Target General Infomation
Target ID
T68547
Former ID
TTDS00095
Target Name
Histone deacetylase 1
Gene Name
HDAC1
Synonyms
HDAC1
Target Type
Successful
Disease Acute myeloid leukemia; Refractory sickle cell ulcers [ICD9:205, 282.5, 282.6; ICD10: C92.0, D57]
Cancer [ICD9: 140-229; ICD10: C00-C96]
Cutaneous T-cell lymphoma [ICD9: 202.1, 202.2; ICD10: C84.0, C84.1]
Cerebrovascular ischaemia [ICD9: 434.91; ICD10: I61-I63]
Friedreich's ataxia [ICD9: 334; ICD10: G11.1]
General leukaemia cancer [ICD9: 204-208; ICD10: C91-C95]
Hepatocellular carcinoma [ICD9: 155; ICD10: C22.0]
Hodgkin's lymphoma; Multiple myeloma [ICD9: 201, 202.8, 203.0; ICD10: C81, C81-C86, C90]
Melanoma [ICD9: 172; ICD10: C43]
Myelofibrosis; Essential thrombocythemia; Polycythemia vera [ICD9: 238.71, 289.0, 289.83, 289.9, 776.4; ICD10: C94.4, D47.1, D47.3, D75.1, D75.2, D75.8, P61.1]
Primary myelofibrosis; Post-polycythemia vera; Post-essential thrombocytopenia; Cutaneous T cell-lymphomas [ICD9: 203.0, 287.3, 287.4, 287.5, 289.0, 289.83, 776.4; ICD10: C90.0, C94.4, D47.1, D69.6, D75.1, P61.0, P61.1]
Peripheral T-cell lymphoma [ICD9: 202.7; ICD10: C84.4]
Renal cell carcinoma; Hormone refractory prostate cancer [ICD9: 140-229, 185, 189, 203.0, 205.0; ICD10: C61, C64, C90.0, C92.0]
Solid tumours [ICD9: 140-199, 210-229; ICD10: C00-D48]
Severe mood disorders [ICD9: 296; ICD10: F30-F39]
Type 2 diabetes [ICD9: 250; ICD10: E11]
Urea cycle disorders [ICD9: 270.6; ICD10: E72.2]
Unspecified [ICD code not available]
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 transcriptionalregulation, cell cycle progression and developmental events. Histone deacetylases act via the formation of large multiprotein complexes. Deacetylates SP proteins, SP1 and SP3, and regulates their function. Component of the BRG1-RB1-HDAC1 complex, which negatively regulates the CREST- mediated transcription in resting neurons. Upon calcium stimulation, HDAC1 is released from the complex and CREBBPis recruited, which facilitates transcriptional activation. Deacetylates TSHZ3 and regulates its transcriptional repressor activity. Deacetylates 'Lys-310' in RELA and thereby inhibits the transcriptional activity of NF-kappa-B. Deacetylates NR1D2 and abrogates the effect of KAT5-mediated relieving of NR1D2 transcription repression activity. Component of a RCOR/GFI/KDM1A/HDAC complex that suppresses, via histone deacetylase (HDAC) recruitment, a number of genes implicated in multilineage blood cell development. Involved in CIART-mediated transcriptional repression of the circadian transcriptional activator: CLOCK-ARNTL/BMAL1 heterodimer. Required for the transcriptional repression of circadian target genes, such as PER1, mediated by the large PER complex or CRY1 through histone deacetylation.
