Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTYHPU6)

• DTT Name: Histone deacetylase 10 (HDAC10)
• Synonyms: Polyamine deacetylase HDAC10; HD10
• Gene Name: HDAC10
• DTT Type: Patented-recorded target; [1]
• Related Disease: Solid tumour/cancer [ICD-11: 2A00-2F9Z]
• BioChemical Class: Carbon-nitrogen hydrolase
• UniProt ID: HDA10_HUMAN
• TTD ID: T94324
• EC Number: EC 3.5.1.48
• Sequence:
  MGTALVYHEDMTATRLLWDDPECEIERPERLTAALDRLRQRGLEQRCLRLSAREASEEEL
  GLVHSPEYVSLVRETQVLGKEELQALSGQFDAIYFHPSTFHCARLAAGAGLQLVDAVLTG
  AVQNGLALVRPPGHHGQRAAANGFCVFNNVAIAAAHAKQKHGLHRILVVDWDVHHGQGIQ
  YLFEDDPSVLYFSWHRYEHGRFWPFLRESDADAVGRGQGLGFTVNLPWNQVGMGNADYVA
  AFLHLLLPLAFEFDPELVLVSAGFDSAIGDPEGQMQATPECFAHLTQLLQVLAGGRVCAV
  LEGGYHLESLAESVCMTVQTLLGDPAPPLSGPMAPCQSALESIQSARAAQAPHWKSLQQQ
  DVTAVPMSPSSHSPEGRPPPLLPGGPVCKAAASAPSSLLDQPCLCPAPSVRTAVALTTPD
  ITLVLPPDVIQQEASALREETEAWARPHESLAREEALTALGKLLYLLDGMLDGQVNSGIA
  ATPASAAAATLDVAVRRGLSHGAQRLLCVALGQLDRPPDLAHDGRSLWLNIRGKEAAALS
  MFHVSTPLPVMTGGFLSCILGLVLPLAYGFQPDLVLVALGPGHGLQGPHAALLAAMLRGL
  AGGRVLALLEENSTPQLAGILARVLNGEAPPSLGPSSVASPEDVQALMYLRGQLEPQWKM
  LQCHPHLVA
• Function: 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. Polyamine deacetylase (PDAC), which acts preferentially on N(8)-acetylspermidine, and also on acetylcadaverine and acetylputrescine.
• KEGG Pathway:
  Neutrophil extracellular trap formation (hsa04613)
  Alcoholism (hsa05034)
  Viral carcinogenesis (hsa05203)
• Reactome Pathway:
  Constitutive Signaling by NOTCH1 PEST Domain Mutants (R-HSA-2644606)
  Constitutive Signaling by NOTCH1 HD+PEST Domain Mutants (R-HSA-2894862)
  HDACs deacetylate histones (R-HSA-3214815)
  Notch-HLH transcription pathway (R-HSA-350054)
  NOTCH1 Intracellular Domain Regulates Transcription (R-HSA-2122947)

Molecular Interaction Atlas (MIA) of This DTT

7 Patented Agent(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
PMID29671355-Compound-21	DMPJN0M	N. A.	N. A.	Patented	[1]
PMID29671355-Compound-25	DMPV0KZ	N. A.	N. A.	Patented	[1]
PMID29671355-Compound-43	DMVPMWJ	N. A.	N. A.	Patented	[1]
PMID29671355-Compound-44	DM80A3V	N. A.	N. A.	Patented	[1]
PMID29671355-Compound-56	DM0VBMI	N. A.	N. A.	Patented	[1]
PMID29671355-Compound-62	DMWRS34	N. A.	N. A.	Patented	[1]
PMID29671355-Compound-8	DM7YQJK	N. A.	N. A.	Patented	[1]

