Preferred Label : Abequolixron;
NCIt synonyms : LXR-b Agonist RGX-104; Liver X Receptor beta Agonist RGX-104;
NCIt definition : An orally bioavailable agonist of the nuclear receptor liver X receptor beta (LXRbeta;
NR1H2; LXR-b), with potential immunomodulating and antineoplastic activities. Upon
oral administration, abequolixron selectively targets and binds to LXRbeta, thereby
activating LXRbeta-mediated signaling, leading to the transcription of certain tumor
suppressor genes and the downregulation of certain tumor promoter genes. This particularly
activates the expression of apolipoprotein E (ApoE), a tumor suppressor protein, in
tumor cells and certain immune cells. This activates the innate immune system, resulting
in depletion of immunosuppressive myeloid-derived suppressor cells (MDSCs), tumor
cells and endothelial cells in the tumor microenvironment. This reverses immune evasion,
enhances anti-tumor immune responses and inhibits proliferation of tumor cells. LXRbeta,
a member of the oxysterol receptor family, which is in the nuclear receptor family
of transcription factors, plays a key role in cholesterol transport, glucose metabolism
and the modulation of inflammatory responses; activation of LXRbeta suppresses tumor
cell invasion, angiogenesis, tumor progression, and metastasis in a variety of tumor
cell types. The expression of the ApoE protein becomes silenced in human cancers as
they grow, become invasive, and metastasize; ApoE silencing is related to reduced
survival in cancer patients. The LXR-ApoE pathway regulates the ability of cancers
to evade the immune system and recruit blood vessels.;
UNII : Q26B92650V;
CAS number : 610318-54-2;
Molecule name : RGX 104; RGX-104; SB-742881;
NCI Metathesaurus CUI : CL520758;
Origin ID : C131910;
UMLS CUI : C5554540;
Semantic type(s)
- concept_is_in_subset