BioChemical Class
Carbon-nitrogen hydrolase
Target Validation
T68547
UniProt ID
EC Number
EC 3.5.1.98
Sequence
MAQTQGTRRKVCYYYDGDVGNYYYGQGHPMKPHRIRMTHNLLLNYGLYRKMEIYRPHKAN
AEEMTKYHSDDYIKFLRSIRPDNMSEYSKQMQRFNVGEDCPVFDGLFEFCQLSTGGSVAS
AVKLNKQQTDIAVNWAGGLHHAKKSEASGFCYVNDIVLAILELLKYHQRVLYIDIDIHHG
DGVEEAFYTTDRVMTVSFHKYGEYFPGTGDLRDIGAGKGKYYAVNYPLRDGIDDESYEAI
FKPVMSKVMEMFQPSAVVLQCGSDSLSGDRLGCFNLTIKGHAKCVEFVKSFNLPMLMLGG
GGYTIRNVARCWTYETAVALDTEIPNELPYNDYFEYFGPDFKLHISPSNMTNQNTNEYLE
KIKQRLFENLRMLPHAPGVQMQAIPEDAIPEESGDEDEDDPDKRISICSSDKRIACEEEF
SDSEEEGEGGRKNSSNFKKAKRVKTEDEKEKDPEEKKEVTEEEKTKEEKPEAKGVKEEVK
LA
Drugs and Mode of Action
Drug(s) Panobinostat Drug Info Approved Multiple myeloma [1]
Romidepsin Drug Info Approved Cutaneous T-cell lymphoma [2], [3]
Vorinostat Drug Info Approved Cutaneous T-cell lymphoma [4], [5]
HBI-8000 Drug Info Registered Cancer [6], [7]
NVP-LAQ824 Drug Info Phase 3 Severe mood disorders [8]
Panobinostat Drug Info Phase 3 Type 2 diabetes [9], [10]
Romidepsin Drug Info Phase 3 Renal cell carcinoma; Hormone refractory prostate cancer [2], [3]
ITF2357 Drug Info Phase 2 Myelofibrosis; Essential thrombocythemia; Polycythemia vera [11], [12]
MGCD-0103 Drug Info Phase 2 Solid tumours [13], [14]
Panobinostat Drug Info Phase 2 Primary myelofibrosis; Post-polycythemia vera; Post-essential thrombocytopenia; Cutaneous T cell-lymphomas [4], [10]
Phenylbutyrate Drug Info Phase 2 Urea cycle disorders [15], [16]
Resminostat Drug Info Phase 2 Hepatocellular carcinoma [17], [18]
Romidepsin Drug Info Phase 2 Peripheral T-cell lymphoma [2], [3]
SB-623 Drug Info Phase 2 Cerebrovascular ischaemia [19]
SNDX-275 Drug Info Phase 2 Hodgkin's lymphoma; Multiple myeloma [20], [21]
Sodium butyrate Drug Info Phase 2 Acute myeloid leukemia; Refractory sickle cell ulcers [22]
CHR-3996 Drug Info Phase 1 Solid tumours [23], [24]
OBP-801 Drug Info Phase 1 Cancer [25]
RG-2833 Drug Info Phase 1 Friedreich's ataxia [26], [27]
SB-639 Drug Info Phase 1 Cancer [28]
4SC-202 Drug Info Preclinical Cancer [18]
Chlamydocin Drug Info Preclinical Cancer [29]
Depudecin Drug Info Preclinical Cancer [30]
HC-Toxin Drug Info Preclinical Cancer [31]
M-carboxycinnamic acid bishydroxamide Drug Info Preclinical Cancer [32]
Scriptaid Drug Info Preclinical Cancer [15], [33]
SK-7041 Drug Info Preclinical Cancer [34]
SK-7068 Drug Info Preclinical Cancer [34]
AN-9 Drug Info Discontinued in Phase 2 Melanoma [35]
Tacedinaline Drug Info Discontinued in Phase 2 Cancer [36], [37]
NVP-LAQ824 Drug Info Discontinued in Phase 1/2 General leukaemia cancer [8]
Pyroxamide Drug Info Discontinued in Phase 1 Cancer [38]
Oxamflatin Drug Info Terminated Cancer [39]
Inhibitor (E)-8-Biphenyl-4-yl-1-oxazol-2-yl-oct-7-en-1-one Drug Info [40]
1,1,1-Trifluoro-8-(4-phenoxy-phenoxy)-octan-2-one Drug Info [41]
1,1,1-Trifluoro-8-phenoxy-octan-2-one Drug Info [41]
2-(methylsulfonylthio)ethyl 2-propylpentanoate Drug Info [42]
4-Benzenesulfonylamino-N-hydroxy-benzamide Drug Info [43]
4-Benzoylamino-N-hydroxy-benzamide Drug Info [44]
4-Butyrylamino-N-hydroxy-benzamide Drug Info [45]
4-Chloro-N-(5-hydroxycarbamoyl-pentyl)-benzamide Drug Info [46]
