Therapeutic Targets Database
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TTD Target ID: TTDR01167

Target Information
NameHistone deacetylase 6    
Type of targetResearch target    
SynonymsHD6    
DiseaseMultiple myeloma
[ICD9: 203.0   ICD10: C90.0]
[1]
EC NumberEC 3.5.1.98
UniProt IDQ9UBN7
PDB Structure3C5K; 3GV4; 3PHD.    
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 and developmental events. Histone deacetylases act via the formation of large multiprotein complexes. Plays a central role in microtubuldependent cell motility via deacetylation of tubulin.    
SequenceMTSTGQDSTTTRQRRSRQNPQSPPQDSSVTSKRNIKKGAVPRSIPNLAEVKKKGKMKKLG QAMEEDLIVGLQGMDLNLEAEALAGTGLVLDEQLNEFHCLWDDSFPEGPERLHAIKEQLI QEGLLDRCVSFQARFAEKEELMLVHSLEYIDLMETTQYMNEGELRVLADTYDSVYLHPNS YSCACLASGSVLRLVDAVLGAEIRNGMAIIRPPGHHAQHSLMDGYCMFNHVAVAARYAQQ KHRIRRVLIVDWDVHHGQGTQFTFDQDPSVLYFSIHRYEQGRFWPHLKASNWSTTGFGQG QGYTINVPWNQVGMRDADYIAAFLHVLLPVALEFQPQLVLVAAGFDALQGDPKGEMAATP AGFAQLTHLLMGLAGGKLILSLEGGYNLRALAEGVSASLHTLLGDPCPMLESPGAPCRSA QASVSCALEALEPFWEVLVRSTETVERDNMEEDNVEESEEEGPWEPPVLPILTWPVLQSR TGLVYDQNMMNHCNLWDSHHPEVPQRILRIMCRLEELGLAGRCLTLTPRPATEAELLTCH SAEYVGHLRATEKMKTRELHRESSNFDSIYICPSTFACAQLATGAACRLVEAVLSGEVLN GAAVVRPPGHHAEQDAACGFCFFNSVAVAARHAQTISGHALRILIVDWDVHHGNGTQHMF EDDPSVLYVSLHRYDHGTFFPMGDEGASSQIGRAAGTGFTVNVAWNGPRMGDADYLAAWH RLVLPIAYEFNPELVLVSAGFDAARGDPLGGCQVSPEGYAHLTHLLMGLASGRIILILEG GYNLTSISESMAACTRSLLGDPPPLLTLPRPPLSGALASITETIQVHRRYWRSLRVMKVE DREGPSSSKLVTKKAPQPAKPRLAERMTTREKKVLEAGMGKVTSASFGEESTPGQTNSET AVVALTQDQPSEAATGGATLAQTISEAAIGGAMLGQTTSEEAVGGATPDQTTSEETVGGA ILDQTTSEDAVGGATLGQTTSEEAVGGATLAQTTSEAAMEGATLDQTTSEEAPGGTELIQ TPLASSTDHQTPPTSPVQGTTPQISPSTLIGSLRTLELGSESQGASESQAPGEENLLGEA AGGQDMADSMLMQGSRGLTDQAIFYAVTPLPWCPHLVAVCPIPAAGLDVTQPCGDCGTIQ ENWVCLSCYQVYCGRYINGHMLQHHGNSGHPLVLSYIDLSAWCYYCQAYVHHQALLDVKN IAHQNKFGEDMPHPH//
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]
(S)-2-Amino-N-cyclopentyl-7-mercaptoheptanamide[3]
2- (methylsulfonylthio)ethyl 2-propylpentanoate[4]
4-Benzoylamino-N-hydroxy-benzamide[5]
4-Butyrylamino-N-hydroxy-benzamide[6]
4-Chloro-N- (5-hydroxycarbamoyl-pentyl)-benzamide[7]
4-Dimethylamino-N- (6-mercapto-hexyl)-benzamide[8]
4-Hydroxy-N- (5-hydroxycarbamoyl-pentyl)-benzamide[9]
4-Phenylbutyrohydroxamic acid[10]
5- (4-Chloro-phenyl)-pentanoic acid hydroxyamide[11]
5- (4-hydroxyphenyl)-3H-1,2-dithiole-3-thione[4]
5-Mercapto-pentanoic acid phenylamide[8]
6- (2-Bromo-acetylamino)-hexanoic acid phenylamide[8]
6- (9H-carbazol-9-yl)-N-hydroxyhexanamide[12]
6-Mercapto-hexanoic acid phenylamide[8]
6-Phenoxy-hexane-1-thiol[8]
