MLchartDataset catalogue

lartesertib

Term · Oncology and biomedicine · MLC-T-ONC-014720

An orally bioavailable ATP-competitive inhibitor of ataxia telangiectasia mutated kinase (ATM), with potential chemo-/radio-sensitizing and antineoplastic activities. Upon oral administration, lartesertib targets and binds to ATM, thereby inhibiting the kinase activity of ATM and ATM-mediated signaling. This prevents DNA damage checkpoint activation, disrupts DNA damage repair, induces tumor cell apoptosis, and leads to cell death of ATM-overexpressing tumor cells. In addition, by preventing DNA damage repair, M4076 sensitizes tumor cells to chemo- and radiotherapy and increases their anti-tumor activity. ATM, a serine/threonine protein kinase upregulated in a variety of cancer cell types, is activated in response to DNA damage and plays a key role in DNA-strand repair.

Table 1. Record
IdentifierMLC-T-ONC-014720
FieldOncology and biomedicine
Synonymsataxia telangiectasia mutated kinase inhibitor M4076; ATM kinase inhibitor M4076
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-014720",
  "term": "lartesertib",
  "field": "Oncology and biomedicine",
  "definition": "An orally bioavailable ATP-competitive inhibitor of ataxia telangiectasia mutated kinase (ATM), with potential chemo-/radio-sensitizing and antineoplastic activities. Upon oral administration, lartesertib targets and binds to ATM, thereby inhibiting the kinase activity of ATM and ATM-mediated signaling. This prevents DNA damage checkpoint activation, disrupts DNA damage repair, induces tumor cell apoptosis, and leads to cell death of ATM-overexpressing tumor cells. In addition, by preventing DNA damage repair, M4076 sensitizes tumor cells to chemo- and radiotherapy and increases their anti-tumor activity. ATM, a serine/threonine protein kinase upregulated in a variety of cancer cell types, is activated in response to DNA damage and plays a key role in DNA-strand repair.",
  "synonyms": [
    "ataxia telangiectasia mutated kinase inhibitor M4076",
    "ATM kinase inhibitor M4076"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/lartesertib/"
}

Record 9,936 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.