Details of the Target

General Information of Target

Target ID LDTP13764
Target Name Histone deacetylase 5 (HDAC5)
Gene Name HDAC5
Gene ID 10014
Synonyms
KIAA0600; Histone deacetylase 5; HD5; EC 3.5.1.98; Antigen NY-CO-9
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MSCTRMIQVLDPRPLTSSVMPVDVAMRLCLAHSPPVKSFLGPYDEFQRRHFVNKLKPLKS
CLNIKHKAKSQNDWKCSHNQAKKRVVFADSKGLSLTAIHVFSDLPEEPAWDLQFDLLDLN
DISSALKHHEEKNLILDFPQPSTDYLSFRSHFQKNFVCLENCSLQERTVTGTVKVKNVSF
EKKVQIRITFDSWKNYTDVDCVYMKNVYGGTDSDTFSFAIDLPPVIPTEQKIEFCISYHA
NGQVFWDNNDGQNYRIVHVQWKPDGVQTQMAPQDCAFHQTSPKTELESTIFGSPRLASGL
FPEWQSWGRMENLASYR
Target Type
Patented-recorded
Target Bioclass
Enzyme
Family
Histone deacetylase family, HD type 2 subfamily
Subcellular location
Nucleus
Function
Responsible for the deacetylation of lysine residues on the N-terminal part of the core histones (H2A, H2B, H3 and H4). Histone deacetylation gives a tag for epigenetic repression and plays an important role in transcriptional regulation, cell cycle progression and developmental events. Histone deacetylases act via the formation of large multiprotein complexes. Involved in muscle maturation by repressing transcription of myocyte enhancer MEF2C. During muscle differentiation, it shuttles into the cytoplasm, allowing the expression of myocyte enhancer factors. Involved in the MTA1-mediated epigenetic regulation of ESR1 expression in breast cancer. Serves as a corepressor of RARA and causes its deacetylation. In association with RARA, plays a role in the repression of microRNA-10a and thereby in the inflammatory response.
TTD ID
T07930
Uniprot ID
Q9UQL6
DrugMap ID
TTUELN5
Ensemble ID
ENST00000225983.10
HGNC ID
HGNC:14068
ChEMBL ID
CHEMBL2563

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
HCT15 SNV: p.A478V .
HKGZCC SNV: p.Q559E .
HT115 SNV: p.T31A .
IM95 SNV: p.P358L .
J82 SNV: p.R710G .
JURKAT SNV: p.T335I .
KARPAS422 SNV: p.E566D .
SAOS2 SNV: p.G625V .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 2 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C807(1.05)  LDD1514  [1]
AOyne
 Probe Info  		13.00  LDD0443  [2]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0284  AC24 HEK-293T C807(1.05)  LDD1523  [1]
 LDCM0293  AC32 HEK-293T C807(1.15)  LDD1532  [1]
 LDCM0302  AC40 HEK-293T C807(0.98)  LDD1541  [1]
 LDCM0310  AC48 HEK-293T C807(0.92)  LDD1549  [1]
 LDCM0319  AC56 HEK-293T C807(1.07)  LDD1558  [1]
 LDCM0328  AC64 HEK-293T C807(1.04)  LDD1567  [1]
 LDCM0345  AC8 HEK-293T C807(1.00)  LDD1569  [1]
 LDCM0275  AKOS034007705 HEK-293T C807(1.05)  LDD1514  [1]
 LDCM0367  CL1 HEK-293T C698(1.00)  LDD1571  [1]
 LDCM0370  CL101 HEK-293T C698(0.85)  LDD1574  [1]
 LDCM0374  CL105 HEK-293T C698(0.98)  LDD1578  [1]
 LDCM0378  CL109 HEK-293T C698(0.91)  LDD1582  [1]
 LDCM0383  CL113 HEK-293T C698(0.95)  LDD1587  [1]
 LDCM0387  CL117 HEK-293T C698(0.81)  LDD1591  [1]
 LDCM0390  CL12 HEK-293T C807(1.12)  LDD1594  [1]
 LDCM0392  CL121 HEK-293T C698(0.99)  LDD1596  [1]
 LDCM0396  CL125 HEK-293T C698(0.98)  LDD1600  [1]
 LDCM0400  CL13 HEK-293T C698(0.89)  LDD1604  [1]
 LDCM0412  CL24 HEK-293T C807(1.22)  LDD1616  [1]
 LDCM0413  CL25 HEK-293T C698(0.77)  LDD1617  [1]
 LDCM0425  CL36 HEK-293T C807(1.22)  LDD1629  [1]
 LDCM0426  CL37 HEK-293T C698(0.91)  LDD1630  [1]
 LDCM0438  CL48 HEK-293T C807(1.19)  LDD1642  [1]
 LDCM0439  CL49 HEK-293T C698(1.40)  LDD1643  [1]
 LDCM0452  CL60 HEK-293T C807(1.16)  LDD1655  [1]
 LDCM0453  CL61 HEK-293T C698(0.91)  LDD1656  [1]
 LDCM0465  CL72 HEK-293T C807(1.20)  LDD1668  [1]
 LDCM0466  CL73 HEK-293T C698(1.32)  LDD1669  [1]
 LDCM0478  CL84 HEK-293T C807(1.09)  LDD1681  [1]
 LDCM0479  CL85 HEK-293T C698(1.24)  LDD1682  [1]
 LDCM0491  CL96 HEK-293T C807(1.34)  LDD1694  [1]
 LDCM0492  CL97 HEK-293T C698(0.67)  LDD1695  [1]

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
Histone deacetylase 5 (HDAC5) Histone deacetylase family Q9UQL6
Transporter and channel
Click To Hide/Show 1 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
14-3-3 protein zeta/delta (YWHAZ) 14-3-3 family P63104
Transcription factor
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Myocyte-specific enhancer factor 2C (MEF2C) MEF2 family Q06413
Runt-related transcription factor 3 (RUNX3) . Q13761
Trans-acting T-cell-specific transcription factor GATA-3 (GATA3) . P23771
Other
Click To Hide/Show 3 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
14-3-3 protein sigma (SFN) 14-3-3 family P31947
Breast cancer metastasis-suppressor 1 (BRMS1) BRMS1 family Q9HCU9
Ankyrin repeat family A protein 2 (ANKRA2) . Q9H9E1

The Drug(s) Related To This Target

Approved
Click To Hide/Show 6 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Decitabine Small molecular drug DB01262
Phenylbutyric Acid Small molecular drug DB06819
Propanoic Acid Small molecular drug DB03766
Romidepsin Small molecular drug DB06176
Valproic Acid Small molecular drug DB00313
Vorinostat Small molecular drug DB02546
Investigative
Click To Hide/Show 2 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Abexinostat Small molecular drug DB12565
Tmp269 Small molecular drug D0R7JA
Patented
Click To Hide/Show 7 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid29671355-compound-23 Small molecular drug D00HXJ
Pmid29671355-compound-25 Small molecular drug D0RA0D
Pmid29671355-compound-31 Small molecular drug D0DI9S
Pmid29671355-compound-43 Small molecular drug D0BP8I
Pmid29671355-compound-45a Small molecular drug D0YN2T
Pmid29671355-compound-62 Small molecular drug D07WAT
Pmid29671355-compound-67 Small molecular drug D0M0RE

References

1 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
2 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.