6-benzenesulfinylhexanoic acid hydroxamide[13]
6-benzenesulfonylhexanoic acid hydroxamide[13]
6-phenylsulfanylhexanoic acid hydroxamide[13]
7- (Biphenyl-3-yloxy)-1-oxazol-2-yl-heptan-1-one[2]
7- (Biphenyl-4-yloxy)-1,1,1-trifluoro-heptan-2-one[7]
7- (Biphenyl-4-yloxy)-1-oxazol-2-yl-heptan-1-one[2]
7- (Naphthalen-2-yloxy)-1-oxazol-2-yl-heptan-1-one[2]
7-Mercapto-heptanoic acid benzothiazol-2-ylamide[8]
7-Mercapto-heptanoic acid biphenyl-3-ylamide[8]
7-Mercapto-heptanoic acid biphenyl-4-ylamide[8]
7-Mercapto-heptanoic acid phenylamide[8]
7-Mercapto-heptanoic acid pyridin-3-ylamide[8]
7-Mercapto-heptanoic acid quinolin-3-ylamide[8]
7-mercapto-N- (4-phenylthiazol-2-yl)heptanamide[3]
8- (Biphenyl-4-yloxy)-1,1,1-trifluoro-octan-2-one[2]
8-Mercapto-octanoic acid phenylamide[8]
8-Oxo-8-phenyl-octanoic acid[9]
8-Oxo-8-phenyl-octanoic acid hydroxyamide[7]
9,9,9-Trifluoro-8-oxo-nonanoic acid phenylamide[7]
9- (Biphenyl-4-yloxy)-1,1,1-trifluoro-nonan-2-one[7]
Cyclostellettamine derivative[14]
N- (2-Mercapto-ethyl)-N'-phenyl-oxalamide[15]
N- (2-Mercapto-ethyl)-N'-phenyl-succinamide[15]
N- (5-Hydroxycarbamoyl-pentyl)-4-nitro-benzamide[7]
N- (6-Hydroxycarbamoyl-hexyl)-benzamide[9]
N- (6-Mercapto-hexyl)-benzamide[8]
N- (biphenyl-3-yl)-6-[16]
N- (quinolin-3-yl)-6-[16]
N- (quinolin-6-yl)-6-[16]
N- (quinolin-8-yl)-6-[16]
N-Hydroxy-4- ([5]
N-Hydroxy-4- ([5]
N-Hydroxy-4- (2-phenyl-butyrylamino)-benzamide[5]
N-Hydroxy-4- (3-phenyl-propionylamino)-benzamide[5]
N-Hydroxy-4- (4-phenyl-butyrylamino)-benzamide[5]
N-Hydroxy-4- (5-phenyl-pentanoylamino)-benzamide[5]
N-Hydroxy-4- (pentanoylamino-methyl)-benzamide[6]
N-Hydroxy-4- (phenylacetylamino-methyl)-benzamide[6]
N-Hydroxy-4-phenylacetylamino-benzamide[5]
N-[5- (Formyl-hydroxy-amino)-pentyl]-benzamide[17]
N-phenyl-6- (sulfamoylamino)hexanamide[16]
N1- (biphenyl-3-yl)-N8-hydroxyoctanediamide[16]
N1- (biphenyl-4-yl)-N8-hydroxyoctanediamide[18]
N1-hydroxy-N8- (4-phenylthiazol-2-yl)octanediamide[18]
NILTUBACIN[10]
Octanedioic acid bis-hydroxyamide[19]
Octanedioic acid hydroxyamide pyridin-2-ylamide[9]
Octanedioic acid hydroxyamide pyridin-4-ylamide[9]
PSAMMAPLIN A[7]
ST-2741[20]
ST-2986[21]
ST-2987[21]
ST-3050[21]
Thioacetic acid S- (6-phenylcarbamoyl-hexyl) ester[8]
Tubacin[1][22]
cyclo (-L-Am7[23]
cyclo (-L-Am7[23]
cyclo (-L-Am7[23]
cyclo (-L-Am7[23]
cyclo (-L-Am7[23]
cyclo (-L-Am7[23]
cyclo (-L-Am7[23]
cyclo (-L-Am7[23]
cyclo (-L-Am7[23]
cyclo (-L-Am7[23]
cyclo (-L-Am7[23]
cyclo (-L-Am7[23]
cyclo (-L-Am7[23]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127. To Reference
