MLchartDataset catalogue

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.

Table 1. Record
IdentifierMLC-T-ONC-015439
FieldOncology and biomedicine
SynonymsCDK4/CDK6/ARK5 inhibitor ON 123300
ReferencesNational 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.