53 Investigative Drug(s) Targeting This DTT

Drug Name	Drug ID	Indication	ICD 11	Highest Status	REF
(E)-8-Biphenyl-4-yl-1-oxazol-2-yl-oct-7-en-1-one	DM5LSY9	Discovery agent	N.A.	Investigative	[2]
2-(methylsulfonylthio)ethyl 2-propylpentanoate	DMM52D3	Discovery agent	N.A.	Investigative	[3]
4-Benzoylamino-N-hydroxy-benzamide	DMYBPFS	Discovery agent	N.A.	Investigative	[4]
4-Butyrylamino-N-hydroxy-benzamide	DMRY6B4	Discovery agent	N.A.	Investigative	[5]
4-Chloro-N-(5-hydroxycarbamoyl-pentyl)-benzamide	DM5AVG3	Discovery agent	N.A.	Investigative	[6]
4-Dimethylamino-N-(6-mercapto-hexyl)-benzamide	DM0M8G5	Discovery agent	N.A.	Investigative	[7]
4-Hydroxy-N-(5-hydroxycarbamoyl-pentyl)-benzamide	DMULOHZ	Discovery agent	N.A.	Investigative	[6]
5-(4-Chloro-phenyl)-pentanoic acid hydroxyamide	DM6CRVS	Discovery agent	N.A.	Investigative	[8]
5-(4-hydroxyphenyl)-3H-1,2-dithiole-3-thione	DM7KQXL	Discovery agent	N.A.	Investigative	[3]
5-Mercapto-pentanoic acid phenylamide	DMET3OJ	Discovery agent	N.A.	Investigative	[7]
6-(2-Bromo-acetylamino)-hexanoic acid phenylamide	DM9LKXD	Discovery agent	N.A.	Investigative	[7]
6-benzenesulfinylhexanoic acid hydroxamide	DM2I95Z	Discovery agent	N.A.	Investigative	[9]
6-benzenesulfonylhexanoic acid hydroxamide	DMY9IK8	Discovery agent	N.A.	Investigative	[9]
6-Mercapto-hexanoic acid phenylamide	DMD2FW9	Discovery agent	N.A.	Investigative	[7]
6-Phenoxy-hexane-1-thiol	DMVYIN2	Discovery agent	N.A.	Investigative	[7]
6-phenylsulfanylhexanoic acid hydroxamide	DM3OLM6	Discovery agent	N.A.	Investigative	[9]
7-(Biphenyl-3-yloxy)-1-oxazol-2-yl-heptan-1-one	DMLCGSY	Discovery agent	N.A.	Investigative	[2]
7-(Biphenyl-4-yloxy)-1,1,1-trifluoro-heptan-2-one	DM28GZ7	Discovery agent	N.A.	Investigative	[10]
7-(Biphenyl-4-yloxy)-1-oxazol-2-yl-heptan-1-one	DMY027P	Discovery agent	N.A.	Investigative	[2]
7-(Naphthalen-2-yloxy)-1-oxazol-2-yl-heptan-1-one	DM4VQN8	Discovery agent	N.A.	Investigative	[2]
7-Mercapto-heptanoic acid benzothiazol-2-ylamide	DMPYTHV	Discovery agent	N.A.	Investigative	[7]
7-Mercapto-heptanoic acid biphenyl-3-ylamide	DMEQKPO	Discovery agent	N.A.	Investigative	[7]
7-Mercapto-heptanoic acid biphenyl-4-ylamide	DMJMOUK	Discovery agent	N.A.	Investigative	[7]
7-Mercapto-heptanoic acid phenylamide	DM4912P	Discovery agent	N.A.	Investigative	[7]
7-Mercapto-heptanoic acid pyridin-3-ylamide	DMQ9PLA	Discovery agent	N.A.	Investigative	[7]
7-Mercapto-heptanoic acid quinolin-3-ylamide	DMTAGJ1	Discovery agent	N.A.	Investigative	[7]
8-(Biphenyl-4-yloxy)-1,1,1-trifluoro-octan-2-one	DM23XGW	Discovery agent	N.A.	Investigative	[2]
8-Mercapto-octanoic acid phenylamide	DMD3FWU	Discovery agent	N.A.	Investigative	[7]
8-Oxo-8-phenyl-octanoic acid	DMXDQ25	Discovery agent	N.A.	Investigative	[6]
9,9,9-Trifluoro-8-oxo-nonanoic acid phenylamide	DMVBCID	Discovery agent	N.A.	Investigative	[10]
9-(Biphenyl-4-yloxy)-1,1,1-trifluoro-nonan-2-one	DMIY3D6	Discovery agent	N.A.	Investigative	[10]
Cyclostellettamine derivative	DMFTDPQ	Discovery agent	N.A.	Investigative	[11]
N-(2-Mercapto-ethyl)-N'-phenyl-oxalamide	DM0GOPV	Discovery agent	N.A.	Investigative	[12]
N-(2-Mercapto-ethyl)-N'-phenyl-succinamide	DMJLFOQ	Discovery agent	N.A.	Investigative	[12]
N-(5-Hydroxycarbamoyl-pentyl)-4-nitro-benzamide	DMSUW7M	Discovery agent	N.A.	Investigative	[6]
N-(6-Hydroxycarbamoyl-hexyl)-benzamide	DMIZVMT	Discovery agent	N.A.	Investigative	[6]
N-(6-Mercapto-hexyl)-benzamide	DM01Y37	Discovery agent	N.A.	Investigative	[7]
N-Hydroxy-4-((R)-2-phenyl-butyrylamino)-benzamide	DMCN91A	Discovery agent	N.A.	Investigative	[4]
N-Hydroxy-4-((S)-2-phenyl-butyrylamino)-benzamide	DMVK2Y3	Discovery agent	N.A.	Investigative	[4]
N-Hydroxy-4-(2-phenyl-butyrylamino)-benzamide	DMHEQ41	Discovery agent	N.A.	Investigative	[4]
N-Hydroxy-4-(3-phenyl-propionylamino)-benzamide	DMUOCQB	Discovery agent	N.A.	Investigative	[4]
N-Hydroxy-4-(4-phenyl-butyrylamino)-benzamide	DMVEOBY	Discovery agent	N.A.	Investigative	[4]
N-Hydroxy-4-(5-phenyl-pentanoylamino)-benzamide	DMISRMT	Discovery agent	N.A.	Investigative	[4]
N-Hydroxy-4-(pentanoylamino-methyl)-benzamide	DMGTNQY	Discovery agent	N.A.	Investigative	[5]
N-Hydroxy-4-(phenylacetylamino-methyl)-benzamide	DMDUOH4	Discovery agent	N.A.	Investigative	[5]
N-Hydroxy-4-phenylacetylamino-benzamide	DMCRU17	Discovery agent	N.A.	Investigative	[4]
Octanedioic acid hydroxyamide pyridin-2-ylamide	DMHNWS1	Discovery agent	N.A.	Investigative	[6]
Octanedioic acid hydroxyamide pyridin-4-ylamide	DM945RK	Discovery agent	N.A.	Investigative	[6]
PSAMMAPLIN A	DM6T0IQ	Discovery agent	N.A.	Investigative	[10]
ST-2986	DMNERM6	Discovery agent	N.A.	Investigative	[13]
ST-2987	DMWXTM8	Solid tumour/cancer	2A00-2F9Z	Investigative	[13]
ST-3050	DM19K2D	Discovery agent	N.A.	Investigative	[13]
Thioacetic acid S-(6-phenylcarbamoyl-hexyl) ester	DMBOKSF	Discovery agent	N.A.	Investigative	[7]

