DNA polymerase theta inhibitor GSK4524101
Term · Oncology and biomedicine · MLC-T-ONC-013100
An orally bioavailable inhibitor of DNA polymerase (pol) theta, with potential chemosensitizing and antineoplastic activities. Upon oral administration, pol theta inhibitor GSK4524101 specifically targets, binds to and inhibits the activity of pol theta. This prevents pol theta-mediated repair of double-stranded DNA breaks via the microhomology-mediated end joining (MMEJ) process. This causes apoptosis and inhibits proliferation in cancer cells. GSK4524101may have a synergistic effect if administered in combination with agents that cause DNA damage. Pol theta plays a key role in DNA synthesis and repair that is highly expressed in cancer cells while nearly absent in most healthy tissues. It plays a key role in cancer cell survival.
| Identifier | MLC-T-ONC-013100 |
|---|---|
| Field | Oncology and biomedicine |
| Synonyms | pol theta inhibitor GSK4524101; POLQi GSK4524101 |
| References | National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-013100",
"term": "DNA polymerase theta inhibitor GSK4524101",
"field": "Oncology and biomedicine",
"definition": "An orally bioavailable inhibitor of DNA polymerase (pol) theta, with potential chemosensitizing and antineoplastic activities. Upon oral administration, pol theta inhibitor GSK4524101 specifically targets, binds to and inhibits the activity of pol theta. This prevents pol theta-mediated repair of double-stranded DNA breaks via the microhomology-mediated end joining (MMEJ) process. This causes apoptosis and inhibits proliferation in cancer cells. GSK4524101may have a synergistic effect if administered in combination with agents that cause DNA damage. Pol theta plays a key role in DNA synthesis and repair that is highly expressed in cancer cells while nearly absent in most healthy tissues. It plays a key role in cancer cell survival.",
"synonyms": [
"pol theta inhibitor GSK4524101",
"POLQi GSK4524101"
],
"references": [
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/dna-polymerase-theta-inhibitor-gsk4524101/"
}
Record 6,118 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.