Target Information
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] | ||||
Cutaneous T-cell lymphoma [ICD9: 202.1, 202.2; ICD10: C84.0, C84.1] | |||||
Cerebrovascular ischaemia [ICD9: 434.91; ICD10: I61-I63] | |||||
Cancer [ICD9: 140-229; ICD10: C00-C96] | |||||
Friedreich's ataxia [ICD9: 334; ICD10: G11.1] | |||||
General leukaemia cancer [ICD9: 204-208; ICD10: C91-C95] | |||||
Hodgkin's lymphoma; Multiple myeloma [ICD9: 201, 202.8, 203.0; ICD10: C81, C81-C86, C90] | |||||
Hepatocellular carcinoma [ICD9: 155; ICD10: C22.0] | |||||
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] | |||||
Melanoma [ICD9: 172; ICD10: C43] | |||||
Peripheral T-cell lymphoma [ICD9: 202.7; ICD10: C84.4] | |||||
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] | |||||
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 | [556264] |
Romidepsin | Drug Info | Approved | Cutaneous T-cell lymphoma | [530677], [542036] | |
Vorinostat | Drug Info | Approved | Cutaneous T-cell lymphoma | [537114], [541932] | |
HBI-8000 | Drug Info | Registered | Cancer | [543057], [548485] | |
NVP-LAQ824 | Drug Info | Phase 3 | Severe mood disorders | [536580] | |
Panobinostat | Drug Info | Phase 3 | Type 2 diabetes | [532695], [542511] | |
Romidepsin | Drug Info | Phase 3 | Renal cell carcinoma; Hormone refractory prostate cancer | [530677], [542036] | |
ITF2357 | Drug Info | Phase 2 | Myelofibrosis; Essential thrombocythemia; Polycythemia vera | [537520], [542513] | |
MGCD-0103 | Drug Info | Phase 2 | Solid tumours | [529426], [542038] | |
Panobinostat | Drug Info | Phase 2 | Primary myelofibrosis; Post-polycythemia vera; Post-essential thrombocytopenia; Cutaneous T cell-lymphomas | [537114], [542511] | |
Phenylbutyrate | Drug Info | Phase 2 | Urea cycle disorders | [536447], [543164] | |
Resminostat | Drug Info | Phase 2 | Hepatocellular carcinoma | [542522], [551497] | |
Romidepsin | Drug Info | Phase 2 | Peripheral T-cell lymphoma | [530677], [542036] | |
SB-623 | Drug Info | Phase 2 | Cerebrovascular ischaemia | [525202] | |
SNDX-275 | Drug Info | Phase 2 | Hodgkin's lymphoma; Multiple myeloma | [542037], [547063] | |
Sodium butyrate | Drug Info | Phase 2 | Acute myeloid leukemia; Refractory sickle cell ulcers | [531969] | |
CHR-3996 | Drug Info | Phase 1 | Solid tumours | [531893], [543102] | |
OBP-801 | Drug Info | Phase 1 | Cancer | [525149] | |
RG-2833 | Drug Info | Phase 1 | Friedreich's ataxia | [542521], [549368] | |
SB-639 | Drug Info | Phase 1 | Cancer | [531947] | |
4SC-202 | Drug Info | Preclinical | Cancer | [551497] | |
Chlamydocin | Drug Info | Preclinical | Cancer | [534024] | |
Depudecin | Drug Info | Preclinical | Cancer | [544324] | |
HC-Toxin | Drug Info | Preclinical | Cancer | [534075] | |
M-carboxycinnamic acid bishydroxamide | Drug Info | Preclinical | Cancer | [534436] | |
Scriptaid | Drug Info | Preclinical | Cancer | [536447], [542524] | |
SK-7041 | Drug Info | Preclinical | Cancer | [527163] | |
SK-7068 | Drug Info | Preclinical | Cancer | [527163] | |
AN-9 | Drug Info | Discontinued in Phase 2 | Melanoma | [545713] | |
Tacedinaline | Drug Info | Discontinued in Phase 2 | Cancer | [543093], [545228] | |
NVP-LAQ824 | Drug Info | Discontinued in Phase 1/2 | General leukaemia cancer | [536580] | |
Pyroxamide | Drug Info | Discontinued in Phase 1 | Cancer | [547711] | |
Oxamflatin | Drug Info | Terminated | Cancer | [546336] | |
