Details of the Target

General Information of Target

Target ID LDTP05004
Target Name Histone H4 (H4C1; H4C2; H4C3; H4C4; H4C5; H4C6; H4C8; H4C9; H4C11; H4C12; H4C13; H4C14; H4C15; H4C16)
Gene Name H4C1; H4C2; H4C3; H4C4; H4C5; H4C6; H4C8; H4C9; H4C11; H4C12; H4C13; H4C14; H4C15; H4C16
Gene ID 121504
Synonyms
H4/A; H4FA; HIST1H4A; H4/I; H4FI; HIST1H4B; H4/G; H4FG; HIST1H4C; H4/B; H4FB; HIST1H4D; H4/J; H4FJ; HIST1H4E; H4/C; H4FC; HIST1H4F; H4/H; H4FH; HIST1H4H; H4/M; H4FM; HIST1H4I; H4/E; H4FE; HIST1H4J; H4/D; H4FD; HIST1H4K; H4/K; H4FK; HIST1H4L; H4/N; H4F2; H4FN; HIST2H4; HIST2H4A; H4/O; H4FO; HIST2H4B; H4-16; HIST4H4; Histone H4
3D Structure
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2D Sequence (FASTA)
Download
3D Structure (PDB)
Download
Sequence
MSGRGKGGKGLGKGGAKRHRKVLRDNIQGITKPAIRRLARRGGVKRISGLIYEETRGVLK
VFLENVIRDAVTYTEHAKRKTVTAMDVVYALKRQGRTLYGFGG
Target Bioclass
Other
Family
Histone H4 family
Subcellular location
Nucleus
Function
Core component of nucleosome. Nucleosomes wrap and compact DNA into chromatin, limiting DNA accessibility to the cellular machineries which require DNA as a template. Histones thereby play a central role in transcription regulation, DNA repair, DNA replication and chromosomal stability. DNA accessibility is regulated via a complex set of post-translational modifications of histones, also called histone code, and nucleosome remodeling.
Uniprot ID
P62805
Ensemble ID
ENST00000244537.6
HGNC ID
HGNC:4781
ChEMBL ID
CHEMBL5876

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 33 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
P1
 Probe Info  		1.70  LDD0452  [2]
P2
 Probe Info  		2.87  LDD0453  [2]
P3
 Probe Info  		1.67  LDD0454  [2]
A-EBA
 Probe Info  		5.34  LDD0215  [3]
ILS-1
 Probe Info  		3.44  LDD0415  [4]
TH211
 Probe Info  		Y89(8.21); Y52(5.05)  LDD0257  [5]
TH214
 Probe Info  		Y89(20.00); Y73(19.93)  LDD0258  [5]
TH216
 Probe Info  		Y73(5.07)  LDD0259  [5]
YN-1
 Probe Info  		2.13  LDD0444  [6]
YN-4
 Probe Info  		100.00  LDD0445  [6]
AZ-9
 Probe Info  		D25(1.15); E54(0.92); E64(1.00); E53(1.00)  LDD2208  [7]
ONAyne
 Probe Info  		K78(0.00); K32(0.00); K80(0.00); K13(0.00)  LDD0273  [8]
OPA-S-S-alkyne
 Probe Info  		K17(2.72); K13(2.72); K92(7.01); K32(7.50)  LDD3494  [9]
Probe 1
 Probe Info  		Y52(15.82); Y73(67.23); Y89(19.86)  LDD3495  [10]
AF-2
 Probe Info  		1.59  LDD0422  [11]
HHS-482
 Probe Info  		Y73(2.36); Y89(1.14)  LDD0285  [12]
HHS-475
 Probe Info  		Y89(0.70); Y73(1.63)  LDD0264  [13]
HHS-465
 Probe Info  		Y73(7.14); Y89(2.01)  LDD2237  [14]
AMP probe
 Probe Info  		N.A.  LDD0200  [15]
ATP probe
 Probe Info  		K92(0.00); K32(0.00); K80(0.00); K78(0.00)  LDD0199  [15]
m-APA
 Probe Info  		N.A.  LDD2231  [16]
CY-1
 Probe Info  		D86(0.00); K92(0.00); M85(0.00); Y89(0.00)  LDD0246  [17]
aONE
 Probe Info  		K78(0.00); K92(0.00)  LDD0002  [18]
1d-yne
 Probe Info  		K80(0.00); K92(0.00)  LDD0356  [19]
NHS
