Details of the Target

General Information of Target

Target ID LDTP02825
Target Name Histone H2AX (H2AX)
Gene Name H2AX
Gene ID 3014
Synonyms
H2AFX; Histone H2AX; H2a/x; Histone H2A.X
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSGRGKTGGKARAKAKSRSSRAGLQFPVGRVHRLLRKGHYAERVGAGAPVYLAAVLEYLT
AEILELAGNAARDNKKTRIIPRHLQLAIRNDEELNKLLGGVTIAQGGVLPNIQAVLLPKK
TSATVGPKAPSGGKKATQASQEY
Target Type
Literature-reported
Target Bioclass
Other
Family
Histone H2A family
Subcellular location
Nucleus
Function
Variant histone H2A which replaces conventional H2A in a subset of nucleosomes. 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. Required for checkpoint-mediated arrest of cell cycle progression in response to low doses of ionizing radiation and for efficient repair of DNA double strand breaks (DSBs) specifically when modified by C-terminal phosphorylation.
TTD ID
T55244
Uniprot ID
P16104
DrugMap ID
TTNQTLJ
Ensemble ID
ENST00000375167.1
HGNC ID
HGNC:4739

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
STPyne
 Probe Info  		K120(6.22); K128(5.42); K134(9.74); K37(8.04)  LDD0277  [1]
AZ-9
 Probe Info  		E92(1.09)  LDD2208  [2]
ONAyne
 Probe Info  		N.A.  LDD0273  [1]
OPA-S-S-alkyne
 Probe Info  		K37(2.89)  LDD3494  [3]
Acrolein
 Probe Info  		N.A.  LDD0222  [4]
NHS
 Probe Info  		N.A.  LDD0010  [5]
SF
 Probe Info  		Y40(0.00); K37(0.00); Y143(0.00)  LDD0028  [6]
1c-yne
 Probe Info  		N.A.  LDD0228  [7]
1d-yne
 Probe Info  		K119(0.00); K128(0.00); K96(0.00)  LDD0357  [7]
Crotonaldehyde
 Probe Info  		N.A.  LDD0219  [4]
Methacrolein
 Probe Info  		N.A.  LDD0218  [4]
PAL-AfBPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
C292
 Probe Info  		5.98  LDD1962  [8]
C361
 Probe Info  		18.90  LDD2022  [8]
FFF probe4
 Probe Info  		5.16  LDD0466  [9]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0108  Chloroacetamide HeLa N.A.  LDD0222  [4]
 LDCM0109  NEM HeLa N.A.  LDD0227  [4]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 6 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Double-strand break repair protein MRE11 (MRE11) MRE11/RAD32 family P49959
Protein phosphatase 1D (PPM1D) PP2C family O15297
Serine/threonine-protein kinase VRK1 (VRK1) CK1 Ser/Thr protein kinase family Q99986
Mitogen-activated protein kinase 8 (MAPK8) CMGC Ser/Thr protein kinase family P45983
Transcription activator BRG1 (SMARCA4) SNF2/RAD54 helicase family P51532
Breast cancer type 1 susceptibility protein (BRCA1) . P38398
Other
Click To Hide/Show 8 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Histone H2B type 1-D (H2BC5) Histone H2B family P58876
Histone H3.1t (H3-4) Histone H3 family Q16695
Histone H4 (H4C1; H4C2; H4C3; H4C4; H4C5; H4C6; H4C8; H4C9; H4C11; H4C12; H4C13; H4C14; H4C15; H4C16) Histone H4 family P62805
Prelamin-A/C (LMNA) Intermediate filament family P02545
Mediator of DNA damage checkpoint protein 1 (MDC1) . Q14676
Nibrin (NBN) . O60934
Telomeric repeat-binding factor 2 (TERF2) . Q15554
TP53-binding protein 1 (TP53BP1) . Q12888

References

1 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
2 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.
3 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
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 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
6 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
7 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.
8 Large-scale chemoproteomics expedites ligand discovery and predicts ligand behavior in cells. Science. 2024 Apr 26;384(6694):eadk5864. doi: 10.1126/science.adk5864. Epub 2024 Apr 26.
Mass spectrometry data entry: PXD041587
9 Ligand and Target Discovery by Fragment-Based Screening in Human Cells. Cell. 2017 Jan 26;168(3):527-541.e29. doi: 10.1016/j.cell.2016.12.029. Epub 2017 Jan 19.