Inhibitor | (E)-8-Biphenyl-4-yl-1-oxazol-2-yl-oct-7-en-1-one | Drug Info | [526871] | ||
1,1,1-Trifluoro-8-(4-phenoxy-phenoxy)-octan-2-one | Drug Info | [526450] | |||
1,1,1-Trifluoro-8-phenoxy-octan-2-one | Drug Info | [526450] | |||
2-(methylsulfonylthio)ethyl 2-propylpentanoate | Drug Info | [529333] | |||
4-Benzenesulfonylamino-N-hydroxy-benzamide | Drug Info | [526165] | |||
4-Benzoylamino-N-hydroxy-benzamide | Drug Info | [527691] | |||
4-Butyrylamino-N-hydroxy-benzamide | Drug Info | [526922] | |||
4-Chloro-N-(5-hydroxycarbamoyl-pentyl)-benzamide | Drug Info | [526878] | |||
4-Dimethylamino-N-(6-mercapto-hexyl)-benzamide | Drug Info | [527439] | |||
4-Hydroxy-N-(5-hydroxycarbamoyl-pentyl)-benzamide | Drug Info | [526266] | |||
4-Phenylbutyrohydroxamic acid | Drug Info | [530700] | |||
4-tert-butyl-N-hydroxybenzamide | Drug Info | [528882] | |||
4SC-202 | Drug Info | [551497] | |||
5-(4-Chloro-phenyl)-pentanoic acid hydroxyamide | Drug Info | [527056] | |||
5-(4-hydroxyphenyl)-3H-1,2-dithiole-3-thione | Drug Info | [529333] | |||
5-Mercapto-pentanoic acid phenylamide | Drug Info | [527439] | |||
6-(2-Bromo-acetylamino)-hexanoic acid phenylamide | Drug Info | [527439] | |||
6-(3-Benzoyl-ureido)-hexanoic acid hydroxyamide | Drug Info | [530898] | |||
6-(9H-carbazol-9-yl)-N-hydroxyhexanamide | Drug Info | [531216] | |||
6-benzenesulfinylhexanoic acid hydroxamide | Drug Info | [527980] | |||
6-benzenesulfonylhexanoic acid hydroxamide | Drug Info | [527980] | |||
6-Mercapto-hexanoic acid phenylamide | Drug Info | [527439] | |||
6-Phenoxy-hexane-1-thiol | Drug Info | [527439] | |||
6-phenylsulfanylhexanoic acid hydroxamide | Drug Info | [527980] | |||
7-(1H-indol-5-yloxy)-N-hydroxyheptanamide | Drug Info | [528478] | |||
7-(3-Benzoyl-ureido)-heptanoic acid hydroxyamide | Drug Info | [530898] | |||
7-(4-(dimethylamino)phenoxy)-N-hydroxyheptanamide | Drug Info | [528478] | |||
7-(Biphenyl-3-yloxy)-1-oxazol-2-yl-heptan-1-one | Drug Info | [526871] | |||
7-(Biphenyl-4-yloxy)-1,1,1-trifluoro-heptan-2-one | Drug Info | [526450] | |||
7-(Biphenyl-4-yloxy)-1-oxazol-2-yl-heptan-1-one | Drug Info | [526871] | |||
7-(Biphenyl-4-yloxy)-heptanoic acid hydroxyamide | Drug Info | [526708] | |||
7-(Naphthalen-2-yloxy)-1-oxazol-2-yl-heptan-1-one | Drug Info | [526871] | |||
7-Biphenyl-4-yl-heptanoic acid hydroxyamide | Drug Info | [526847] | |||
7-Mercapto-heptanoic acid benzothiazol-2-ylamide | Drug Info | [527439] | |||
7-Mercapto-heptanoic acid biphenyl-3-ylamide | Drug Info | [527439] | |||
7-Mercapto-heptanoic acid biphenyl-4-ylamide | Drug Info | [527439] | |||
7-Mercapto-heptanoic acid phenylamide | Drug Info | [527439] | |||
7-Mercapto-heptanoic acid pyridin-3-ylamide | Drug Info | [527439] | |||
7-Mercapto-heptanoic acid quinolin-3-ylamide | Drug Info | [527439] | |||
7-mercapto-N-(4-phenylthiazol-2-yl)heptanamide | Drug Info | [529093] | |||
7-Phenoxy-heptanoic acid hydroxyamide | Drug Info | [526847] | |||
8-(3-Benzoyl-ureido)-octanoic acid hydroxyamide | Drug Info | [530898] | |||
8-(4-bromophenyl)-N-hydroxy-8-oxooctanamide | Drug Info | [529911] | |||
8-(Biphenyl-3-yloxy)-1,1,1-trifluoro-octan-2-one | Drug Info | [526450] | |||
8-(biphenyl-4-yl)-N-hydroxy-8-oxooctanamide | Drug Info | [529911] | |||
8-(Biphenyl-4-yloxy)-1,1,1-trifluoro-octan-2-one | Drug Info | [526450] | |||
