Therapeutic Targets Database
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TTD Target ID: TTDR01156

Target Information
NameHistone deacetylase 2    
Type of targetResearch target    
SynonymsHDAC2    
DiseaseColon cancer
[ICD9: 153, 154   ICD10: C18-C21]
[1]
BioChemical ClassHydrolases acting on carbon-nitrogen bonds    
PathwayCell cycle
Chronic myeloid leukemia
Huntington's disease
Notch signaling pathway
Pathways in cancer
UniProt IDQ92769
PDB Structure3MAX.    
FunctionResponsible 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.    
SequenceMAYSQGGGKKKVCYYYDGDIGNYYYGQGHPMKPHRIRMTHNLLLNYGLYRKMEIYRPHKA TAEEMTKYHSDEYIKFLRSIRPDNMSEYSKQMQRFNVGEDCPVFDGLFEFCQLSTGGSVA GAVKLNRQQTDMAVNWAGGLHHAKKSEASGFCYVNDIVLAILELLKYHQRVLYIDIDIHH GDGVEEAFYTTDRVMTVSFHKYGEYFPGTGDLRDIGAGKGKYYAVNFPMRDGIDDESYGQ IFKPIISKVMEMYQPSAVVLQCGADSLSGDRLGCFNLTVKGHAKCVEVVKTFNLPLLMLG GGGYTIRNVARCWTYETAVALDCEIPNELPYNDYFEYFGPDFKLHISPSNMTNQNTPEYM EKIKQRLFENLRMLPHAPGVQMQAIPEDAVHEDSGDEDGEDPDKRISIRASDKRIACDEE FSDSEDEGEGGRRNVADHKKGAKKARIEEDKKETEDKKTDVKEEDKSKDNSGEKTDTKGT KSEQLSNP
Target ValidationClick to Find Target Validation Information.    
QSAR ModelClick to Find Target QSAR Model.    
Inhibitor (E)-8-Biphenyl-4-yl-1-oxazol-2-yl-oct-7-en-1-one[2]
1,1,1-Trifluoro-8- (4-phenoxy-phenoxy)-octan-2-one[3]
1,1,1-Trifluoro-8-phenoxy-octan-2-one[3]
2- (allyloxy)-N8-hydroxy-N1-phenyloctanediamide[4]
2- (benzyloxy)-N7-hydroxy-N1-phenylheptanediamide[4]
2- (methylsulfonylthio)ethyl 2-propylpentanoate[5]
4-Benzoylamino-N-hydroxy-benzamide[6]
4-Butyrylamino-N-hydroxy-benzamide[7]
4-Chloro-N- (5-hydroxycarbamoyl-pentyl)-benzamide[8]
4-Dimethylamino-N- (6-mercapto-hexyl)-benzamide[9]
4-Hydroxy-N- (5-hydroxycarbamoyl-pentyl)-benzamide[10]
4-Phenylbutyrohydroxamic acid[11]
5- (4-Chloro-phenyl)-pentanoic acid hydroxyamide[12]
5- (4-hydroxyphenyl)-3H-1,2-dithiole-3-thione[5]
5- (Biphenyl-4-yl)-pentanoic acid N-hydroxyamide[13]
5-Mercapto-pentanoic acid phenylamide[9]
6- (2-Bromo-acetylamino)-hexanoic acid phenylamide[9]
6-Mercapto-hexanoic acid phenylamide[9]
6-Phenoxy-hexane-1-thiol[9]
6-benzenesulfinylhexanoic acid hydroxamide[14]
6-benzenesulfonylhexanoic acid hydroxamide[14]
6-phenylsulfanylhexanoic acid hydroxamide[14]
7- (Biphenyl-3-yloxy)-1-oxazol-2-yl-heptan-1-one[2]
7- (Biphenyl-4-yloxy)-1,1,1-trifluoro-heptan-2-one[3]
7- (Biphenyl-4-yloxy)-1-oxazol-2-yl-heptan-1-one[2]
7- (Biphenyl-4-yloxy)-heptanoic acid hydroxyamide[15]
7- (Naphthalen-2-yloxy)-1-oxazol-2-yl-heptan-1-one[2]
7-Biphenyl-4-yl-heptanoic acid hydroxyamide[16]
7-Mercapto-heptanoic acid benzothiazol-2-ylamide[9]
7-Mercapto-heptanoic acid biphenyl-3-ylamide[9]
7-Mercapto-heptanoic acid biphenyl-4-ylamide[9]
7-Mercapto-heptanoic acid phenylamide[9]
7-Mercapto-heptanoic acid pyridin-3-ylamide[9]
7-Mercapto-heptanoic acid quinolin-3-ylamide[9]
7-Phenoxy-heptanoic acid hydroxyamide[16]
8- (Biphenyl-3-yloxy)-1,1,1-trifluoro-octan-2-one[3]
8- (Biphenyl-4-yloxy)-1,1,1-trifluoro-octan-2-one[3]
8- (Biphenyl-4-yloxy)-2-oxo-octanoic acid[15]
8-Mercapto-octanoic acid phenylamide[9]
8-Oxo-8-phenyl-octanoic acid[10]
8-Oxo-8-phenyl-octanoic acid hydroxyamide[8]
8-Phenyl-octanoic acid hydroxyamide[16]