4-Dimethylamino-N-(6-mercapto-hexyl)-benzamide Drug Info [47]
4-Hydroxy-N-(5-hydroxycarbamoyl-pentyl)-benzamide Drug Info [48]
4-Phenylbutyrohydroxamic acid Drug Info [49]
4-tert-butyl-N-hydroxybenzamide Drug Info [50]
4SC-202 Drug Info [18]
5-(4-Chloro-phenyl)-pentanoic acid hydroxyamide Drug Info [51]
5-(4-hydroxyphenyl)-3H-1,2-dithiole-3-thione Drug Info [42]
5-Mercapto-pentanoic acid phenylamide Drug Info [47]
6-(2-Bromo-acetylamino)-hexanoic acid phenylamide Drug Info [47]
6-(3-Benzoyl-ureido)-hexanoic acid hydroxyamide Drug Info [52]
6-(9H-carbazol-9-yl)-N-hydroxyhexanamide Drug Info [53]
6-benzenesulfinylhexanoic acid hydroxamide Drug Info [54]
6-benzenesulfonylhexanoic acid hydroxamide Drug Info [54]
6-Mercapto-hexanoic acid phenylamide Drug Info [47]
6-Phenoxy-hexane-1-thiol Drug Info [47]
6-phenylsulfanylhexanoic acid hydroxamide Drug Info [54]
7-(1H-indol-5-yloxy)-N-hydroxyheptanamide Drug Info [55]
7-(3-Benzoyl-ureido)-heptanoic acid hydroxyamide Drug Info [52]
7-(4-(dimethylamino)phenoxy)-N-hydroxyheptanamide Drug Info [55]
7-(Biphenyl-3-yloxy)-1-oxazol-2-yl-heptan-1-one Drug Info [40]
7-(Biphenyl-4-yloxy)-1,1,1-trifluoro-heptan-2-one Drug Info [41]
7-(Biphenyl-4-yloxy)-1-oxazol-2-yl-heptan-1-one Drug Info [40]
7-(Biphenyl-4-yloxy)-heptanoic acid hydroxyamide Drug Info [56]
7-(Naphthalen-2-yloxy)-1-oxazol-2-yl-heptan-1-one Drug Info [40]
7-Biphenyl-4-yl-heptanoic acid hydroxyamide Drug Info [57]
7-Mercapto-heptanoic acid benzothiazol-2-ylamide Drug Info [47]
7-Mercapto-heptanoic acid biphenyl-3-ylamide Drug Info [47]
7-Mercapto-heptanoic acid biphenyl-4-ylamide Drug Info [47]
7-Mercapto-heptanoic acid phenylamide Drug Info [47]
7-Mercapto-heptanoic acid pyridin-3-ylamide Drug Info [47]
7-Mercapto-heptanoic acid quinolin-3-ylamide Drug Info [47]
7-mercapto-N-(4-phenylthiazol-2-yl)heptanamide Drug Info [58]
7-Phenoxy-heptanoic acid hydroxyamide Drug Info [57]
8-(3-Benzoyl-ureido)-octanoic acid hydroxyamide Drug Info [52]
8-(4-bromophenyl)-N-hydroxy-8-oxooctanamide Drug Info [59]
8-(Biphenyl-3-yloxy)-1,1,1-trifluoro-octan-2-one Drug Info [41]
8-(biphenyl-4-yl)-N-hydroxy-8-oxooctanamide Drug Info [59]
8-(Biphenyl-4-yloxy)-1,1,1-trifluoro-octan-2-one Drug Info [41]
8-(Biphenyl-4-yloxy)-2-oxo-octanoic acid Drug Info [56]
8-Mercapto-octanoic acid phenylamide Drug Info [47]
8-Oxo-8-phenyl-octanoic acid Drug Info [48]
8-Oxo-8-phenyl-octanoic acid hydroxyamide Drug Info [46]
8-Phenyl-octanoic acid hydroxyamide Drug Info [57]
9,9,9-Trifluoro-8-oxo-nonanoic acid phenylamide Drug Info [41]
9-(Biphenyl-4-yloxy)-1,1,1-trifluoro-nonan-2-one Drug Info [41]
ADS-100380 Drug Info [60]
ADS-102550 Drug Info [60]
AN-9 Drug Info [61]
Azithromycin-N-benzyltriazolyldecahydroxamic Acid Drug Info [62]
Azithromycin-N-benzyltriazolylhexahydroxamic Acid Drug Info [62]
Azithromycin-N-benzyltriazolylnonahydroxamic Acid Drug Info [62]
Azithromycin-N-benzyltriazolyloctahydroxamic Acid Drug Info [62]
Azithromycinarylalkylhydroxamic Acid Drug Info [62]
AZUMAMIDE B Drug Info [63]
AZUMAMIDE C Drug Info [63]
AZUMAMIDE E Drug Info [63]
Chlamydocin Drug Info [64]
CHR-3996 Drug Info [23]