 Probe Info  		K92(0.00); K80(0.00); K32(0.00); K78(0.00)  LDD0010  [18]
OSF
 Probe Info  		N.A.  LDD0029  [20]
SF
 Probe Info  		K92(0.00); Y73(0.00); Y52(0.00); K32(0.00)  LDD0028  [20]
STPyne
 Probe Info  		K92(0.00); K32(0.00); K78(0.00)  LDD0009  [18]
1c-yne
 Probe Info  		N.A.  LDD0228  [19]
Acrolein
 Probe Info  		N.A.  LDD0217  [21]
Crotonaldehyde
 Probe Info  		N.A.  LDD0219  [21]
Methacrolein
 Probe Info  		H76(0.00); K32(0.00)  LDD0218  [21]
W1
 Probe Info  		K32(0.00); K92(0.00); D25(0.00); Y89(0.00)  LDD0236  [22]
PAL-AfBPP Probe
Click To Hide/Show 5 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
STS-2
 Probe Info  		1.55  LDD0138  [23]
Diazir
 Probe Info  		N.A.  LDD0011  [18]
Photocelecoxib
 Probe Info  		Y52(0.00); E54(0.00); E64(0.00); D69(0.00)  LDD0019  [24]
Photoindomethacin
 Probe Info  		N.A.  LDD0155  [24]
DA-2
 Probe Info  		N.A.  LDD0072  [25]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0166  Afatinib A431 1.59  LDD0422  [11]
 LDCM0108  Chloroacetamide HeLa H76(0.00); K32(0.00)  LDD0222  [21]
 LDCM0116  HHS-0101 DM93 Y89(0.70); Y73(1.63)  LDD0264  [13]
 LDCM0117  HHS-0201 DM93 Y89(0.69); Y73(0.73)  LDD0265  [13]
 LDCM0118  HHS-0301 DM93 Y89(0.62); Y73(1.10)  LDD0266  [13]
 LDCM0119  HHS-0401 DM93 Y89(0.67); Y73(0.82)  LDD0267  [13]
 LDCM0120  HHS-0701 DM93 Y89(0.43); Y73(0.76)  LDD0268  [13]
 LDCM0107  IAA HeLa H76(0.00); K32(0.00)  LDD0221  [21]
 LDCM0123  JWB131 DM93 Y73(2.36); Y89(1.14)  LDD0285  [12]
 LDCM0124  JWB142 DM93 Y73(3.70); Y89(1.53)  LDD0286  [12]
 LDCM0125  JWB146 DM93 Y73(1.86); Y89(0.67)  LDD0287  [12]
 LDCM0126  JWB150 DM93 Y73(1.25); Y89(3.80)  LDD0288  [12]
 LDCM0127  JWB152 DM93 Y73(3.32); Y89(2.09)  LDD0289  [12]
 LDCM0128  JWB198 DM93 Y73(1.02); Y89(2.15)  LDD0290  [12]
 LDCM0129  JWB202 DM93 Y73(3.04); Y89(0.46)  LDD0291  [12]
 LDCM0130  JWB211 DM93 Y73(2.06); Y89(1.07)  LDD0292  [12]
 LDCM0109  NEM HeLa N.A.  LDD0223  [21]
 LDCM0110  W12 Hep-G2 K13(0.50); Q28(0.86); K32(0.87); N26(0.94)  LDD0237  [22]
 LDCM0111  W14 Hep-G2 K13(0.65); K78(1.02); H76(1.15); D25(1.19)  LDD0238  [22]
 LDCM0112  W16 Hep-G2 R36(0.92); K32(0.93); Q28(0.95); D25(0.99)  LDD0239  [22]
 LDCM0113  W17 Hep-G2 K60(0.88); N65(0.88); D25(1.01); N26(1.03)  LDD0240  [22]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 16 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Protein arginine N-methyltransferase 1 (PRMT1) Protein arginine N-methyltransferase family Q99873
Protein arginine N-methyltransferase 5 (PRMT5) Protein arginine N-methyltransferase family O14744
N-lysine methyltransferase KMT5A (KMT5A) Histone-lysine methyltransferase family Q9NQR1
Histone acetyltransferase type B catalytic subunit (HAT1) HAT1 family O14929
Histone deacetylase 1 (HDAC1) Histone deacetylase family Q13547
Lysine-specific demethylase 4A (KDM4A) JHDM3 histone demethylase family O75164
DNA replication licensing factor MCM2 (MCM2) MCM family P49736
DNA replication licensing factor MCM3 (MCM3) MCM family P25205