9,9,9-Trifluoro-8-oxo-nonanoic acid phenylamide[3]
9- (Biphenyl-4-yloxy)-1,1,1-trifluoro-nonan-2-one[3]
CI-994[11]
Cyclostellettamine derivative[17]
DEPUDECIN[11]
N- (2-Mercapto-ethyl)-N'-phenyl-oxalamide[18]
N- (2-Mercapto-ethyl)-N'-phenyl-succinamide[18]
N- (2-amino-5-[19]
N- (2-amino-5-[19]
N- (2-amino-5-[19]
N- (2-amino-5-[19]
N- (2-amino-5-[19]
N- (2-amino-5-[20]
N- (2-aminophenyl)-4-methoxybenzamide[21]
N- (2-aminophenyl)benzamide[19]
N- (2-aminophenyl)nicotinamide[20]
N- (2-aminophenyl)quinoxaline-6-carboxamide[21]
N- (3'-acetyl-4-aminobiphenyl-3-yl)benzamide[19]
N- (4'-acetyl-4-aminobiphenyl-3-yl)benzamide[19]
N- (4-amino-3'-methoxybiphenyl-3-yl)benzamide[19]
N- (4-amino-3'-methylbiphenyl-3-yl)benzamide[19]
N- (4-amino-4'-bromobiphenyl-3-yl)benzamide[19]
N- (4-amino-4'-fluorobiphenyl-3-yl)benzamide[19]
N- (4-amino-4'-methoxybiphenyl-3-yl)benzamide[19]
N- (4-amino-4'-vinylbiphenyl-3-yl)benzamide[19]
N- (4-aminobiphenyl-3-yl)benzamide[19]
N- (4-aminobiphenyl-3-yl)nicotinamide[20]
N- (4-hydroxybiphenyl-3-yl)benzamide[20]
N- (5-Hydroxycarbamoyl-pentyl)-4-nitro-benzamide[8]
N- (6-Hydroxycarbamoyl-hexyl)-benzamide[10]
N- (6-Mercapto-hexyl)-benzamide[9]
N-Hydroxy-4- ([6]
N-Hydroxy-4- ([6]
N-Hydroxy-4- (2-phenyl-butyrylamino)-benzamide[6]
N-Hydroxy-4- (4-phenyl-butyrylamino)-benzamide[6]
N-Hydroxy-4- (5-phenyl-pentanoylamino)-benzamide[6]
N-Hydroxy-4- (pentanoylamino-methyl)-benzamide[7]
N-Hydroxy-4- (phenylacetylamino-methyl)-benzamide[7]
N-Hydroxy-4-phenylacetylamino-benzamide[6]
N-Hydroxy-E-3- (4'-chlorobiphenyl-4-yl)-acrylamide[13]
N-Hydroxy-E-3- (4'-cyanobiphenyl-4-yl)-acrylamide[13]
N-Hydroxy-E-3- (biphenyl-4-yl)-acrylamide[13]
N-hydroxy-4- (3-phenylpropanamido)benzamide[22]
N7-hydroxy-2-methoxy-N1-phenylheptanediamide[4]
N7-hydroxy-N1-phenyl-2-propoxyheptanediamide[4]
N8,2-dihydroxy-N1-phenyloctanediamide[4]
N8-hydroxy-2-methoxy-N1-phenyloctanediamide[4]
Octanedioic acid bis-hydroxyamide[23]
Octanedioic acid hydroxyamide pyridin-2-ylamide[10]
Octanedioic acid hydroxyamide pyridin-4-ylamide[10]
PSAMMAPLIN A[8]
ST-2986[24]
ST-2987[24]
Thioacetic acid S- (6-phenylcarbamoyl-hexyl) ester[9]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Induction of HDAC2 expression upon loss of APC in colorectal tumorigenesis. Cancer Cell. 2004 May;5(5):455-63. To Reference
Ref 2Bioorg Med Chem Lett. 2003 Nov 17;13(22):3909-13.Heterocyclic ketones as inhibitors of histone deacetylase. To Reference
Ref 3Bioorg Med Chem Lett. 2002 Dec 2;12(23):3443-7.Trifluoromethyl ketones as inhibitors of histone deacetylase. To Reference
Ref 4Bioorg Med Chem Lett. 2007 Nov 15;17(22):6261-5. Epub 2007 Sep 8.Omega-alkoxy analogues of SAHA (vorinostat) as inhibitors of HDAC: a study of chain-length and stereochemical dependence. To Reference
Ref 5Bioorg Med Chem Lett. 2008 Mar 15;18(6):1893-7. Epub 2008 Feb 8.New sulfurated derivatives of valproic acid with enhanced histone deacetylase inhibitory activity. To Reference
Ref 6J Med Chem. 2005 Aug 25;48(17):5530-5.Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors. To Reference
