CK1 alpha degrader CC-91633

{
  "id": "MLC-T-ONC-012624",
  "term": "CK1 alpha degrader CC-91633",
  "field": "Oncology and biomedicine",
  "definition": "An orally bioavailable degrader of casein kinase 1 alpha (CK1alpha; CK1a), with potential antineoplastic activity. Upon oral administration, CK1a degrader CC-91633 binds to and degrades CK1a, thereby inhibits the activity of CK1a. This prevents the enhanced binding of murine double minute X (MDMX) to p53, reduces the formation of CK1a and MDM2 complex, and prevents the interaction of MDM2 with p53. This prevents the inhibition of p53 and increases p53 activity. This induces p53-mediated cell cycle arrest, thereby inhibiting tumor cell proliferation. CK1a, a serine/threonine kinase and a leukemic stem cell target, acts as a tumor suppressor in several cancers through the negative regulation of Wnt/beta-catenin signaling and p53. It negatively regulates p53 by phosphorylating MDMX, thus enhancing binding of MDMX to p53, as well as by forming a complex with MDM2.",
  "synonyms": [
    "CK1 alpha degrader BMS986397",
    "CK1a degrader CC-91633"
  ],
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/ck1-alpha-degrader-cc-91633/"
}