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The Human Epigenetic Drug Database (HEDD) is a comprehensive web-based database for epigenetic drugs, which focuses on the storage and integration of epigenetic drug datasets that were obtained from laboratory experiments that is essential for understanding the mechanism of action of these epigenetic drugs at a systematic level.

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Suberoylanilide hydroxamic acid

Category:HDACi
Cas Number:149647-78-9
Molecular Formula:C14H20N2O3
Molecular Weight:264.3202 g/mol
Smiles:C1=CC=C(C=C1)NC(=O)CCCCCCC(=O)NO
Description:Suberoylanilide hydroxamic acid is a synthetic hydroxamic acid derivative with antineoplastic activity. Vorinostat, a second generation polar-planar compound, binds to the catalytic domain of the histone deacetylases (HDACs). This allows the hydroxamic moiety to chelate zinc ion located in the catalytic pockets of HDAC, thereby inhibiting deacetylation and leading to an accumulation of both hyperacetylated histones and transcription factors. Hyperacetylation of histone proteins results in the upregulation of the cyclin-dependant kinase p21, followed by G1 arrest. Hyperacetylation of non-histone proteins such as tumor suppressor p53, alpha tubulin, and heat-shock protein 90 produces additional anti-proliferative effects. This agent also induces apoptosis and sensitizes tumor cells to cell death processes. Vorinostat crosses the blood-brain barrier.
synonyms:
Structure:
3D Conformer:3D View
Downlaod:Structure File Download (6.0KB)

Target list

IdDrug NameTargetPubmedIdCo-crystal Complex
57 Suberoylanilide hydroxamic acidHistone deacetylase(Homo sapiens (human))18430569
58 Suberoylanilide hydroxamic acidHistone deacetylase 3/Nuclear receptor corepressor 2(Homo sapiens (human))18430569
59 Suberoylanilide hydroxamic acidHistone deacetylase (HDAC1 and HDAC2)25380299
60 Suberoylanilide hydroxamic acidHistone deacetylase 1 (HDAC1)25380299
61 Suberoylanilide hydroxamic acidHistone deacetylase 325380299
62 Suberoylanilide hydroxamic acidNuclear receptor corepressor 1(Homo sapiens)23865683
63 Suberoylanilide hydroxamic acidHistone deacetylase25380299
64 Suberoylanilide hydroxamic acidHistone deacetylase 4 (HDAC4)20451378
65 Suberoylanilide hydroxamic acidHistone deacetylase20451378
66 Suberoylanilide hydroxamic acidHistone deacetylase 4 (HDAC4)21634430
67 Suberoylanilide hydroxamic acidHistone deacetylase18412327
68 Suberoylanilide hydroxamic acidHistone deacetylase25380299
69 Suberoylanilide hydroxamic acidHistone deacetylase 320451378
70 Suberoylanilide hydroxamic acidHistone deacetylase21634430
71 Suberoylanilide hydroxamic acidHistone deacetylase21634430
72 Suberoylanilide hydroxamic acidHistone deacetylase 5 (HDAC5)20451378
73 Suberoylanilide hydroxamic acid20451378
74 Suberoylanilide hydroxamic acidHistone deacetylase 5 (HDAC5)21634430
75 Suberoylanilide hydroxamic acidHistone deacetylase 321634430
76 Suberoylanilide hydroxamic acidHistone deacetylase (HDAC1 and HDAC2)20451378
Total Page:27 Page   of 27