8-(Biphenyl-4-yloxy)-2-oxo-octanoic acid | Drug Info | [526708] | |||
8-Mercapto-octanoic acid phenylamide | Drug Info | [527439] | |||
8-Oxo-8-phenyl-octanoic acid | Drug Info | [526266] | |||
8-Oxo-8-phenyl-octanoic acid hydroxyamide | Drug Info | [526878] | |||
8-Phenyl-octanoic acid hydroxyamide | Drug Info | [526847] | |||
9,9,9-Trifluoro-8-oxo-nonanoic acid phenylamide | Drug Info | [526450] | |||
9-(Biphenyl-4-yloxy)-1,1,1-trifluoro-nonan-2-one | Drug Info | [526450] | |||
ADS-100380 | Drug Info | [528523] | |||
ADS-102550 | Drug Info | [528523] | |||
AN-9 | Drug Info | [536272] | |||
Azithromycin-N-benzyltriazolyldecahydroxamic Acid | Drug Info | [529875] | |||
Azithromycin-N-benzyltriazolylhexahydroxamic Acid | Drug Info | [529875] | |||
Azithromycin-N-benzyltriazolylnonahydroxamic Acid | Drug Info | [529875] | |||
Azithromycin-N-benzyltriazolyloctahydroxamic Acid | Drug Info | [529875] | |||
Azithromycinarylalkylhydroxamic Acid | Drug Info | [529875] | |||
AZUMAMIDE B | Drug Info | [529411] | |||
AZUMAMIDE C | Drug Info | [529411] | |||
AZUMAMIDE E | Drug Info | [529411] | |||
Chlamydocin | Drug Info | [536509] | |||
CHR-3996 | Drug Info | [531893] | |||
Cyclo(-L-Am7(S2Py)-A2in-L-Ala-D-Pro-) | Drug Info | [529054] | |||
Cyclo(-L-Am7(S2Py)-Aib-L-Ala-D-Pro-) | Drug Info | [529054] | |||
Cyclo(-L-Am7(S2Py)-Aib-L-Ala-D-Tic-) | Drug Info | [529054] | |||
Cyclo(-L-Am7(S2Py)-Aib-L-Ph4-D-Pro-) | Drug Info | [529054] | |||
Cyclo(-L-Am7(S2Py)-Aib-L-Ph5-D-Pro-) | Drug Info | [529054] | |||
Cyclo(-L-Am7(S2Py)-Aib-L-Phe-D-Pro-) | Drug Info | [529054] | |||
Cyclo(-L-Am7(S2Py)-Aib-L-Phg-D-Pro-) | Drug Info | [529054] | |||
Cyclo(-L-Am7(S2Py)-Aib-L-Ser(Bzl)-D-Pro-) | Drug Info | [529054] | |||
Cyclo(-L-Am7(S2Py)-Aib-L-Ser-D-Pro-) | Drug Info | [529054] | |||
Cyclo(-L-Am7(S2Py)-D-2MePhe-L-Ala-D-Pro-) | Drug Info | [529054] | |||
Cyclo(-L-Am7(S2Py)-D-A1in-L-Ala-D-Pro-) | Drug Info | [529054] | |||
Cyclo(-L-Am7(S2Py)-L-2MePhe-L-Ala-D-Pro-) | Drug Info | [529054] | |||
Cyclo(-L-Am7(S2Py)-L-A1in-L-Ala-D-Pro-) | Drug Info | [529054] | |||
Cyclostellettamine derivative | Drug Info | [527058] | |||
Depudecin | Drug Info | [536272], [536509] | |||
Desclasinose Azithromycinarylalkyl Hydroxamate | Drug Info | [529875] | |||
Gymnochrome E | Drug Info | [530729] | |||
HC-Toxin | Drug Info | [536509] | |||
ITF2357 | Drug Info | [537114], [537520] | |||
LARGAZOLE | Drug Info | [530933] | |||
M-carboxycinnamic acid bishydroxamide | Drug Info | [536272], [536509] | |||
MGCD-0103 | Drug Info | [536272], [536509], [537647] | |||
N,8-dihydroxy-8-(naphthalen-2-yl)octanamide | Drug Info | [529911] | |||
N-(2,3-Dimethylphenyl)-N'-hydroxyoctanediamide | Drug Info | [530704] | |||
N-(2,4-Dimethylphenyl)-N'-hydroxyoctanediamide | Drug Info | [530704] | |||
N-(2,5-Dimethylphenyl)-N'-hydroxyoctanediamide | Drug Info | [530704] | |||
N-(2,6-Dimethylphenyl)-N'-hydroxyoctanediamide | Drug Info | [530704] | |||
N-(2-amino-5-(thiophen-2-yl)phenyl)nicotinamide | Drug Info | [529767] | |||
N-(2-aminophenyl)-4-(chroman-3-ylmethyl)benzamide | Drug Info | [529129] | |||
N-(2-aminophenyl)-4-methoxybenzamide | Drug Info | [529104] | |||
N-(2-aminophenyl)nicotinamide | Drug Info | [529767] | |||
N-(2-aminophenyl)quinoxaline-6-carboxamide | Drug Info | [529104] | |||
N-(2-Ethylphenyl)-N'-hydroxyoctanediamide | Drug Info | [530704] | |||
N-(2-Mercapto-ethyl)-N'-phenyl-oxalamide | Drug Info | [527500] | |||
