Preferred Label : PPAR Gamma Inhibitor FX-909;
NCIt synonyms : PPAR-gamma Inhibitor FX-909; PPARG Inverse Agonist FX-909; Peroxisome Proliferator-Activated Receptor Gamma Inhibitor FX-909; PPARG Inhibitor FX-909;
NCIt definition : An orally available inverse agonist and inhibitor of the transcription factor (TF)
peroxisome proliferator-activated receptor gamma (PPAR gamma; PPARG), with potential
antineoplastic activity. Upon oral administration, PPARG inhibitor FX-909 selectively
targets and covalently binds to a region of PPARG that is sequestered from the mutation
site. The binding promotes a repressive conformation of PPARG and inhibits the activity
of PPARG. This inhibits both basal- and ligand-activated transcription by PPARG and
prevents PPARG-mediated transcription of target genes, such as FABP4/Fabp4, AGT/Agt,
IVT/Ivd and ARG1/Arg1. This may inhibit proliferation in PPARG-overactivated tumor
cells. PPARG, a nuclear receptor, is genetically altered, including amplification,
missense mutations, and fusions, in certain tumor cells commonly associated with the
luminal lineage subtype.;
Molecule name : FX-909; FX 909;
Origin ID : C201115;
chemical_or_drug_has_physiologic_effect
- concept_is_in_subset
- has_target
