEESPGKRLDAGLTNGFGGARSEQEPGGGL
GRKATPRRRCASESSISSSNSPLCDSSFNAPKCGRGKPALVRRHTLEDRSELISCIENGN
YAKAARIAAEVGQSSMWISTDAAASVLEPLKVVWAKCSGYPSYPALIIDPKMPRVPGHHN
GVTIPAPPLDVLKIGEHMQTKSDEKLFLVLFFDNKRSWQWLPKSKMVPLGIDETIDKLKM
MEGRNSSIRKAVRIAFDRAMNHLSRVHGEPTSDLSDID
Target Type
Literature-reported
Target Bioclass
Transcription factor
Subcellular location
Nucleus
Function
Scaffold subunit of various histone acetyltransferase (HAT) complexes, such as the MOZ/MORF and HBO1 complexes, that acts as a regulator of hematopoiesis. Plays a key role in HBO1 complex by directing KAT7/HBO1 specificity towards histone H3 'Lys-14' acetylation (H3K14ac), thereby promoting erythroid differentiation.
TTD ID
T35809
Uniprot ID
O95696
DrugMap ID
TTT09OB
Ensemble ID
ENST00000216267.12
HGNC ID
HGNC:1102
ChEMBL ID
CHEMBL2176774

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 11 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C937(1.58)  LDD3312  [1]
BTD
 Probe Info  		C86(1.18)  LDD2098  [2]
AHL-Pu-1
 Probe Info  		C86(2.43)  LDD0168  [3]
IA-alkyne
 Probe Info  		N.A.  LDD0036  [4]
Lodoacetamide azide
 Probe Info  		C937(0.00); C729(0.00); C199(0.00)  LDD0037  [4]
NAIA_5
 Probe Info  		N.A.  LDD2224  [5]
IPM
 Probe Info  		N.A.  LDD0005  [6]
TFBX
 Probe Info  		N.A.  LDD0148  [7]
Phosphinate-6
 Probe Info  		N.A.  LDD0018  [8]
Acrolein
 Probe Info  		N.A.  LDD0217  [9]
Methacrolein
 Probe Info  		N.A.  LDD0218  [9]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0524  2-Cyano-N-(2-morpholin-4-yl-ethyl)-acetamide MDA-MB-231 C86(1.09)  LDD2117  [2]
 LDCM0025  4SU-RNA HEK-293T C86(2.43)  LDD0168  [3]
 LDCM0026  4SU-RNA+native RNA HEK-293T C86(2.55); C177(2.07)  LDD0169  [3]
 LDCM0632  CL-Sc Hep-G2 C805(1.72)  LDD2227  [5]
 LDCM0213  Electrophilic fragment 2 MDA-MB-231 C20(1.33); C86(1.21); C393(0.98); C261(0.43)  LDD1702  [2]
 LDCM0203  EV-96 T cell C441, C448(4.39)  LDD0523  [10]
 LDCM0022  KB02 HEK-293T C805(0.91); C729(1.00); C393(0.92); C338(0.96)  LDD1492  [11]
 LDCM0023  KB03 HEK-293T C805(0.93); C729(0.93); C393(1.07); C338(0.98)  LDD1497  [11]
 LDCM0024  KB05 HMCB C937(1.58)  LDD3312  [1]
 LDCM0505  Nucleophilic fragment 15b MDA-MB-231 C86(1.18)  LDD2098  [2]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Ubiquitin thioesterase ZRANB1 (ZRANB1) Peptidase C64 family Q9UGI0
Transcription factor
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Homeobox-containing protein 1 (HMBOX1) . Q6NT76
Protein polybromo-1 (PBRM1) . Q86U86
Other
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Colorectal mutant cancer protein (MCC) MCC family P23508
Tuftelin-interacting protein 11 (TFIP11) TFP11/STIP family Q9UBB9
Centrosomal protein of 70 kDa (CEP70) . Q8NHQ1
Melanoma-associated antigen 11 (MAGEA11) . P43364
PRKCA-binding protein (PICK1) . Q9NRD5
Run domain Beclin-1-interacting and cysteine-rich domain-containing protein (RUBCN) . Q92622

The Drug(s) Related To This Target

Investigative
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Ni-57 Small molecular drug D0O6XT
Of-1 Small molecular drug D08RDI

References

1 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
2 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
3 Chemoproteomic capture of RNA binding activity in living cells. Nat Commun. 2023 Oct 7;14(1):6282. doi: 10.1038/s41467-023-41844-z.
Mass spectrometry data entry: PXD044625
4 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
5 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
6 A modification-centric assessment tool for the performance of chemoproteomic probes. Nat Chem Biol. 2022 Aug;18(8):904-912. doi: 10.1038/s41589-022-01074-8. Epub 2022 Jul 21.
Mass spectrometry data entry: PXD027758 , PXD027755 , PXD027760 , PXD027762 , PXD027756 , PXD027591 , PXD007149 , PXD030064 , PXD032392 , PXD027789 , PXD027767 , PXD027764
7 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
8 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
9 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.
10 An Activity-Guided Map of Electrophile-Cysteine Interactions in Primary Human T Cells. Cell. 2020 Aug 20;182(4):1009-1026.e29. doi: 10.1016/j.cell.2020.07.001. Epub 2020 Jul 29.
11 Accelerating multiplexed profiling of protein-ligand interactions: High-throughput plate-based reactive cysteine profiling with minimal input. Cell Chem Biol. 2024 Mar 21;31(3):565-576.e4. doi: 10.1016/j.chembiol.2023.11.015. Epub 2023 Dec 19.
Mass spectrometry data entry: PXD044402