MLchartDataset catalogue

XPO1 inhibitor WJ01024

Term · Oncology and biomedicine · MLC-T-ONC-017604

An orally bioavailable inhibitor of the nuclear export protein exportin-1 (XPO1; chromosome region maintenance 1 protein homolog; CRM1), with potential antineoplastic and pro-apoptotic activities. Upon administration, XPO1 inhibitor WJ01024 reversibly binds to the cargo binding site of XPO1, and prevents the XPO1-mediated nuclear export of cargo proteins, including tumor suppressor proteins (TSPs), such as p53, FOXO, p21, and p27, and leads to their selective accumulation in the nuclei of tumor cells. This restores the nuclear localization and function of TSPs, which leads to the induction of apoptosis in tumor cells. XPO1, the major export factor that transports proteins and RNA from the nucleus to the cytoplasm, is overexpressed in a variety of cancer cell types while minimally expressed in normal, healthy cells. The dysregulated export of TSPs into the cytoplasm prevents TSP-initiated apoptosis. XPO1 overexpression leads to uncontrolled tumor cell proliferation and is associated with poor prognosis.

Table 1. Record
IdentifierMLC-T-ONC-017604
FieldOncology and biomedicine
ReferencesNational Cancer Institute Thesaurus (CC BY 4.0)
Record as JSON
{
  "id": "MLC-T-ONC-017604",
  "term": "XPO1 inhibitor WJ01024",
  "field": "Oncology and biomedicine",
  "definition": "An orally bioavailable inhibitor of the nuclear export protein exportin-1 (XPO1; chromosome region maintenance 1 protein homolog; CRM1), with potential antineoplastic and pro-apoptotic activities. Upon administration, XPO1 inhibitor WJ01024 reversibly binds to the cargo binding site of XPO1, and prevents the XPO1-mediated nuclear export of cargo proteins, including tumor suppressor proteins (TSPs), such as p53, FOXO, p21, and p27, and leads to their selective accumulation in the nuclei of tumor cells. This restores the nuclear localization and function of TSPs, which leads to the induction of apoptosis in tumor cells. XPO1, the major export factor that transports proteins and RNA from the nucleus to the cytoplasm, is overexpressed in a variety of cancer cell types while minimally expressed in normal, healthy cells. The dysregulated export of TSPs into the cytoplasm prevents TSP-initiated apoptosis. XPO1 overexpression leads to uncontrolled tumor cell proliferation and is associated with poor prognosis.",
  "references": [
    "National Cancer Institute Thesaurus"
  ],
  "url": "https://mlchart.com/terminology/oncology/xpo1-inhibitor-wj01024/"
}

Record 17,515 of 17,721 in Oncology and biomedicine terminology (MLC-0111). Request the full dataset.