Description
XCT790 is an inverse agonist of estrogen-related receptor α (ERRα; IC
50 = ~300-500 nM). It demonstrates 90-100% inhibition of ERRα constitutive activity and has no significant activity at related nuclear receptors at 10 μM. XCT790 associates with the ligand-binding domain of ERRα and blocks ERRα/PGC-1α-dependent signaling, suppressing the expression of monoamine oxidases A and B. XCT790 induces proteasomal degradation of ERRα and potentiates the degradation of the estrogen receptor ERα by fulvestrant .
Uses
XCT790 is a potent inverse agonist of ERRα.
Definition
ChEBI: XCT 790 is a member of cinnamamides.
Biochem/physiol Actions
XCT 790 is a 5′adenosine monophosphate-activated protein kinase (AMPK) activator. It also acts as a proton ionophore and an uncoupler of oxidative phosphorylation in mitochondria. XCT790 impairs vascular endothelial growth factor (VEGF) and angiopoietin 2 (Ang-2) expression and exhibits suppression of endometrial tumor via estrogen-related receptor (ERRα) inhibition. XCT790 mediates cell cycle arrest and favors apoptosis in triple-negative breast cancer (TNBC).
References
[1] lu x, peng l, lv m, ding k. recent advance in the design of small molecular modulators of estrogen-related receptors. curr pharm des. 2012;18(23):3421-31.
[2] wu f, wang j, wang y, kwok tt, kong sk, wong c. estrogen-related receptor alpha (erralpha) inverse agonist xct-790 induces cell death in chemotherapeutic resistant cancer cells. chem biol interact. 2009 oct 7;181(2):236-42.
