Narazaciclib
Term · Oncology and biomedicine · MLC-T-ONC-015439
An orally bioavailable inhibitor of NUAK family SNF1-like kinase 1 (AMPK-related protein kinase 5; ARK5), and the cyclin-dependent kinases 4 (CDK4) and 6 (CDK6), with potential antineoplastic activity. Upon oral administration,narazaciclib specifically binds to and inhibits ARK5, which interferes with the activation of ARK5-mediated signal transduction pathways and reduces cell proliferation in cancer cells that overexpress ARK5. In addition, ON 123300 inhibits CDK4 and 6 and prevents the phosphorylation of retinoblastoma (Rb) protein in early G1. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, which causes G1 phase cell cycle arrest, suppresses DNA synthesis and inhibits cancer cell growth. ARK5, a member of the AMP-activated protein kinase (AMPK) family, is associated with tumor growth and invasion. Overexpression of CDK4/6, which is seen in certain types of cancer, causes cell cycle deregulation.
| Identifier | MLC-T-ONC-015439 |
|---|---|
| Field | Oncology and biomedicine |
| Synonyms | CDK4/CDK6/ARK5 inhibitor ON 123300 |
| References | National Cancer Institute Thesaurus (CC BY 4.0) |
Record as JSON
{
"id": "MLC-T-ONC-015439",
"term": "Narazaciclib",
"field": "Oncology and biomedicine",
"definition": "An orally bioavailable inhibitor of NUAK family SNF1-like kinase 1 (AMPK-related protein kinase 5; ARK5), and the cyclin-dependent kinases 4 (CDK4) and 6 (CDK6), with potential antineoplastic activity. Upon oral administration,narazaciclib specifically binds to and inhibits ARK5, which interferes with the activation of ARK5-mediated signal transduction pathways and reduces cell proliferation in cancer cells that overexpress ARK5. In addition, ON 123300 inhibits CDK4 and 6 and prevents the phosphorylation of retinoblastoma (Rb) protein in early G1. Inhibition of Rb phosphorylation prevents CDK-mediated G1-S phase transition, which causes G1 phase cell cycle arrest, suppresses DNA synthesis and inhibits cancer cell growth. ARK5, a member of the AMP-activated protein kinase (AMPK) family, is associated with tumor growth and invasion. Overexpression of CDK4/6, which is seen in certain types of cancer, causes cell cycle deregulation.",
"synonyms": [
"CDK4/CDK6/ARK5 inhibitor ON 123300"
],
"references": [
"National Cancer Institute Thesaurus"
],
"url": "https://mlchart.com/terminology/oncology/narazaciclib/"
}
Record 11,596 of 17,717 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.