Estrogen-related receptors: novel potential regulators of osteoarthritis pathogenesis

Table 1 Some small molecular modulators of estrogen-related receptors

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)

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