Ref 7J Med Chem. 2004 Jan 15;47(2):467-74.Zn2+-chelating motif-tethered short-chain fatty acids as a novel class of histone deacetylase inhibitors. To Reference
Ref 8J Med Chem. 2003 Nov 20;46(24):5097-116.Histone deacetylase inhibitors. To Reference
Ref 9J Med Chem. 2005 Feb 24;48(4):1019-32.Novel inhibitors of human histone deacetylases: design, synthesis, enzyme inhibition, and cancer cell growth inhibition of SAHA-based non-hydroxamates. To Reference
Ref 10J Med Chem. 2002 Feb 14;45(4):753-7.Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates. To Reference
Ref 11Nat Chem Biol. 2010 Mar;6(3):238-243. Epub 2010 Feb 7.Chemical phylogenetics of histone deacetylases. To Reference
Ref 12Bioorg Med Chem Lett. 2004 May 17;14(10):2477-81.Stereodefined and polyunsaturated inhibitors of histone deacetylase based on (2E,4E)-5-arylpenta-2,4-dienoic acid hydroxyamides. To Reference
Ref 13Eur J Med Chem. 2009 May;44(5):1900-12. Epub 2008 Nov 19.Design, synthesis, and evaluation of biphenyl-4-yl-acrylohydroxamic acid derivatives as histone deacetylase (HDAC) inhibitors. To Reference
Ref 14J Med Chem. 2006 Jan 26;49(2):800-5.Aromatic sulfide inhibitors of histone deacetylase based on arylsulfinyl-2,4-hexadienoic acid hydroxyamides. To Reference
Ref 15Bioorg Med Chem Lett. 2003 Oct 6;13(19):3331-5.Alpha-keto amides as inhibitors of histone deacetylase. To Reference
Ref 16Bioorg Med Chem Lett. 2003 Nov 3;13(21):3817-20.A novel series of histone deacetylase inhibitors incorporating hetero aromatic ring systems as connection units. To Reference
Ref 17Bioorg Med Chem Lett. 2004 May 17;14(10):2617-20.Three new cyclostellettamines, which inhibit histone deacetylase, from a marine sponge of the genus Xestospongia. To Reference
Ref 18Bioorg Med Chem Lett. 2005 Apr 15;15(8):1969-72.Mercaptoamide-based non-hydroxamic acid type histone deacetylase inhibitors. To Reference
Ref 19Bioorg Med Chem Lett. 2010 May 15;20(10):3142-5. Epub 2010 Mar 30.Exploration of the HDAC2 foot pocket: Synthesis and SAR of substituted N-(2-aminophenyl)benzamides. To Reference
Ref 20Bioorg Med Chem Lett. 2008 Dec 1;18(23):6104-9. Epub 2008 Oct 14.SAR profiles of spirocyclic nicotinamide derived selective HDAC1/HDAC2 inhibitors (SHI-1:2). To Reference
Ref 21J Med Chem. 2007 Nov 15;50(23):5543-6. Epub 2007 Oct 17.Novel aminophenyl benzamide-type histone deacetylase inhibitors with enhanced potency and selectivity. To Reference
Ref 22Eur J Med Chem. 2009 Nov;44(11):4470-6. Epub 2009 Jun 17.Design, synthesis and preliminary biological evaluation of N-hydroxy-4-(3-phenylpropanamido)benzamide (HPPB) derivatives as novel histone deacetylase inhibitors. To Reference
Ref 23J Med Chem. 2002 Jul 18;45(15):3296-309.Structure-activity relationships on phenylalanine-containing inhibitors of histone deacetylase: in vitro enzyme inhibition, induction of differentiation, and inhibition of proliferation in Friend leukemic cells. To Reference
Ref 24Bioorg Med Chem Lett. 2009 Apr 15;19(8):2346-9. Epub 2009 Feb 12.N-Hydroxy-(4-oxime)-cinnamide: a versatile scaffold for the synthesis of novel histone deacetylase [correction of deacetilase] (HDAC) inhibitors. To Reference



 

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