Cyclo(-L-Am7(S2Py)-A2in-L-Ala-D-Pro-) Drug Info [65]
Cyclo(-L-Am7(S2Py)-Aib-L-Ala-D-Pro-) Drug Info [65]
Cyclo(-L-Am7(S2Py)-Aib-L-Ala-D-Tic-) Drug Info [65]
Cyclo(-L-Am7(S2Py)-Aib-L-Ph4-D-Pro-) Drug Info [65]
Cyclo(-L-Am7(S2Py)-Aib-L-Ph5-D-Pro-) Drug Info [65]
Cyclo(-L-Am7(S2Py)-Aib-L-Phe-D-Pro-) Drug Info [65]
Cyclo(-L-Am7(S2Py)-Aib-L-Phg-D-Pro-) Drug Info [65]
Cyclo(-L-Am7(S2Py)-Aib-L-Ser(Bzl)-D-Pro-) Drug Info [65]
Cyclo(-L-Am7(S2Py)-Aib-L-Ser-D-Pro-) Drug Info [65]
Cyclo(-L-Am7(S2Py)-D-2MePhe-L-Ala-D-Pro-) Drug Info [65]
Cyclo(-L-Am7(S2Py)-D-A1in-L-Ala-D-Pro-) Drug Info [65]
Cyclo(-L-Am7(S2Py)-L-2MePhe-L-Ala-D-Pro-) Drug Info [65]
Cyclo(-L-Am7(S2Py)-L-A1in-L-Ala-D-Pro-) Drug Info [65]
Cyclostellettamine derivative Drug Info [66]
Depudecin Drug Info [61], [64]
Desclasinose Azithromycinarylalkyl Hydroxamate Drug Info [62]
Gymnochrome E Drug Info [67]
HC-Toxin Drug Info [64]
ITF2357 Drug Info [4], [11]
LARGAZOLE Drug Info [68]
M-carboxycinnamic acid bishydroxamide Drug Info [61], [64]
MGCD-0103 Drug Info [61], [64], [69]
N,8-dihydroxy-8-(naphthalen-2-yl)octanamide Drug Info [59]
N-(2,3-Dimethylphenyl)-N'-hydroxyoctanediamide Drug Info [70]
N-(2,4-Dimethylphenyl)-N'-hydroxyoctanediamide Drug Info [70]
N-(2,5-Dimethylphenyl)-N'-hydroxyoctanediamide Drug Info [70]
N-(2,6-Dimethylphenyl)-N'-hydroxyoctanediamide Drug Info [70]
N-(2-amino-5-(thiophen-2-yl)phenyl)nicotinamide Drug Info [71]
N-(2-aminophenyl)-4-(chroman-3-ylmethyl)benzamide Drug Info [72]
N-(2-aminophenyl)-4-methoxybenzamide Drug Info [73]
N-(2-aminophenyl)nicotinamide Drug Info [71]
N-(2-aminophenyl)quinoxaline-6-carboxamide Drug Info [73]
N-(2-Ethylphenyl)-N'-hydroxyoctanediamide Drug Info [70]
N-(2-Mercapto-ethyl)-N'-phenyl-oxalamide Drug Info [74]
N-(2-Mercapto-ethyl)-N'-phenyl-succinamide Drug Info [74]
N-(3,4-Dimethylphenyl)-N'-hydroxyoctanediamide Drug Info [70]
N-(3,5-Dimethylphenyl)-N'-hydroxyoctanediamide Drug Info [70]
N-(3-Ethylphenyl)-N'-hydroxyoctanediamide Drug Info [70]
N-(4-aminobiphenyl-3-yl)nicotinamide Drug Info [71]
N-(4-Ethylphenyl)-N'-hydroxyoctanediamide Drug Info [70]
N-(4-hydroxybiphenyl-3-yl)benzamide Drug Info [71]
N-(5-Hydroxycarbamoyl-pentyl)-4-nitro-benzamide Drug Info [46]
N-(6-Hydroxycarbamoyl-hexyl)-benzamide Drug Info [48]
N-(6-Mercapto-hexyl)-benzamide Drug Info [47]
N-hydroxy-2,2'-bithiophene-5-carboxamide Drug Info [60]
N-Hydroxy-4-((R)-2-phenyl-butyrylamino)-benzamide Drug Info [44]
N-Hydroxy-4-((S)-2-phenyl-butyrylamino)-benzamide Drug Info [44]
N-Hydroxy-4-(2-phenyl-butyrylamino)-benzamide Drug Info [44]
N-Hydroxy-4-(3-phenyl-propionylamino)-benzamide Drug Info [75]
N-Hydroxy-4-(4-phenyl-butyrylamino)-benzamide Drug Info [44]
N-Hydroxy-4-(5-phenyl-pentanoylamino)-benzamide Drug Info [44]
N-Hydroxy-4-(pentanoylamino-methyl)-benzamide Drug Info [45]
N-Hydroxy-4-(phenylacetylamino-methyl)-benzamide Drug Info [45]
N-Hydroxy-4-phenylacetylamino-benzamide Drug Info [44]
N-hydroxy-5-(pyridin-2-yl)thiophene-2-carboxamide Drug Info [60]
N-hydroxy-5-(pyridin-3-yl)thiophene-2-carboxamide Drug Info [60]
N-hydroxy-5-(pyridin-4-yl)thiophene-2-carboxamide Drug Info [60]
