Preferred Label : Felezonexor;
NCIt synonyms : XPO1 Inhibitor SL-801;
NCIt 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, felezonexor 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. As a selective inhibitor of nuclear
export (SINE), SL-801 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.;
UNII : PAW9EP9BXO;
InChIKey : CMASLSTVVOYJQY-UHFFFAOYSA-N;
CAS number : 1076235-04-5;
Molecule name : SL 801; CBS 9106; SL-801;
NCI Metathesaurus CUI : CL1405652;
Origin ID : C171660;
UMLS CUI : C5419243;
Semantic type(s)
- concept_is_in_subset
- has_target