Ref 2Bioorg Med Chem Lett. 2003 Nov 17;13(22):3909-13.Heterocyclic ketones as inhibitors of histone deacetylase. To Reference
Ref 3J Med Chem. 2007 Nov 1;50(22):5425-38. Epub 2007 Oct 11.Design, synthesis, structure--selectivity relationship, and effect on human cancer cells of a novel series of histone deacetylase 6-selective inhibitors. To Reference
Ref 4Bioorg 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 5J Med Chem. 2005 Aug 25;48(17):5530-5.Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors. To Reference
Ref 6J 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 7J Med Chem. 2003 Nov 20;46(24):5097-116.Histone deacetylase inhibitors. To Reference
Ref 8J 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 9J 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 10Nat Chem Biol. 2010 Mar;6(3):238-243. Epub 2010 Feb 7.Chemical phylogenetics of histone deacetylases. To Reference
Ref 11Bioorg 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 12Bioorg Med Chem Lett. 2010 Dec 1;20(23):7067-70. Epub 2010 Oct 12.Inhibitors selective for HDAC6 in enzymes and cells. To Reference
Ref 13J 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 14Bioorg 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 15Bioorg Med Chem Lett. 2005 Apr 15;15(8):1969-72.Mercaptoamide-based non-hydroxamic acid type histone deacetylase inhibitors. To Reference
Ref 16Bioorg Med Chem Lett. 2009 Jan 15;19(2):336-40. Epub 2008 Nov 27.Sulfamides as novel histone deacetylase inhibitors. To Reference
Ref 17Bioorg Med Chem Lett. 2004 Jan 19;14(2):449-53.Design, synthesis, and activity of HDAC inhibitors with a N-formyl hydroxylamine head group. To Reference
Ref 18Bioorg Med Chem Lett. 2009 Jun 1;19(11):3023-6. Epub 2009 Apr 20.Isoxazole moiety in the linker region of HDAC inhibitors adjacent to the Zn-chelating group: effects on HDAC biology and antiproliferative activity. To Reference
Ref 19J 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 20Bioorg Med Chem Lett. 2009 May 15;19(10):2840-3. Epub 2009 Mar 26.Exploring bis-(indolyl)methane moiety as an alternative and innovative CAP group in the design of histone deacetylase (HDAC) inhibitors. To Reference
Ref 21Bioorg 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
Ref 22Nat Rev Drug Discov. 2006 Sep;5(9):769-84.Anticancer activities of histone deacetylase inhibitors. To Reference
Ref 23Bioorg Med Chem. 2007 Dec 15;15(24):7830-9. Epub 2007 Aug 26.Molecular design of histone deacetylase inhibitors by aromatic ring shifting in chlamydocin framework. To Reference



 

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