N-hydroxy-5-phenylthiophene-2-carboxamide Drug Info [60]
N-hydroxy-6-oxo-6-phenylhexanamide Drug Info [59]
N-hydroxy-7-(4-methoxyphenyl)-7-oxoheptanamide Drug Info [59]
N-hydroxy-7-(naphthalen-2-yl)-7-oxoheptanamide Drug Info [59]
N-hydroxy-7-(naphthalen-2-yloxy)heptanamide Drug Info [55]
N-hydroxy-7-oxo-7-phenylheptanamide Drug Info [59]
N-hydroxy-8-(2-methoxyphenyl)-8-oxooctanamide Drug Info [59]
N-hydroxy-8-(4-methoxyphenyl)-8-oxooctanamide Drug Info [59]
N-hydroxy-8-(naphthalen-2-yl)non-8-enamide Drug Info [59]
N-hydroxy-8-(naphthalen-2-yl)oct-7-enamide Drug Info [59]
N-hydroxy-8-(naphthalen-2-yl)octanamide Drug Info [59]
N-hydroxy-8-oxo-8-(pyridin-3-yl)octanamide Drug Info [59]
N-hydroxy-9-oxo-9-phenylnonanamide Drug Info [59]
N-Hydroxy-N'-(2-methylphenyl)octanediamide Drug Info [70]
N-Hydroxy-N'-(3-methylphenyl)octanediamide Drug Info [70]
N-Hydroxy-N'-(4-methoxyphenyl)octanediamide Drug Info [70]
N-Hydroxy-N'-(4-methylphenyl)octanediamide Drug Info [70]
N-hydroxybenzo[b]thiophene-2-carboxamide Drug Info [76]
N1-(biphenyl-3-yl)-N8-hydroxyoctanediamide Drug Info [77]
N1-(biphenyl-4-yl)-N8-hydroxyoctanediamide Drug Info [78]
N1-hydroxy-N8-(4-phenylthiazol-2-yl)octanediamide Drug Info [78]
nexturastat A Drug Info [79]
NSC-746457 Drug Info [80]
NVP-LAQ824 Drug Info [81]
OBP-801 Drug Info [82]
Octanedioic acid bis-hydroxyamide Drug Info [83]
Octanedioic acid hydroxyamide pyridin-2-ylamide Drug Info [48]
Octanedioic acid hydroxyamide pyridin-4-ylamide Drug Info [48]
Oxamflatin Drug Info [61], [64]
Panobinostat Drug Info [61], [64], [84], [69]
Phenylbutyrate Drug Info [15]
PSAMMAPLIN A Drug Info [46]
Pyroxamide Drug Info [61], [64]
Resminostat Drug Info [18]
Romidepsin Drug Info [2]
SB-623 Drug Info [64]
SB-639 Drug Info [64]
Scriptaid Drug Info [61], [15], [64]
SK-683 Drug Info [85]
SK-7041 Drug Info [61], [64]
SK-7068 Drug Info [61], [64]
SNDX-275 Drug Info [4]
Sodium butyrate Drug Info [86], [61]
ST-2986 Drug Info [87]
ST-2987 Drug Info [87]
ST-3050 Drug Info [87]
Tacedinaline Drug Info [61], [64]
Thioacetic acid S-(6-phenylcarbamoyl-hexyl) ester Drug Info [47]
Vorinostat Drug Info [61], [88], [69]
Modulator HBI-8000 Drug Info [89]
histone deacetylase-1 inhibitors (cancer) Drug Info [90]
RG-2833 Drug Info [89]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
KEGG Pathway Cell cycle
Notch signaling pathway
Thyroid hormone signaling pathway
Huntington&#039
s disease
Amphetamine addiction
Alcoholism
Epstein-Barr virus infection
Pathways in cancer
Transcriptional misregulation in cancer
Viral carcinogenesis
MicroRNAs in cancer
Chronic myeloid leukemia
NetPath Pathway TCR Signaling Pathway
PANTHER Pathway Wnt signaling pathway
p53 pathway
Pathway Interaction Database Regulation of nuclear SMAD2/3 signaling
Notch signaling pathway
E2F transcription factor network
Presenilin action in Notch and Wnt signaling
Signaling events mediated by HDAC Class I
Regulation of Telomerase
Glucocorticoid receptor regulatory network
Sumoylation by RanBP2 regulates transcriptional repression
Regulation of Androgen receptor activity
IL3-mediated signaling events
Validated nuclear estrogen receptor alpha network
