Details of the Target

General Information of Target

Target ID LDTP02390
Target Name Histone H2A.Z (H2AZ1)
Gene Name H2AZ1
Gene ID 3015
Synonyms
H2AFZ; H2AZ; Histone H2A.Z; H2A/z
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MAGGKAGKDSGKAKTKAVSRSQRAGLQFPVGRIHRHLKSRTTSHGRVGATAAVYSAAILE
YLTAEVLELAGNASKDLKVKRITPRHLQLAIRGDEELDSLIKATIAGGGVIPHIHKSLIG
KKGQQKTV
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. May be involved in the formation of constitutive heterochromatin. May be required for chromosome segregation during cell division.
TTD ID
T53766
Uniprot ID
P0C0S5
DrugMap ID
TTQZ1TP
Ensemble ID
ENST00000296417.6
HGNC ID
HGNC:4741

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
TH211
 Probe Info  		Y61(7.95); Y54(7.41)  LDD0257  [1]
STPyne
 Probe Info  		K116(10.00); K126(7.59)  LDD0277  [2]
ONAyne
 Probe Info  		N.A.  LDD0273  [2]
OPA-S-S-alkyne
 Probe Info  		K16(1.12); K14(1.12)  LDD3494  [3]
5E-2FA
 Probe Info  		N.A.  LDD2235  [4]
1c-yne
 Probe Info  		N.A.  LDD0228  [5]
HHS-465
 Probe Info  		N.A.  LDD2240  [6]
PAL-AfBPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
FFF probe3
 Probe Info  		5.54  LDD0464  [7]
STS-1
 Probe Info  		N.A.  LDD0136  [8]
Photocelecoxib
 Probe Info  		N.A.  LDD0019  [9]

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
Fumarate hydratase, mitochondrial (FH) Class-II fumarase/aspartase family P07954
Other
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Actin-related protein 6 (ACTR6) Actin family Q9GZN1
Alpha-2-macroglobulin (A2M) Protease inhibitor I39 (alpha-2-macroglobulin) family P01023
Zinc finger HIT domain-containing protein 1 (ZNHIT1) ZNHIT1 family O43257

References

1 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.
2 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
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 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
5 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.
6 Global profiling identifies a stress-responsive tyrosine site on EDC3 regulating biomolecular condensate formation. Cell Chem Biol. 2022 Dec 15;29(12):1709-1720.e7. doi: 10.1016/j.chembiol.2022.11.008. Epub 2022 Dec 6.
Mass spectrometry data entry: PXD038010
7 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.
8 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.
9 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