References

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• [4] Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors. J Med Chem. 2005 Aug 25;48(17):5530-5.
• [5] Zn2+-chelating motif-tethered short-chain fatty acids as a novel class of histone deacetylase inhibitors. J Med Chem. 2004 Jan 15;47(2):467-74.
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• [7] Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxama... J Med Chem. 2005 Feb 24;48(4):1019-32.
• [8] Stereodefined and polyunsaturated inhibitors of histone deacetylase based on (2E,4E)-5-arylpenta-2,4-dienoic acid hydroxyamides. Bioorg Med Chem Lett. 2004 May 17;14(10):2477-81.
• [9] Aromatic sulfide inhibitors of histone deacetylase based on arylsulfinyl-2,4-hexadienoic acid hydroxyamides. J Med Chem. 2006 Jan 26;49(2):800-5.
• [10] Histone deacetylase inhibitors. J Med Chem. 2003 Nov 20;46(24):5097-116.
• [11] Three new cyclostellettamines, which inhibit histone deacetylase, from a marine sponge of the genus Xestospongia. Bioorg Med Chem Lett. 2004 May 17;14(10):2617-20.
• [12] Mercaptoamide-based non-hydroxamic acid type histone deacetylase inhibitors. Bioorg Med Chem Lett. 2005 Apr 15;15(8):1969-72.
• [13] N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors. Bioorg Med Chem Lett. 2009 Apr 15;19(8):2346-9.