Retinoic acid receptors-mediated signaling
Hedgehog signaling events mediated by Gli proteins
Regulation of nuclear beta catenin signaling and target gene transcription
Validated targets of C-MYC transcriptional repression
Regulation of retinoblastoma protein
Notch-mediated HES/HEY network
Reactome G0 and Early G1
p75NTR negatively regulates cell cycle via SC1
TCF transactivating complex
NOTCH1 Intracellular Domain Regulates Transcription
SMAD4 heterotrimer regulates transcription
Constitutive Signaling by NOTCH1 PEST Domain Mutants
Constitutive Signaling by NOTCH1 HD+PEST Domain Mutants
HDACs deacetylate histones
Deactivation of the beta-catenin transactivating complex
NoRC negatively regulates rRNA expression
RNA Polymerase I Transcription Initiation
Factors involved in megakaryocyte development and platelet production
WikiPathways SIDS Susceptibility Pathways
Notch Signaling Pathway
TGF beta Signaling Pathway
IL-6 signaling pathway
Apoptosis-related network due to altered Notch3 in ovarian cancer
SMAD4 heterotrimer
Notch Signaling Pathway
Retinoblastoma (RB) in Cancer
Neural Crest Differentiation
TWEAK Signaling Pathway
Integrated Breast Cancer Pathway
Signalling by NGF
RNA Polymerase I, RNA Polymerase III, and Mitochondrial Transcription
Mitotic G1-G1/S phases
Factors involved in megakaryocyte development and platelet production
Cell Cycle
Androgen receptor signaling pathway
References
REF 1Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
REF 2Hughes B: 2009 FDA drug approvals. Nat Rev Drug Discov. 2010 Feb;9(2):89-92.
REF 3(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7006).
REF 4Emerging therapies for multiple myeloma. Expert Opin Emerg Drugs. 2009 Mar;14(1):99-127.
REF 5(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 6852).
REF 6(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8305).
REF 7Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025931)
REF 8Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2.
REF 9Progress of HDAC inhibitor panobinostat in the treatment of cancer. Curr Drug Targets. 2014 Jun;15(6):622-34.
REF 10(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7489).
REF 11Emerging drugs for the therapy of primary and post essential thrombocythemia, post polycythemia vera myelofibrosis. Expert Opin Emerg Drugs. 2009 Jun 24.
REF 12(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7490).
REF 13MGCD0103, a novel isotype-selective histone deacetylase inhibitor, has broad spectrum antitumor activity in vitro and in vivo. Mol Cancer Ther. 2008 Apr;7(4):759-68.
REF 14(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7008).
REF 15Emerging disease-modifying therapies for the treatment of motor neuron disease/amyotropic lateral sclerosis. Expert Opin Emerg Drugs. 2007 May;12(2):229-52.
REF 16(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8480).
REF 17(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7502).
REF 182011 Pipeline of 4SC AG.
REF 19ClinicalTrials.gov (NCT02448641) Study of Modified Stem Cells (SB623) in Patients With Chronic Motor Deficit From Ischemic Stroke. U.S. National Institutes of Health.
