Skip to main content

Table 1 Some small molecular modulators of estrogen-related receptors

From: Estrogen-related receptors: novel potential regulators of osteoarthritis pathogenesis

Physiological effects Molecular modulators Targets Notes References
Inverse agonists XCT790 ERRα The detailed molecular mechanism of XCT790 binding to ERRα remains ambiguous Kokabu et al. (2019), Vitto et al. (2019)
LingH2-10 ERRα IC50 = 0.64 ± 0.12 μM Ning et al. (2017)
Thiazolidinediones ERRα   Patch et al. (2011)
Statins ERRα Inhibiting effect in vivo; Inverse effect in vitro Tripathi et al. (2020)
DY40 ERRβ The most potent ERRβ inverse agonist Yu et al. (2017)
GSK5182 ERRγ Relatively non‐toxic with an oral LD50 in mice of greater than 1000 mg/kg Joo et al. (2015)
DY181 ERRγ The most potent ERRγ inverse agonist; IC50 = 0.01 μM Yu et al. (2017)
Tetrasubstituted olefin analog ERRγ   Kim et al. (2019b)
4-OHT ERRβ, ERRγ   Coward et al. (2001)
TAM ERRβ, ERRγ   Coward et al. (2001)
DES ERRα, ERRβ, ERRγ Long-term use of DES can increase the risk of malignant tumors of the genital system Lu et al. (2012)
Agonists Cholesterol ERRα The detailed molecular mechanism of cholesterol binding with ERRα remains ambiguous Casaburi et al. (2018); Li et al. (2019b)
DY 131 ERRβ   Tiek et al. (2019)
GSK4716 ERRγ A potent ERRγ agonist with excellent selectivity over ERRα and ERRβ Kim et al. (2009)
Flavone and isoflavone ERRα, ERRβ   Suetsugi et al. (2003)
GSK9089 ERRβ, ERRγ   Zuercher et al. (2005)