Disease list

ConditionsDrug NameStatusNct NumberPhases
cutaneous T cell lymphoma
CTCL
Suberoylanilide hydroxamic acidCompletedapproved(N021991)
Myeloproliferative disorders
leukemia
5-Aza-2'-deoxycytidine
Suberoylanilide hydroxamic acid
CompletedNCT00357708Phase 1
LymphomaSuberoylanilide hydroxamic acidCompletedNCT00771472Phase 1
Advanced cancer relapsed and refractorySuberoylanilide hydroxamic acidCompletedNCT00632931Phase 1
LeukemiajMDS5-Aza-2'-deoxycytidine
Suberoylanilide hydroxamic acid
CompletedNCT00479232Phase 1
CancerSuberoylanilide hydroxamic acidCompletedNCT00045006Phase 1
Pelvic cancerjradiotherapySuberoylanilide hydroxamic acidCompletedNCT00455351Phase 1
Hematologic and solid cancerSuberoylanilide hydroxamic acidTerminatedNCT01116154Phase 1
TumorsSuberoylanilide hydroxamic acidCompletedNCT00127127Phase 1
Brain
CNS
intestine tumors
lymphoma
Suberoylanilide hydroxamic acidCompletedNCT00499811Phase 1
LymphomaSuberoylanilide hydroxamic acidCompletedNCT00127140Phase 1
Colorectal cancerSuberoylanilide hydroxamic acidCompletedNCT00336141Phase 1
Hematologia and solid cancerSuberoylanilide hydroxamic acidCompletedNCT00005634Phase 1
Brain
neuroblastoma
CNS
hematologic tumors
Isotretinoi
Suberoylanilide hydroxamic acid
CompletedNCT00217412Phase 1
Leukemia
myelodysplastic syndromes
Idarubicin
Suberoylanilide hydroxamic acid
CompletedNCT00331513Phase 1
NSCL cancerSuberoylanilide hydroxamic acid
gemcitabine
platinum
CompletedNCT00423449Phase 1
Advanced cancerSuberoylanilide hydroxamic acid
pemetrexed
cisplatin
CompletedNCT00106626Phase 1
NSCL
prostate
bladder
urothelial cancers
Suberoylanilide hydroxamic acid
docetaxel
TerminatedNCT00565227Phase 1
Unspecified adult solid tumor
protocol specific
Carboplatin
paclitaxel
Suberoylanilide hydroxamic acid
CompletedNCT00287937Phase 1
Malignant solid tumorSuberoylanilide hydroxamic acid
vinorelbine
TerminatedNCT00801151Phase 1
Total Page:5 Page   of 5

High-throughoutput Dataset

TitleDrug NameCategorySample typePMID
Genome-wide DNA Methylation Analysis Reveals Novel Targets for Drug Development in Mantle Cell Lymphoma 5-aza-2'-deoxycytidine
Suberoylanilide hydroxamic acid
DNMTi
HDACi
human Mantle Cell Lymphoma (MCL) lines Mantle Cell Lymphoma (MCL) patients20427703
Histone deacetylase inhibitors antagonize distinct pathways to suppress tumorigenesis of embryonal rhabdomyosarcoma. Trichostatin A
Suberoylanilide hydroxamic acid
HDACihuman embryonal rhabdomyosarcoma cells (RD and 381T)26636678
RNA expression in MDA-MB-231 cells treated for 24h with SAHA, Pargyline, or both [HG-U133A_2] Pargyline
Suberoylanilide hydroxamic acid
HDMi
HDACi
human breast cancer cells (MDA-MB-231)21452019
23354309
Transcriptional response to histone deacetylase inhibitors Suberoylanilide hydroxamic acid
Valproic acid
HDACihuman lymphoma cell leu-kemia cells (LCL cells)
Dose-Responsive Gene Expression in Suberoylanilide Hydroxamic Acid (SAHA) Treated Resting CD4+ T Cells Suberoylanilide hydroxamic acidHDACihuman CD4+ T cells26258524
Histone deacetylase inhibitors cause the selective depletion of bromodomain containing proteins Trichostatin A
Suberoylanilide hydroxamic acid
HDACi human cervical carcinoma passage cells ( HeLa cells )25755299
Vascular histone deacetylation by pharmacological HDAC inhibition [TSA, ChIP-seq] Trichostatin A
Suberoylanilide hydroxamic acid
HDACi human vascular endothelial cells24732587
HDAC Inhibitors induce tumor cell-selective pro-apoptotic transcriptional responses Suberoylanilide hydroxamic acid
Romidepsin
HDACihuman tumor cell lines(BJ and BJ LTSTERas cells) 23449455
Expression data of rhabdoid tumor cell line A204 treated with HDAC-inhibitor SAHA Suberoylanilide hydroxamic acidHDACi human rhabdoid tumor cell line A204
A Multi-loop, Double-cube Microarray Design Applied to Prostate Cancer Cell Lines with Variable Sensitivity to Histone Deacetylase Inhibitor Suberoylanilide hydroxamic acid
Valproic acid
HDACi human Prostate Cancer Cell Lines (DU-145 and PC3)18980983
Effect of histone deacetylase inhibitors on miRNA expression in thyroid cancer cells Trichostatin A
Suberoylanilide hydroxamic acid
HDACihuman BCPAP papillary thyroid carcinoma cells21946411
BCL6 repression of EP300 provides a basis for rational combinatorial therapy in diffuse large B cell lymphomas Suberoylanilide hydroxamic acid
Valproic acid
Trichostatin A
HDACihuman diffuse large B-cell lymphomas cell lines (DLBCL cell lines)21041953
Gene expression profiles of HCT116 colorectal carcinoma cells treated with HDAC inhibitors Suberoylanilide hydroxamic acid
Romidepsin
HDACihuman HCT116 colorectal carcinoma cells20739454
Primary human erythroid progenitor cells SAHA treatment samples Suberoylanilide hydroxamic acidHDACi human erythroid progenitor cells20616024
Effect of HDAC inhibitors on expression of androgen induced genes Trichostatin A
Suberoylanilide hydroxamic acid
Panobinostat
HDACi human LNCaP prostate cancer cells19176386
Anti-tumor Activity of Histone Deacetylase Inhibitors in Non-Small Cell Lung Cancer Cells Trichostatin A
Suberoylanilide hydroxamic acid
HDACi human non-small cell lung cancer (NSCLC)18606719
HDACI and DAC induce specific epigenetic profile in DLBCL Panobinostat
Suberoylanilide hydroxamic acid
HDACihuman diffuse large B-cell lymphoma cells (DLBCL)21772049
miRNA expression profiling of NB4 control cells versus NB4 cells treated with SAHA (Vorinostat) Suberoylanilide hydroxamic acidHDACi human acute myeloid leukemia cells24349422
HDAC inhibitors cause site-specific chromatin remodeling at PU.1-bound enhancers in K562 cells sodium butyrate
Suberoylanilide hydroxamic acid
HDACihuman the myelogenous leukemia cell lines (K562)
Inhibition of class I histone deacetylases 1 and 2 promotes urothelial carcinoma cell death by various mechanisms (HDAC inhibitor treatments) Suberoylanilide hydroxamic acid
Romidepsin
Givinostat
abexinostat
HDACihuman VM-CUB1 cells human UM-UC-3 cells26772204
Total Page:2

