ATM kinase inhibitor WSD-0628
Term · Oncology and biomedicine · MLC-T-ONC-011278
An orally bioavailable, brain-penetrable inhibitor of ataxia telangiectasia mutated (ATM) kinase, with potential chemo-and radio-sensitizing and antineoplastic activities. Upon oral administration, ATM kinase inhibitor WSD-0628 selectively 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 apoptosis in damaged tumor cells, and leads to cell death in ATM-overexpressing tumor cells. WSD-0628 hypersensitizes tumors to chemo/radiotherapy. In addition, WSD-0628 is able to cross the blood-brain barrier (BBB). ATM, a serine/threonine protein kinase belonging to the phosphatidylinositol 3-kinase-related kinase (PIKK) family of protein kinases, is upregulated in a variety of cancer cell types. It is activated in response to DNA double-strand breaks (DSB) and plays a key role in DNA repair.
| Identifier | MLC-T-ONC-011278 |
|---|---|
| Field | Oncology and biomedicine |
| Synonyms | ATM inhibitor WSD-0628 |
| References | National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-011278",
"term": "ATM kinase inhibitor WSD-0628",
"field": "Oncology and biomedicine",
"definition": "An orally bioavailable, brain-penetrable inhibitor of ataxia telangiectasia mutated (ATM) kinase, with potential chemo-and radio-sensitizing and antineoplastic activities. Upon oral administration, ATM kinase inhibitor WSD-0628 selectively 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 apoptosis in damaged tumor cells, and leads to cell death in ATM-overexpressing tumor cells. WSD-0628 hypersensitizes tumors to chemo/radiotherapy. In addition, WSD-0628 is able to cross the blood-brain barrier (BBB). ATM, a serine/threonine protein kinase belonging to the phosphatidylinositol 3-kinase-related kinase (PIKK) family of protein kinases, is upregulated in a variety of cancer cell types. It is activated in response to DNA double-strand breaks (DSB) and plays a key role in DNA repair.",
"synonyms": [
"ATM inhibitor WSD-0628"
],
"references": [
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/atm-kinase-inhibitor-wsd-0628/"
}
Record 2,555 of 17,717 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.