N-(2-Mercapto-ethyl)-N'-phenyl-succinamide | Drug Info | [527500] | |||
N-(3,4-Dimethylphenyl)-N'-hydroxyoctanediamide | Drug Info | [530704] | |||
N-(3,5-Dimethylphenyl)-N'-hydroxyoctanediamide | Drug Info | [530704] | |||
N-(3-Ethylphenyl)-N'-hydroxyoctanediamide | Drug Info | [530704] | |||
N-(4-aminobiphenyl-3-yl)nicotinamide | Drug Info | [529767] | |||
N-(4-Ethylphenyl)-N'-hydroxyoctanediamide | Drug Info | [530704] | |||
N-(4-hydroxybiphenyl-3-yl)benzamide | Drug Info | [529767] | |||
N-(5-Hydroxycarbamoyl-pentyl)-4-nitro-benzamide | Drug Info | [526878] | |||
N-(6-Hydroxycarbamoyl-hexyl)-benzamide | Drug Info | [526266] | |||
N-(6-Mercapto-hexyl)-benzamide | Drug Info | [527439] | |||
N-hydroxy-2,2'-bithiophene-5-carboxamide | Drug Info | [528523] | |||
N-Hydroxy-4-((R)-2-phenyl-butyrylamino)-benzamide | Drug Info | [527691] | |||
N-Hydroxy-4-((S)-2-phenyl-butyrylamino)-benzamide | Drug Info | [527691] | |||
N-Hydroxy-4-(2-phenyl-butyrylamino)-benzamide | Drug Info | [527691] | |||
N-Hydroxy-4-(3-phenyl-propionylamino)-benzamide | Drug Info | [530261] | |||
N-Hydroxy-4-(4-phenyl-butyrylamino)-benzamide | Drug Info | [527691] | |||
N-Hydroxy-4-(5-phenyl-pentanoylamino)-benzamide | Drug Info | [527691] | |||
N-Hydroxy-4-(pentanoylamino-methyl)-benzamide | Drug Info | [526922] | |||
N-Hydroxy-4-(phenylacetylamino-methyl)-benzamide | Drug Info | [526922] | |||
N-Hydroxy-4-phenylacetylamino-benzamide | Drug Info | [527691] | |||
N-hydroxy-5-(pyridin-2-yl)thiophene-2-carboxamide | Drug Info | [528523] | |||
N-hydroxy-5-(pyridin-3-yl)thiophene-2-carboxamide | Drug Info | [528523] | |||
N-hydroxy-5-(pyridin-4-yl)thiophene-2-carboxamide | Drug Info | [528523] | |||
N-hydroxy-5-phenylthiophene-2-carboxamide | Drug Info | [528523] | |||
N-hydroxy-6-oxo-6-phenylhexanamide | Drug Info | [529911] | |||
N-hydroxy-7-(4-methoxyphenyl)-7-oxoheptanamide | Drug Info | [529911] | |||
N-hydroxy-7-(naphthalen-2-yl)-7-oxoheptanamide | Drug Info | [529911] | |||
N-hydroxy-7-(naphthalen-2-yloxy)heptanamide | Drug Info | [528478] | |||
N-hydroxy-7-oxo-7-phenylheptanamide | Drug Info | [529911] | |||
N-hydroxy-8-(2-methoxyphenyl)-8-oxooctanamide | Drug Info | [529911] | |||
N-hydroxy-8-(4-methoxyphenyl)-8-oxooctanamide | Drug Info | [529911] | |||
N-hydroxy-8-(naphthalen-2-yl)non-8-enamide | Drug Info | [529911] | |||
N-hydroxy-8-(naphthalen-2-yl)oct-7-enamide | Drug Info | [529911] | |||
N-hydroxy-8-(naphthalen-2-yl)octanamide | Drug Info | [529911] | |||
N-hydroxy-8-oxo-8-(pyridin-3-yl)octanamide | Drug Info | [529911] | |||
N-hydroxy-9-oxo-9-phenylnonanamide | Drug Info | [529911] | |||
N-Hydroxy-N'-(2-methylphenyl)octanediamide | Drug Info | [530704] | |||
N-Hydroxy-N'-(3-methylphenyl)octanediamide | Drug Info | [530704] | |||
N-Hydroxy-N'-(4-methoxyphenyl)octanediamide | Drug Info | [530704] | |||
N-Hydroxy-N'-(4-methylphenyl)octanediamide | Drug Info | [530704] | |||
N-hydroxybenzo[b]thiophene-2-carboxamide | Drug Info | [529285] | |||
N1-(biphenyl-3-yl)-N8-hydroxyoctanediamide | Drug Info | [529866] | |||
N1-(biphenyl-4-yl)-N8-hydroxyoctanediamide | Drug Info | [530106] | |||
N1-hydroxy-N8-(4-phenylthiazol-2-yl)octanediamide | Drug Info | [530106] | |||
nexturastat A | Drug Info | [532053] | |||
NSC-746457 | Drug Info | [529805] | |||
NVP-LAQ824 | Drug Info | [535748] | |||
OBP-801 | Drug Info | [543680] | |||
