MLchartDataset catalogue

rucaparib phosphate

Term · Oncology and biomedicine · MLC-T-ONC-016598

The phosphate salt form of rucaparib, an orally bioavailable tricyclic indole and inhibitor of poly(ADP-ribose) polymerases (PARPs) 1 (PARP1), 2 (PARP2) and 3 (PARP3), with potential chemo/radiosensitizing and antineoplastic activities. Upon administration, rucaparib selectively binds to PARP1, 2 and 3 and inhibits PARP-mediated DNA repair. This enhances the accumulation of DNA strand breaks, promotes genomic instability and induces cell cycle arrest and apoptosis. This may enhance the cytotoxicity of DNA-damaging agents and reverse tumor cell resistance to chemotherapy and radiation therapy. PARPs are enzymes activated by single-strand DNA breaks that catalyze the post-translational ADP-ribosylation of nuclear proteins, which induces signaling and the recruitment of other proteins to repair damaged DNA. The PARP-mediated repair pathway plays a key role in DNA repair and is dysregulated in a variety of cancer cell types.

Table 1. Record
IdentifierMLC-T-ONC-016598
FieldOncology and biomedicine
SynonymsPARP1 inhibitor PF-01367338; PARP-1 inhibitor AG014699
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-016598",
  "term": "rucaparib phosphate",
  "field": "Oncology and biomedicine",
  "definition": "The phosphate salt form of rucaparib, an orally bioavailable tricyclic indole and inhibitor of poly(ADP-ribose) polymerases (PARPs) 1 (PARP1), 2 (PARP2) and 3 (PARP3), with potential chemo/radiosensitizing and antineoplastic activities. Upon administration, rucaparib selectively binds to PARP1, 2 and 3 and inhibits PARP-mediated DNA repair. This enhances the accumulation of DNA strand breaks, promotes genomic instability and induces cell cycle arrest and apoptosis. This may enhance the cytotoxicity of DNA-damaging agents and reverse tumor cell resistance to chemotherapy and radiation therapy. PARPs are enzymes activated by single-strand DNA breaks that catalyze the post-translational ADP-ribosylation of nuclear proteins, which induces signaling and the recruitment of other proteins to repair damaged DNA. The PARP-mediated repair pathway plays a key role in DNA repair and is dysregulated in a variety of cancer cell types.",
  "synonyms": [
    "PARP1 inhibitor PF-01367338",
    "PARP-1 inhibitor AG014699"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/rucaparib-phosphate/"
}

Record 14,608 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.