MLchartDataset catalogue

5-Aza-4'-thio-2'-deoxycytidine

Term · Oncology and biomedicine · MLC-T-ONC-009548

An orally bioavailable, nucleoside analog and DNA methyltransferase I (DNMT1) inhibitor, with potential DNA hypomethylating and antineoplastic activities. Upon administration, 5-aza-4'-thio-2'-deoxycytidine (Aza-TdC) gets incorporated into DNA, where it binds to the active site of DNMT1, a maintenance methyltransferase that contributes to the hypermethylation and silencing of tumor suppressor genes. The formation of covalent DNMT1-DNA complexes inhibits DNMT1, prevents DNA methylation of CpG sites, causes CpG demethylation, and results in the re-expression and re-activation of silenced tumor suppressor genes. This inhibits tumor cell proliferation. DNMT1, overactivated in tumor cells, plays a key role in tumor cell proliferation.

Table 1. Record
IdentifierMLC-T-ONC-009548
FieldOncology and biomedicine
AbbreviationAza-TdC
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-009548",
  "term": "5-Aza-4'-thio-2'-deoxycytidine",
  "field": "Oncology and biomedicine",
  "definition": "An orally bioavailable, nucleoside analog and DNA methyltransferase I (DNMT1) inhibitor, with potential DNA hypomethylating and antineoplastic activities. Upon administration, 5-aza-4'-thio-2'-deoxycytidine (Aza-TdC) gets incorporated into DNA, where it binds to the active site of DNMT1, a maintenance methyltransferase that contributes to the hypermethylation and silencing of tumor suppressor genes. The formation of covalent DNMT1-DNA complexes inhibits DNMT1, prevents DNA methylation of CpG sites, causes CpG demethylation, and results in the re-expression and re-activation of silenced tumor suppressor genes. This inhibits tumor cell proliferation. DNMT1, overactivated in tumor cells, plays a key role in tumor cell proliferation.",
  "abbreviation": "Aza-TdC",
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/5-aza-4-thio-2-deoxycytidine/"
}

Record 102 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.