REF 20(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7007).
REF 21Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012663)
REF 22The enhancement of phase 2 enzyme activities by sodium butyrate in normal intestinal epithelial cells is associated with Nrf2 and p53. Mol Cell Biochem. 2012 Nov;370(1-2):7-14.
REF 23A phase I pharmacokinetic and pharmacodynamic study of CHR-3996, an oral class I selective histone deacetylase inhibitor in refractory solid tumors. Clin Cancer Res. 2012 May 1;18(9):2687-94.
REF 24(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8391).
REF 25ClinicalTrials.gov (NCT02414516) A Dose-Escalation Study of OBP-801 in Patients With Advanced Solid Tumors. U.S. National Institutes of Health.
REF 26(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7501).
REF 27Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800035788)
REF 28Epigenetics in vascular disease - therapeutic potential of new agents. Curr Vasc Pharmacol. 2014 Jan;12(1):77-86.
REF 29Preclinical and clinical studies of clindamycin-2-phosphate (author's transl). Jpn J Antibiot. 1977 Jan;30(1):42-50.
REF 30HDAC inhibitors repress the polycomb protein BMI1. Cell Cycle. 2010 Jul 15; 9(14): 2722-2730.
REF 31Inhibition of maize histone deacetylases by HC toxin, the host-selective toxin of Cochliobolus carbonum. Plant Cell. 1995 Nov;7(11):1941-50.
REF 32Selective extraction of an intrinsic fat-cell plasma-membrane glycoprotein by Triton X-100. Correlation with [3H]cytochalasin B binding activity. FEBS Lett. 1977 Nov 1;83(1):71-5.
REF 33(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7505).
REF 34Class I histone deacetylase-selective novel synthetic inhibitors potently inhibit human tumor proliferation. Clin Cancer Res. 2004 Aug 1;10(15):5271-81.
REF 35Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004320)
REF 36(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 8367).
REF 37Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002525)
REF 38Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018698)
REF 39Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007547)
REF 40Bioorg Med Chem Lett. 2003 Nov 17;13(22):3909-13.Heterocyclic ketones as inhibitors of histone deacetylase.
REF 41Bioorg Med Chem Lett. 2002 Dec 2;12(23):3443-7.Trifluoromethyl ketones as inhibitors of histone deacetylase.
REF 42Bioorg 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.
REF 43Bioorg Med Chem Lett. 2001 Nov 5;11(21):2847-50.Design and synthesis of a novel class of histone deacetylase inhibitors.
REF 44J Med Chem. 2005 Aug 25;48(17):5530-5.Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors.
REF 45J 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.
REF 46J Med Chem. 2003 Nov 20;46(24):5097-116.Histone deacetylase inhibitors.
REF 47J 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.
REF 48J Med Chem. 2002 Feb 14;45(4):753-7.Inhibitors of human histone deacetylase: synthesis and enzyme and cellular activity of straight chain hydroxamates.
REF 49Nat Chem Biol. 2010 Mar;6(3):238-243. Epub 2010 Feb 7.Chemical phylogenetics of histone deacetylases.
REF 50Bioorg Med Chem Lett. 2007 Aug 15;17(16):4619-24. Epub 2007 May 27.Design of novel histone deacetylase inhibitors.
REF 51Bioorg 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.
REF 52Bioorg Med Chem Lett. 2010 Jun 1;20(11):3314-21. Epub 2010 Apr 14.Acylurea connected straight chain hydroxamates as novel histone deacetylase inhibitors: Synthesis, SAR, and in vivo antitumor activity.
REF 53Bioorg Med Chem Lett. 2010 Dec 1;20(23):7067-70. Epub 2010 Oct 12.Inhibitors selective for HDAC6 in enzymes and cells.
REF 54J Med Chem. 2006 Jan 26;49(2):800-5.Aromatic sulfide inhibitors of histone deacetylase based on arylsulfinyl-2,4-hexadienoic acid hydroxyamides.
REF 55Bioorg Med Chem Lett. 2007 Jan 1;17(1):136-41. Epub 2006 Sep 30.Structure-activity relationships of aryloxyalkanoic acid hydroxyamides as potent inhibitors of histone deacetylase.
REF 56Bioorg Med Chem Lett. 2003 Oct 6;13(19):3331-5.Alpha-keto amides as inhibitors of histone deacetylase.
