cyclin A/B RxL inhibitor CID-078
Term · Oncology and biomedicine · MLC-T-ONC-012856
An orally bioavailable macrocycle inhibitor of cyclin A and B RxL, with potential antineoplastic activity. Upon oral administration, cyclin A/B RxL inhibitor CID-078 selectively targets and binds to the hydrophobic patch (HP) of cyclins A and B and prevents cyclin A and B substrates containing RxL motifs from binding to cyclins A and B, thereby preventing their interaction, including the interaction of the cyclin A substrate E2F1 with cyclin A-cyclin-dependent kinase 2 (CDK2) and the cyclin B substrate Myt1 with cyclin B-CDK1. This may lead to DNA cell damage and cell cycle arrest during the G1/S transition, induce apoptosis, and inhibit proliferation of susceptible tumor cells. Cyclins A and B play a key role in the regulation and progression of the cell cycle and their function is dysregulated in certain tumor cell types.
| Identifier | MLC-T-ONC-012856 |
|---|---|
| Field | Oncology and biomedicine |
| References | National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-012856",
"term": "cyclin A/B RxL inhibitor CID-078",
"field": "Oncology and biomedicine",
"definition": "An orally bioavailable macrocycle inhibitor of cyclin A and B RxL, with potential antineoplastic activity. Upon oral administration, cyclin A/B RxL inhibitor CID-078 selectively targets and binds to the hydrophobic patch (HP) of cyclins A and B and prevents cyclin A and B substrates containing RxL motifs from binding to cyclins A and B, thereby preventing their interaction, including the interaction of the cyclin A substrate E2F1 with cyclin A-cyclin-dependent kinase 2 (CDK2) and the cyclin B substrate Myt1 with cyclin B-CDK1. This may lead to DNA cell damage and cell cycle arrest during the G1/S transition, induce apoptosis, and inhibit proliferation of susceptible tumor cells. Cyclins A and B play a key role in the regulation and progression of the cell cycle and their function is dysregulated in certain tumor cell types.",
"references": [
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/cyclin-a-b-rxl-inhibitor-cid-078/"
}
Record 5,560 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.