Details of the Target

General Information of Target

Target ID LDTP10029
Target Name Polyamine deacetylase HDAC10 (HDAC10)
Gene Name HDAC10
Gene ID 83933
Synonyms
Polyamine deacetylase HDAC10; EC 3.5.1.48; EC 3.5.1.62; Histone deacetylase 10; HD10
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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Sequence
MLFSLRELVQWLGFATFEIFVHLLALLVFSVLLALRVDGLVPGLSWWNVFVPFFAADGLS
TYFTTIVSVRLFQDGEKRLAVLRLFWVLTVLSLKFVFEMLLCQKLAEQTRELWFGLITSP
LFILLQLLMIRACRVN
Target Type
Patented-recorded
Target Bioclass
Enzyme
Family
Histone deacetylase family, HD type 2 subfamily
Subcellular location
Cytoplasm
Function
Polyamine deacetylase (PDAC), which acts preferentially on N(8)-acetylspermidine, and also on acetylcadaverine and acetylputrescine. Exhibits attenuated catalytic activity toward N(1),N(8)-diacetylspermidine and very low activity, if any, toward N(1)-acetylspermidine. Histone deacetylase activity has been observed in vitro. Has also been shown to be involved in MSH2 deacetylation. The physiological relevance of protein/histone deacetylase activity is unclear and could be very weak. May play a role in the promotion of late stages of autophagy, possibly autophagosome-lysosome fusion and/or lysosomal exocytosis in neuroblastoma cells. May play a role in homologous recombination. May promote DNA mismatch repair.
TTD ID
T94324
Uniprot ID
Q969S8
DrugMap ID
TTYHPU6
Ensemble ID
ENST00000216271.10
HGNC ID
HGNC:18128
ChEMBL ID
CHEMBL5103

Target Site Mutations in Different Cell Lines

Cell line Mutation details Probe for labeling this protein in this cell
CHL1 Deletion: p.M367_S368del
Substitution: p.S370P		 .
NCIH146 SNV: p.G627V .
NCIH2172 SNV: p.G269E .
SKNSH SNV: p.A34S .
SNGM SNV: p.G136D .
TOV21G SNV: p.R505M; p.P588S .

Probe(s) Labeling This Target

ABPP Probe
Click To Hide/Show 3 Probe Related to This Target
Probe name Structure Binding Site(Ratio) Interaction ID Ref
DBIA
 Probe Info  		C23(4.39)  LDD0209  [1]
IA-alkyne
 Probe Info  		C403, C405(5.76)  LDD1706  [2]
TFBX
 Probe Info  		C405(0.00); C403(0.00)  LDD0027  [3]

Competitor(s) Related to This Target

Competitor ID Name Cell line Binding Site(Ratio) Interaction ID Ref
 LDCM0022  KB02 22RV1 C145(1.76)  LDD2243  [4]
 LDCM0023  KB03 Jurkat C23(4.39)  LDD0209  [1]
 LDCM0024  KB05 HMCB C145(1.36)  LDD3312  [4]

The Interaction Atlas With This Target

The Protein(s) Related To This Target

Enzyme
Click To Hide/Show 2 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Ataxin-3 (ATXN3) . P54252
Tripartite motif-containing protein 54 (TRIM54) . Q9BYV2
Transporter and channel
Click To Hide/Show 4 Protein(s) Interacting with This Target
Protein name Family Uniprot ID
Huntingtin (HTT) Huntingtin family P42858
Peroxisome assembly protein 26 (PEX26) Peroxin-26 family Q7Z412
Alpha-synuclein (SNCA) Synuclein family P37840
Optineurin (OPTN) . Q96CV9