Octanedioic acid bis-hydroxyamide | Drug Info | [526376] | |||
Octanedioic acid hydroxyamide pyridin-2-ylamide | Drug Info | [526266] | |||
Octanedioic acid hydroxyamide pyridin-4-ylamide | Drug Info | [526266] | |||
Oxamflatin | Drug Info | [536272], [536509] | |||
Panobinostat | Drug Info | [536272], [536509], [536739], [537647] | |||
Phenylbutyrate | Drug Info | [536447] | |||
PSAMMAPLIN A | Drug Info | [526878] | |||
Pyroxamide | Drug Info | [536272], [536509] | |||
Resminostat | Drug Info | [551497] | |||
Romidepsin | Drug Info | [530677] | |||
SB-623 | Drug Info | [536509] | |||
SB-639 | Drug Info | [536509] | |||
Scriptaid | Drug Info | [536272], [536447], [536509] | |||
SK-683 | Drug Info | [527104] | |||
SK-7041 | Drug Info | [536272], [536509] | |||
SK-7068 | Drug Info | [536272], [536509] | |||
SNDX-275 | Drug Info | [537114] | |||
Sodium butyrate | Drug Info | [535661], [536272] | |||
ST-2986 | Drug Info | [530016] | |||
ST-2987 | Drug Info | [530016] | |||
ST-3050 | Drug Info | [530016] | |||
Tacedinaline | Drug Info | [536272], [536509] | |||
Thioacetic acid S-(6-phenylcarbamoyl-hexyl) ester | Drug Info | [527439] | |||
Vorinostat | Drug Info | [536272], [537319], [537647] | |||
Modulator | HBI-8000 | Drug Info | [1572591] | ||
histone deacetylase-1 inhibitors (cancer) | Drug Info | [1572605] | |||
RG-2833 | Drug Info | [1572591] | |||
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' | |||||
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 525149 | ClinicalTrials.gov (NCT02414516) A Dose-Escalation Study of OBP-801 in Patients With Advanced Solid Tumors. U.S. National Institutes of Health. | ||||
Ref 525202 | ClinicalTrials.gov (NCT02448641) Study of Modified Stem Cells (SB623) in Patients With Chronic Motor Deficit From Ischemic Stroke. U.S. National Institutes of Health. | ||||
Ref 527163 | Class I histone deacetylase-selective novel synthetic inhibitors potently inhibit human tumor proliferation. Clin Cancer Res. 2004 Aug 1;10(15):5271-81. | ||||
Ref 529426 | MGCD0103, 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 531893 | A 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 531947 | Epigenetics in vascular disease - therapeutic potential of new agents. Curr Vasc Pharmacol. 2014 Jan;12(1):77-86. | ||||
Ref 531969 | The 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 532695 | Progress of HDAC inhibitor panobinostat in the treatment of cancer. Curr Drug Targets. 2014 Jun;15(6):622-34. | ||||
Ref 534024 | Preclinical and clinical studies of clindamycin-2-phosphate (author's transl). Jpn J Antibiot. 1977 Jan;30(1):42-50. | ||||
Ref 534075 | Inhibition of maize histone deacetylases by HC toxin, the host-selective toxin of Cochliobolus carbonum. Plant Cell. 1995 Nov;7(11):1941-50. | ||||
Ref 534436 | Selective 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 536447 | Emerging disease-modifying therapies for the treatment of motor neuron disease/amyotropic lateral sclerosis. Expert Opin Emerg Drugs. 2007 May;12(2):229-52. | ||||
Ref 536580 | Novel drugs and therapeutic targets for severe mood disorders. Neuropsychopharmacology. 2008 Aug;33(9):2080-92. Epub 2008 Jan 2. | ||||
Ref 537520 | Emerging drugs for the therapy of primary and post essential thrombocythemia, post polycythemia vera myelofibrosis. Expert Opin Emerg Drugs. 2009 Jun 24. | ||||