DNA replication licensing factor MCM5 (MCM5) MCM family P33992
Histone acetyltransferase KAT5 (KAT5) MYST (SAS/MOZ) family Q92993
Protein kinase C alpha type (PRKCA) AGC Ser/Thr protein kinase family P17252
E3 ubiquitin-protein ligase SIAH1 (SIAH1) SINA (Seven in absentia) family Q8IUQ4
GTP-binding nuclear protein Ran (RAN) Ran family P62826
SWI/SNF-related matrix-associated actin-dependent regulator of chromatin subfamily A member 5 (SMARCA5) SNF2/RAD54 helicase family O60264
2-oxoglutarate and iron-dependent oxygenase JMJD4 (JMJD4) . Q9H9V9
CREB-binding protein (CREBBP) . Q92793
Transporter and channel
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
14-3-3 protein gamma (YWHAG) 14-3-3 family P61981
14-3-3 protein zeta/delta (YWHAZ) 14-3-3 family P63104
Alpha-actinin-2 (ACTN2) Alpha-actinin family P35609
Huntingtin (HTT) Huntingtin family P42858
Transcription factor
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Lethal(3)malignant brain tumor-like protein 1 (L3MBTL1) . Q9Y468
Peregrin (BRPF1) . P55201
Other
Click To Hide/Show 19 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Histone chaperone ASF1A (ASF1A) ASF1 family Q9Y294
Histone H2A type 1-B/E (H2AC4; H2AC8) Histone H2A family P04908
Histone H2AX (H2AX) Histone H2A family P16104
Histone H3-like centromeric protein A (CENPA) Histone H3 family P49450
Histone H3.1 (H3C1; H3C2; H3C3; H3C4; H3C6; H3C7; H3C8; H3C10; H3C11; H3C12) Histone H3 family P68431
Histone H3.1t (H3-4) Histone H3 family Q16695
Histone H3.2 (H3C15; H3C14; H3C13) Histone H3 family Q71DI3
Histone H3.3 (H3-3A; H3-3B) Histone H3 family P84243
Nucleosome-remodeling factor subunit BPTF (BPTF) PBTF family Q12830
SWI/SNF-related matrix-associated actin-dependent regulator of chromatin subfamily B member 1 (SMARCB1) SNF5 family Q12824
Transducin-like enhancer protein 1 (TLE1) WD repeat Groucho/TLE family Q04724
Histone-binding protein RBBP7 (RBBP7) WD repeat RBAP46/RBAP48/MSI1 family Q16576
Bromodomain-containing protein 2 (BRD2) . P25440
Chromobox protein homolog 5 (CBX5) . P45973
Coordinator of PRMT5 and differentiation stimulator (COPRS) . Q9NQ92
MBT domain-containing protein 1 (MBTD1) . Q05BQ5
PHD finger protein 20 (PHF20) . Q9BVI0
PHD finger protein 20-like protein 1 (PHF20L1) . A8MW92
TP53-binding protein 1 (TP53BP1) . Q12888

References

1 Labeling Preferences of Diazirines with Protein Biomolecules. J Am Chem Soc. 2021 May 5;143(17):6691-6700. doi: 10.1021/jacs.1c02509. Epub 2021 Apr 20.
Mass spectrometry data entry: PXD025140
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 2-Ethynylbenzaldehyde-Based, Lysine-Targeting Irreversible Covalent Inhibitors for Protein Kinases and Nonkinases. J Am Chem Soc. 2023 Feb 12. doi: 10.1021/jacs.2c11595. Online ahead of print.
Mass spectrometry data entry: PXD037665
4 A Chemical Proteomic Analysis of Illudin-Interacting Proteins. Chemistry. 2019 Sep 25;25(54):12644-12651. doi: 10.1002/chem.201902919. Epub 2019 Sep 3.
