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Drug-Target Interaction

Drug

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PubChem ID:451668
Structure:
Synonyms:
"5-aza-2′-deoxycytidine"
"5-deoxy-2′-azacytidine"
1,3, 5-Triazin-2(1H)-one, 4-amino-1-(2-deoxy--D-erythro-pentofuranosyl)-
2'-Deoxy-5-azacytidine
2353-33-5
4-amino-1-(2-deoxy-beta-D-erythro-pentofuranosyl)-1,3,5-triazin-2(1H)-one
4-amino-1-(2-deoxy-beta-D-erythro-pentofuranosyl)-s-triazin-2(1H)-one
4-Amino-1-(2-deoxy-beta-D-ribofuranosyl)-1,3,5-triazin-2(1H)-one
4-amino-1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-1,3,5-triazi
4-amino-1-[(2R,4S,5R)-4-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-1,3,5-triazin-2-one
5-Aza-2′-Deoxycytidine
5-Aza-2'-deoxycytidine
5-aza-2-deoxycytidine
5-aza-CdR
5-aza-dC
5-AZAdC
5-azadeoxycytidine
5-Deoxy-2′-azacytidine
5A2dc
A3656_SIGMA
AC-1135
AC1L9PS9
AIDS-000616
AIDS000616
AzadC
CHEBI:50131
CHEMBL1201129
D03665
DAC
Dacogen
Dacogen (TN)
Dacogen, 5-aza-2'-deoxycytidine,NSC 127716, Dacogen, DAC, Decitabine
DB01262
Decitabine
Decitabine (USAN/INN)
Decitabine-Supplied by Selleck Chemicals
Dezocitidine
E-7373
FT-0082622
HMS2235O03
MLS001332587
MLS001332588
MolMap_000063
NCGC_5ADOC
NSC-127716
NSC127716
S1200_Selleck
SBB066121
SMR000857076
TL8001944
ATC-Codes:

Target

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Uniprot ID:POKL_HUMAN
Synonyms:
Putative HERV-K_Xq28 provirus ancestral Pol protein
EC-Numbers:2.7.7.49
Organism:Homo sapiens
Human
PDB IDs:-

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----

References:

18021753
Epigenetic silencing of telomerase and a non-alkylating agent as a novel therapeutic approach for glioma.. Rahima Patel; Leroy Shervington; Robert Lea; Amal Shervington (2008) Brain research display abstract
5-Aza-2'-deoxycytidine (5azadC) inhibits DNA methyltransferase and subsequently induces the expression of genes silenced by methylation. While treatment with 5azadC downregulated hTERT and upregulated MGMT expression in two glioma cell lines, there was no change in the expression of these two genes in the normal cell line. However, cell viability was reduced as a result of 5azadC treatment in all three cell lines. 5azadC treatment reduced telomerase expression and activity and subsequently enhanced chemosensitivity towards cisplatin, taxol and tamoxifen but not with the alkylating agents temozolomide (TMZ), carmustine and chlorambucil. To further evaluate the effect of these findings, the level of hTERT and MGMT expression was measured in a recurrent anaplastic ependymoma, seven glioblastoma and two normal brain tissues. While four of eight gliomas and one of the normal tissues expressed MGMT, hTERT was expressed in all gliomas but not in the normal brain tissue. Results of this study suggest that taxol together with 5azadC may be a good therapeutic combination for glioma. In addition, the work on cell lines can be repeated on tissues utilizing hTERT as the therapeutic target for demethylation using 5azadC in glioma.