Ref 541932 | (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 542036 | (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 542037 | (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 542038 | (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 542511 | (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 542513 | (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 542521 | (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 542522 | (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 542524 | (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 543057 | (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 543093 | (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 543102 | (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 543164 | (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 544324 | HDAC inhibitors repress the polycomb protein BMI1. Cell Cycle. 2010 Jul 15; 9(14): 2722-2730. | ||||
Ref 545228 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800002525) | ||||
Ref 545713 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800004320) | ||||
Ref 546336 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800007547) | ||||
Ref 547063 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800012663) | ||||
Ref 547711 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800018698) | ||||
Ref 548485 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800025931) | ||||
Ref 526165 | Bioorg Med Chem Lett. 2001 Nov 5;11(21):2847-50.Design and synthesis of a novel class of histone deacetylase inhibitors. | ||||
Ref 526266 | J 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 526376 | J 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 526450 | Bioorg Med Chem Lett. 2002 Dec 2;12(23):3443-7.Trifluoromethyl ketones as inhibitors of histone deacetylase. | ||||
Ref 526708 | Bioorg Med Chem Lett. 2003 Oct 6;13(19):3331-5.Alpha-keto amides as inhibitors of histone deacetylase. | ||||
Ref 526847 | Bioorg 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 526871 | Bioorg Med Chem Lett. 2003 Nov 17;13(22):3909-13.Heterocyclic ketones as inhibitors of histone deacetylase. | ||||
Ref 526922 | J 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 527056 | Bioorg 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 527058 | Bioorg 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 527104 | J 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 527439 | J 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 527500 | Bioorg Med Chem Lett. 2005 Apr 15;15(8):1969-72.Mercaptoamide-based non-hydroxamic acid type histone deacetylase inhibitors. | ||||
Ref 527691 | J Med Chem. 2005 Aug 25;48(17):5530-5.Structure-based optimization of phenylbutyrate-derived histone deacetylase inhibitors. | ||||
Ref 527980 | J Med Chem. 2006 Jan 26;49(2):800-5.Aromatic sulfide inhibitors of histone deacetylase based on arylsulfinyl-2,4-hexadienoic acid hydroxyamides. | ||||
Ref 528478 | Bioorg 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 528523 | Bioorg 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 528882 | Bioorg Med Chem Lett. 2007 Aug 15;17(16):4619-24. Epub 2007 May 27.Design of novel histone deacetylase inhibitors. | ||||