Mass spectrometry data entry: PXD014175
5 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
6 Ynamide Electrophile for the Profiling of Ligandable Carboxyl Residues in Live Cells and the Development of New Covalent Inhibitors. J Med Chem. 2022 Aug 11;65(15):10408-10418. doi: 10.1021/acs.jmedchem.2c00272. Epub 2022 Jul 26.
7 2H-Azirine-Based Reagents for Chemoselective Bioconjugation at Carboxyl Residues Inside Live Cells. J Am Chem Soc. 2020 Apr 1;142(13):6051-6059. doi: 10.1021/jacs.9b12116. Epub 2020 Mar 23.
8 A Paal-Knorr agent for chemoproteomic profiling of targets of isoketals in cells. Chem Sci. 2021 Oct 15;12(43):14557-14563. doi: 10.1039/d1sc02230j. eCollection 2021 Nov 10.
Mass spectrometry data entry: PXD028270
9 A chemical proteomics approach for global mapping of functional lysines on cell surface of living cell. Nat Commun. 2024 Apr 8;15(1):2997. doi: 10.1038/s41467-024-47033-w.
Mass spectrometry data entry: PXD042888
10 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.
11 Minimalist linkers suitable for irreversible inhibitors in simultaneous proteome profiling, live-cell imaging and drug screening. Chem Commun (Camb). 2019 Jan 15;55(6):834-837. doi: 10.1039/c8cc08685k.
12 Chemoproteomic profiling of kinases in live cells using electrophilic sulfonyl triazole probes. Chem Sci. 2021 Jan 21;12(9):3295-3307. doi: 10.1039/d0sc06623k.
13 Discovery of a Cell-Active SuTEx Ligand of Prostaglandin Reductase 2. Chembiochem. 2021 Jun 15;22(12):2134-2139. doi: 10.1002/cbic.202000879. Epub 2021 Apr 29.
14 Global targeting of functional tyrosines using sulfur-triazole exchange chemistry. Nat Chem Biol. 2020 Feb;16(2):150-159. doi: 10.1038/s41589-019-0404-5. Epub 2019 Nov 25.
15 Targeted Proteomic Approaches for Proteome-Wide Characterizations of the AMP-Binding Capacities of Kinases. J Proteome Res. 2022 Aug 5;21(8):2063-2070. doi: 10.1021/acs.jproteome.2c00225. Epub 2022 Jul 12.
16 Global profiling of functional histidines in live cells using small-molecule photosensitizer and chemical probe relay labelling. Nat Chem. 2024 Jun 4. doi: 10.1038/s41557-024-01545-6. Online ahead of print.
Mass spectrometry data entry: PXD042377
17 Cyclopropenone, Cyclopropeniminium Ion, and Cyclopropenethione as Novel Electrophilic Warheads for Potential Target Discovery of Triple-Negative Breast Cancer. J Med Chem. 2023 Feb 23;66(4):2851-2864. doi: 10.1021/acs.jmedchem.2c01889. Epub 2023 Feb 10.
18 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
19 Tunable Amine-Reactive Electrophiles for Selective Profiling of Lysine. Angew Chem Int Ed Engl. 2022 Jan 26;61(5):e202112107. doi: 10.1002/anie.202112107. Epub 2021 Dec 16.
20 Solid Phase Synthesis of Fluorosulfate Containing Macrocycles for Chemoproteomic Workflows. bioRxiv [Preprint]. 2023 Feb 18:2023.02.17.529022. doi: 10.1101/2023.02.17.529022.
Mass spectrometry data entry: PXD039931
21 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.
22 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.
23 Design and synthesis of minimalist terminal alkyne-containing diazirine photo-crosslinkers and their incorporation into kinase inhibitors for cell- and tissue-based proteome profiling. Angew Chem Int Ed Engl. 2013 Aug 12;52(33):8551-6. doi: 10.1002/anie.201300683. Epub 2013 Jun 10.
24 Small Molecule Interactome Mapping by Photoaffinity Labeling Reveals Binding Site Hotspots for the NSAIDs. J Am Chem Soc. 2018 Mar 28;140(12):4259-4268. doi: 10.1021/jacs.7b11639. Epub 2018 Mar 15.
Mass spectrometry data entry: PXD007094
25 Cell-based proteome profiling of potential dasatinib targets by use of affinity-based probes. J Am Chem Soc. 2012 Feb 15;134(6):3001-14. doi: 10.1021/ja208518u. Epub 2012 Feb 1.