The Drug(s) Related To This Target

Approved
Click To Hide/Show 7 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
Bufexamac . DB13346
Investigative
Click To Hide/Show 54 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
(E)-8-biphenyl-4-yl-1-oxazol-2-yl-oct-7-en-1-one Small molecular drug D0KE3I
2-(Methylsulfonylthio)Ethyl 2-propylpentanoate Small molecular drug D0H1FZ
4-benzoylamino-n-hydroxy-benzamide Small molecular drug D09ZNU
4-butyrylamino-n-hydroxy-benzamide Small molecular drug D05LLX
4-chloro-n-(5-hydroxycarbamoyl-pentyl)-benzamide Small molecular drug D0A5LS
4-dimethylamino-n-(6-mercapto-hexyl)-benzamide Small molecular drug D06XNP
4-hydroxy-n-(5-hydroxycarbamoyl-pentyl)-benzamide Small molecular drug D04NSP
5-(4-chloro-phenyl)-pentanoic Acid Hydroxyamide Small molecular drug D0V2ZO
5-(4-hydroxyphenyl)-3h-1,2-dithiole-3-thione Small molecular drug D06IQB
5-mercapto-pentanoic Acid Phenylamide Small molecular drug D0D2KE
6-(2-bromo-acetylamino)-hexanoic Acid Phenylamide Small molecular drug D02MQM
6-benzenesulfinylhexanoic Acid Hydroxamide Small molecular drug D00ZSD
6-benzenesulfonylhexanoic Acid Hydroxamide Small molecular drug D05AHZ
6-mercapto-hexanoic Acid Phenylamide Small molecular drug D0B3ZM
6-phenoxy-hexane-1-thiol Small molecular drug D09YBN
6-phenylsulfanylhexanoic Acid Hydroxamide Small molecular drug D0S9JF
7-(Biphenyl-3-yloxy)-1-oxazol-2-yl-heptan-1-one Small molecular drug D0B2ZJ
7-(Biphenyl-4-yloxy)-1,1,1-trifluoro-heptan-2-one Small molecular drug D0Z3BM
7-(Biphenyl-4-yloxy)-1-oxazol-2-yl-heptan-1-one Small molecular drug D02WZK
7-(Naphthalen-2-yloxy)-1-oxazol-2-yl-heptan-1-one Small molecular drug D05VFP
7-mercapto-heptanoic Acid Benzothiazol-2-ylamide Small molecular drug D0Z5KX
7-mercapto-heptanoic Acid Biphenyl-3-ylamide Small molecular drug D05XAN
7-mercapto-heptanoic Acid Biphenyl-4-ylamide Small molecular drug D01XWZ
7-mercapto-heptanoic Acid Phenylamide Small molecular drug D00SEE
7-mercapto-heptanoic Acid Pyridin-3-ylamide Small molecular drug D07FJU
7-mercapto-heptanoic Acid Quinolin-3-ylamide Small molecular drug D0T4IY
8-(Biphenyl-4-yloxy)-1,1,1-trifluoro-octan-2-one Small molecular drug D0AX7B
8-mercapto-octanoic Acid Phenylamide Small molecular drug D0XZ9Q
8-oxo-8-phenyl-octanoic Acid Small molecular drug D0RU1X
9,9,9-trifluoro-8-oxo-nonanoic Acid Phenylamide Small molecular drug D00KFF
9-(Biphenyl-4-yloxy)-1,1,1-trifluoro-nonan-2-one Small molecular drug D05FEJ
Abexinostat Small molecular drug DB12565
Cyclostellettamine Derivative Small molecular drug D0C0VP
N-(2-mercapto-ethyl)-n'-phenyl-oxalamide Small molecular drug D0F0KS
N-(2-mercapto-ethyl)-n'-phenyl-succinamide Small molecular drug D01MFV
N-(5-hydroxycarbamoyl-pentyl)-4-nitro-benzamide Small molecular drug D0C2KD
N-(6-hydroxycarbamoyl-hexyl)-benzamide Small molecular drug D0YY9M
N-(6-mercapto-hexyl)-benzamide Small molecular drug D04HSS
N-hydroxy-4-((R)-2-phenyl-butyrylamino)-benzamide Small molecular drug D04ZDI
N-hydroxy-4-((S)-2-phenyl-butyrylamino)-benzamide Small molecular drug D0QO0L
N-hydroxy-4-(2-phenyl-butyrylamino)-benzamide Small molecular drug D06VBN
N-hydroxy-4-(4-phenyl-butyrylamino)-benzamide Small molecular drug D0S7WQ
N-hydroxy-4-(5-phenyl-pentanoylamino)-benzamide Small molecular drug D0R5VG
N-hydroxy-4-(Pentanoylamino-methyl)-benzamide Small molecular drug D0Z7YS
N-hydroxy-4-(Phenylacetylamino-methyl)-benzamide Small molecular drug D02UTC
N-hydroxy-4-phenylacetylamino-benzamide Small molecular drug D01XXN
Octanedioic Acid Hydroxyamide Pyridin-2-ylamide Small molecular drug D0E8KR
Octanedioic Acid Hydroxyamide Pyridin-4-ylamide Small molecular drug D04GGW
Psammaplin A Small molecular drug D0N0TS
St-2986 Small molecular drug D0N9AK
St-2987 Small molecular drug D0T0SK
St-3050 Small molecular drug D01YBR
Thioacetic Acid S-(6-phenylcarbamoyl-hexyl) Ester Small molecular drug D05GVY
N-hydroxy-4-(3-phenyl-propionylamino)-benzamide . D0R4BS
Patented
Click To Hide/Show 7 Drug(s) Interacting with This Target
Drug Name Drug Type External ID
Pmid29671355-compound-21 Small molecular drug D0LP1K
Pmid29671355-compound-25 Small molecular drug D0RA0D
Pmid29671355-compound-43 Small molecular drug D0BP8I
Pmid29671355-compound-44 Small molecular drug D0N2DK
Pmid29671355-compound-56 Small molecular drug D0CH8Q
Pmid29671355-compound-62 Small molecular drug D07WAT
Pmid29671355-compound-8 Small molecular drug D0LN1T

References

1 Covalent Inhibition by a Natural Product-Inspired Latent Electrophile. J Am Chem Soc. 2023 May 24;145(20):11097-11109. doi: 10.1021/jacs.3c00598. Epub 2023 May 15.
2 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.
3 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
4 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