Ref 529054 | Bioorg 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 529093 | J 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 529104 | J 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 529129 | Bioorg 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 529285 | J Med Chem. 2008 Mar 27;51(6):1505-29. Epub 2008 Feb 5.Histone deacetylase inhibitors: from bench to clinic. | ||||
Ref 529333 | Bioorg 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 529411 | Bioorg 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 529767 | Bioorg 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 529805 | J Med Chem. 2008 Dec 11;51(23):7417-27.Histone deacetylase inhibitors through click chemistry. | ||||
Ref 529866 | Bioorg Med Chem Lett. 2009 Jan 15;19(2):336-40. Epub 2008 Nov 27.Sulfamides as novel histone deacetylase inhibitors. | ||||
Ref 529875 | J Med Chem. 2009 Jan 22;52(2):456-68.Non-peptide macrocyclic histone deacetylase inhibitors. | ||||
Ref 529911 | Eur J Med Chem. 2009 Jul;44(7):2868-76. Epub 2008 Dec 16.3D-QSAR studies of HDACs inhibitors using pharmacophore-based alignment. | ||||
Ref 530016 | Bioorg 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 530106 | Bioorg 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 530261 | Eur 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 530700 | Nat Chem Biol. 2010 Mar;6(3):238-243. Epub 2010 Feb 7.Chemical phylogenetics of histone deacetylases. | ||||
Ref 530704 | J 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 530729 | J Nat Prod. 2010 Apr 23;73(4):712-5.Gymnochromes E and F, cytotoxic phenanthroperylenequinones from a deep-water crinoid, Holopus rangii. | ||||
Ref 530898 | Bioorg 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 530933 | J Med Chem. 2010 Jun 24;53(12):4654-67.Synthesis and biological characterization of the histone deacetylase inhibitor largazole and C7- modified analogues. | ||||
Ref 531216 | Bioorg Med Chem Lett. 2010 Dec 1;20(23):7067-70. Epub 2010 Oct 12.Inhibitors selective for HDAC6 in enzymes and cells. | ||||
Ref 531893 | A 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 532053 | Selective histone deacetylase 6 inhibitors bearing substituted urea linkers inhibit melanoma cell growth. J Med Chem. 2012 Nov 26;55(22):9891-9. | ||||
Ref 535661 | Two 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 535748 | NVP-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 536272 | Anticancer activities of histone deacetylase inhibitors. Nat Rev Drug Discov. 2006 Sep;5(9):769-84. | ||||
Ref 536447 | Emerging disease-modifying therapies for the treatment of motor neuron disease/amyotropic lateral sclerosis. Expert Opin Emerg Drugs. 2007 May;12(2):229-52. | ||||
Ref 536509 | Histone deacetylase inhibitors in cancer therapy: latest developments, trends and medicinal chemistry perspective. Anticancer Agents Med Chem. 2007 Sep;7(5):576-92. | ||||
Ref 536739 | Emerging drugs in cutaneous T cell lymphoma. Expert Opin Emerg Drugs. 2008 Jun;13(2):345-61. | ||||
Ref 537319 | Discovery 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 537520 | Emerging drugs for the therapy of primary and post essential thrombocythemia, post polycythemia vera myelofibrosis. Expert Opin Emerg Drugs. 2009 Jun 24. | ||||
Ref 537647 | Protein methyltransferases as a target class for drug discovery. Nat Rev Drug Discov. 2009 Sep;8(9):724-32. | ||||
Ref 543680 | (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). |
If You Find Any Error in Data or Bug in Web Service, Please Kindly Report It to Dr. Zhou and Dr. Zhang.