lerociclib
Term · Oncology and biomedicine · MLC-T-ONC-014750
An orally bioavailable inhibitor of cyclin-dependent kinase (CDK) types 4 (CDK4) and 6 (CDK6), with potential antineoplastic activity. Upon administration, lerociclib selectively inhibits CDK4 and CDK6, which inhibits the phosphorylation of retinoblastoma protein (Rb) early in the G1 phase, prevents CDK-mediated G1-S phase transition and leads to cell cycle arrest. This suppresses DNA replication and decreases tumor cell proliferation. CDK4 and 6 are serine/threonine kinases that are upregulated in many tumor cell types and play a key role in the regulation of both cell cycle progression from the G1-phase into the S-phase and tumor cell proliferation.
| Identifier | MLC-T-ONC-014750 |
|---|---|
| Field | Oncology and biomedicine |
| Synonyms | 7',8'-dihydro-2'-((5-(4-(1-methylethyl)-1-piperazinyl)-2-pyridinyl)amino)spiro(cyclohexane-1,9'(6'H)-pyrazino(1',2':1,5)pyrrolo(2,3-d)pyrimidin)-6'-one; CDK4/6 inhibitor G1T38; G1T38 free base |
| References | National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-014750",
"term": "lerociclib",
"field": "Oncology and biomedicine",
"definition": "An orally bioavailable inhibitor of cyclin-dependent kinase (CDK) types 4 (CDK4) and 6 (CDK6), with potential antineoplastic activity. Upon administration, lerociclib selectively inhibits CDK4 and CDK6, which inhibits the phosphorylation of retinoblastoma protein (Rb) early in the G1 phase, prevents CDK-mediated G1-S phase transition and leads to cell cycle arrest. This suppresses DNA replication and decreases tumor cell proliferation. CDK4 and 6 are serine/threonine kinases that are upregulated in many tumor cell types and play a key role in the regulation of both cell cycle progression from the G1-phase into the S-phase and tumor cell proliferation.",
"synonyms": [
"7',8'-dihydro-2'-((5-(4-(1-methylethyl)-1-piperazinyl)-2-pyridinyl)amino)spiro(cyclohexane-1,9'(6'H)-pyrazino(1',2':1,5)pyrrolo(2,3-d)pyrimidin)-6'-one",
"CDK4/6 inhibitor G1T38",
"G1T38 free base"
],
"references": [
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/lerociclib/"
}
Record 10,027 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.