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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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5-Azacytidine

Category:DNMTi
Cas Number:320-67-2
Molecular Formula:C8H12N4O5
Molecular Weight:244.20468 g/mol
Smiles:C1=NC(=NC(=O)N1C2C(C(C(O2)CO)O)O)N
Description:Azacitidine is a pyrimidine nucleoside analogue of cytidine with antineoplastic activity. Azacitidine is incorporated into DNA, where it reversibly inhibits DNA methyltransferase, thereby blocking DNA methylation. Hypomethylation of DNA by azacitidine may activate tumor suppressor genes silenced by hypermethylation, resulting in an antitumor effect. This agent is also incorporated into RNA, thereby disrupting normal RNA function and impairing tRNA cytosine-5-methyltransferase activity. (NCI04)
synonyms:
Structure:
3D Conformer:3D View
Downlaod:Structure File Download (5.0KB)

Target list

IdDrug NameTargetPubmedIdCo-crystal Complex
2 5-AzacytidineMultidrug and toxin extrusion protein 1 (Homo sapiens)23241029

Disease list

ConditionsDrug NameStatusNct NumberPhases
myelodysplastic syndromes
MDS
5-AzacytidineCompletedapproved(N050794)
Advanced cancers5-Azacytidine
valproic acid
CompletedNCT00496444Phase 1
Ovarian cancer5-Azacytidine TerminatedNCT00842582Phase 1
MDS|leukemia5-Azacytidine CompletedNCT00350818Phase 1
Leukemia
MDSs
5-Azacytidine
sodium phenylbutyrate
CompletedNCT00004871Phase 1
Leukemia
MDSs
5-Azacytidine
arsenic trioxide
TerminatedNCT00234000Phase 1
Lymphoma
small intestine cancer
5-Azacytidine
sodium phenylbutyrate
CompletedNCT00005639Phase 1
Head and neck cancer5-Azacytidine
liothyronine sodium
radiation: iodine I 131
CompletedNCT00004062Phase 1
MDS
AML
5-Azacytidine
Valproic acid
ATRA
CompletedNCT01575691Phase 1
Squamous cell carcinoma5-Azacytidine
cisplatin
TerminatedNCT00443261Phase 1
Advanced cancers5-Azacytidine
Valproic acid
CompletedNCT00496444Phase 1
Advanced solid tumor malignancies5-Azacytidine
erlotinib
CompletedNCT00996515Phase 1
Leukemia
MDSs
5-Azacytidine
entinostat
CompletedNCT00101179Phase 1
Solid tumors and hematologic
malignancies
SB939
5-Azacytidine
CompletedNCT00741234Phase 1
Leukemia
myelodysplastic syndromes
5-Azacytidine
entinostat
CompletedNCT00101179Phase 1
MDSs5-Azacytidine CompletedNCT00118287Phase 1 2
AML
MDS
leukemia
5-Azacytidine
Ara-C
CompletedNCT00569010Phase 1 2
Leukemia
myelodysplastic syndromes
5-Azacytidine
Suberoylanilide hydroxamic acid
SuspendedNCT00392353Phase 1 2
Lung cancer5-Azacytidine
entinostat
SuspendedNCT00387465Phase 1 2
Hematologic cancers5-Azacytidine
midostaurin
SuspendedNCT01093573Phase 1 2
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High-throughoutput Dataset

TitleDrug NameCategorySample typePMID
RNAseq to investigate transcriptional changes in human MM cell lines due to panobinostat, 5-Azacytidine, panobinostat+5-Azacytidine or n-methyl-2-pyrroldine (NMP) treatments. 5-Azacytidine
Panobinostat
DNMTi
HDACi
human Multiple myeloma cell lines24030150
24813887
DNA Methyltransferase inhibition reverses epigenetically embedded phenotypes in lung cancer preferentially affecting Polycomb target genes 5-Azacytidine DNMTihomo non-small cell lung cancer (NSCLC) cell lines (A549 and HTB56)24334763
Immunomodulatory effect of 5-azacytidine (5-azaC): potential role in the transplantation setting 5-azacytidine DNMTiT cells from volunteer donor19887673
Immunomodulatory effect of 5-azacytidine (5-azaC): potential role in the transplantation setting 5-azacytidine DNMTihuman T lymphocytes 24583822
Aplidin synergizes with cytosine arabinoside: functional relevance of mitochondria in Aplidin-induced cytotoxicity plitidepsin
5-Azacytidine
HDACi
DNMTi
human diffuse large B cell lymphoma cell line (SKI-DLCL cells)17713546
Genome-wide DNA methylation in MDS/secondary AML and de novo AML 5-Azacytidine
Entinostat
DNMTi
HDACi
Bone marrow aspirates from 14 patients with MDS, MDS-associated AML (AML with trilineage dysplasia), chronic myelomonocytic leukemia, or relapsed AML19652201
Combination of HDAC inhibitors and Azacytidine for Cancer Cell Selective Targeting of Esophageal Cancer Cells 5-Azacytidine
Entinostat
DNMTi
HDACi
human esophageal tumor cell lines (OE21 and OE33);human non-neoplastic esophageal epithelial cells (Het1A cells)25923331
Myelodysplastic syndrome marrow stroma shows widespread aberrant hypermethylation that is abrogated by treatment with DNMT inhibitors 5-Azacytidine DNMTiThe study population consisted of 6 MDS patients and 3 healthy controls.
MicroRNA-1 is a candidate tumor suppressor and prognostic marker 5-Azacytidine
Trichostatin A
DNMTi
HDACi
human prostate cancer LNCaP cells22210864
Combinatorial treatment of DNMT inhibitor and LSD1 inhibitor results in cell growth inhibition and reexpression of epigenetically silenced genes 5-Azacytidine
clorgyline
DNMTi
HDMi
human cancer cells (T24 ,HCT116 and HL-60 )24040395
Combinatorial pharmacological approaches target EZH2-mediated gene repression in breast cancer cells 5-Azacytidine
Trichostatin A
3-Deazaneplanocin A
DNMTi
HDACi
HMTi
human breast cancer cells (MCF-7)19934278
Identification of genes that may predict response to azacitidine treatment. 5-AzacytidineDNMTibone marrow CD34+ cells obtained from myelodysplasia and related neoplasms patients
Identification of the gene expression in IPF lung fibroblasts after demethylation 5-AzacytidineDNMTiHuman Idiopathic pulmonary fibrosis (IPF) lung fibroblasts26442443

Complex list

PDBIdDrug NameTargetmethodPubmedId
4QD3 5-AzacytidinePeptidyl-tRNA hydrolase (Pseudomonas aeruginosa)X-RAY DIFFRACTION25101795

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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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