REF 57Bioorg 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.
REF 58J 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.
REF 59Eur J Med Chem. 2009 Jul;44(7):2868-76. Epub 2008 Dec 16.3D-QSAR studies of HDACs inhibitors using pharmacophore-based alignment.
REF 60Bioorg Med Chem Lett. 2007 Jan 15;17(2):363-9. Epub 2006 Oct 24.Identification and optimisation of a series of substituted 5-pyridin-2-yl-thiophene-2-hydroxamic acids as potent histone deacetylase (HDAC) inhibitors.
REF 61Anticancer activities of histone deacetylase inhibitors. Nat Rev Drug Discov. 2006 Sep;5(9):769-84.
REF 62J Med Chem. 2009 Jan 22;52(2):456-68.Non-peptide macrocyclic histone deacetylase inhibitors.
REF 63Bioorg Med Chem Lett. 2008 May 1;18(9):2982-4. Epub 2008 Mar 21.Evaluation of antiangiogenic activity of azumamides by the in vitro vascular organization model using mouse induced pluripotent stem (iPS) cells.
REF 64Histone deacetylase inhibitors in cancer therapy: latest developments, trends and medicinal chemistry perspective. Anticancer Agents Med Chem. 2007 Sep;7(5):576-92.
REF 65Bioorg 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.
REF 66Bioorg 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.
REF 67J Nat Prod. 2010 Apr 23;73(4):712-5.Gymnochromes E and F, cytotoxic phenanthroperylenequinones from a deep-water crinoid, Holopus rangii.
REF 68J Med Chem. 2010 Jun 24;53(12):4654-67.Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues.
REF 69Protein methyltransferases as a target class for drug discovery. Nat Rev Drug Discov. 2009 Sep;8(9):724-32.
REF 70J Med Chem. 2010 Mar 11;53(5):1937-50.Biological and biophysical properties of the histone deacetylase inhibitor suberoylanilide hydroxamic acid are affected by the presence of short alkyl groups on the phenyl ring.
REF 71Bioorg 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).
REF 72Bioorg Med Chem Lett. 2007 Dec 15;17(24):6729-33. Epub 2007 Oct 18.N-(2-Amino-phenyl)-4-(heteroarylmethyl)-benzamides as new histone deacetylase inhibitors.
REF 73J 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.
REF 74Bioorg Med Chem Lett. 2005 Apr 15;15(8):1969-72.Mercaptoamide-based non-hydroxamic acid type histone deacetylase inhibitors.
REF 75Eur 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.
REF 76J Med Chem. 2008 Mar 27;51(6):1505-29. Epub 2008 Feb 5.Histone deacetylase inhibitors: from bench to clinic.
REF 77Bioorg Med Chem Lett. 2009 Jan 15;19(2):336-40. Epub 2008 Nov 27.Sulfamides as novel histone deacetylase inhibitors.
REF 78Bioorg 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.
REF 79Selective histone deacetylase 6 inhibitors bearing substituted urea linkers inhibit melanoma cell growth. J Med Chem. 2012 Nov 26;55(22):9891-9.
REF 80J Med Chem. 2008 Dec 11;51(23):7417-27.Histone deacetylase inhibitors through click chemistry.
REF 81NVP-LAQ824 is a potent novel histone deacetylase inhibitor with significant activity against multiple myeloma. Blood. 2003 Oct 1;102(7):2615-22. Epub 2003 Jun 19.
REF 82(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2658).
REF 83J 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.
REF 84Emerging drugs in cutaneous T cell lymphoma. Expert Opin Emerg Drugs. 2008 Jun;13(2):345-61.
REF 85J Med Chem. 2004 Jun 17;47(13):3409-17.On the function of the 14 A long internal cavity of histone deacetylase-like protein: implications for the design of histone deacetylase inhibitors.
REF 86Two histone deacetylase inhibitors, trichostatin A and sodium butyrate, suppress differentiation into osteoclasts but not into macrophages. Blood. 2003 May 1;101(9):3451-9. Epub 2003 Jan 2.
REF 87Bioorg 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.
REF 88Discovery of a potent class I selective ketone histone deacetylase inhibitor with antitumor activity in vivo and optimized pharmacokinetic properties. J Med Chem. 2009 Jun 11;52(11):3453-6.
REF 89Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
REF 90The ChEMBL database in 2017.

If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.