Complex list

PDBIdDrug NameTargetmethodPubmedId
4LXZ Suberoylanilide hydroxamic acidHistone deacetylase 2 (Homo sapiens)X-RAY DIFFRACTION23897821
1ZZ1 Suberoylanilide hydroxamic acidHistone deacetylase-like amidohydrolase (Alcaligenaceae bacterium FB188)X-RAY DIFFRACTION16242151
4R7L Suberoylanilide hydroxamic acidLeukotriene A-4 hydrolase (Homo sapiens)X-RAY DIFFRACTION
4BZ6 Suberoylanilide hydroxamic acidHISTONE DEACETYLASE 8 (Schistosoma mansoni)X-RAY DIFFRACTION24086136
3C0Z Suberoylanilide hydroxamic acidHistone deacetylase 7a (Homo sapiens)X-RAY DIFFRACTION18285338
4QA0 Suberoylanilide hydroxamic acidHistone deacetylase 8 (Homo sapiens)X-RAY DIFFRACTION25075551
1T69 Suberoylanilide hydroxamic acidHistone deacetylase 8 (Homo sapiens)X-RAY DIFFRACTION15242608
1C3S Suberoylanilide hydroxamic acidHDLP (HISTONE DEACETYLASE-LIKE PROTEIN) (Aquifex aeolicus)X-RAY DIFFRACTION10490031
4QA2 Suberoylanilide hydroxamic acidHistone deacetylase 8(Homo sapiens)X-RAY DIFFRACTION25075551

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The Human Epigenetic Drug Database (HEDD) is a comprehensive web-based database for epigenetic drugs, which focuses on integrating epigenetic drug studies based Omics data from high through experiments that is essential for understanding the mechanism of action of these epigenetic drugs at a systematic level.

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©2016 Group of Computational Epigenomics and Bioinformatics, College of Life Science, Jilin Normal University, China

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