TABLE 3

Synthetic retinoid nuclear receptor agonists

Overview of retinoid nuclear receptor agonists, including their primary pharmacological action, effects on ABCA1 and ABCG1 expression (arrows: mRNA, protein), and effects on cellular cholesterol efflux. Effects on ABCA1, ABCG1, and cholesterol efflux are presented as follows: (↓) decreased; (= ) no effect; (↑) increased. Italicized symbols indicate changes in ABCA1 and ABCG1 mRNA levels, whereas nonitalicized symbols indicate protein levels.

Compound	Primary Action	ABCA1			ABCG1		Cholesterol Efflux		Reference
RXR agonists
Bexarotene	pan-RXR agonist		↑↑	BLECs		—	↑	BLECs	LaClair et al., 2013; Kuntz et al., 2015; Tachibana et al., 2016
			↑	Cortex^{^a}
			↑	Cortex^{^b}
			↑	Cortex^{^c}
HX630	RXR agonist		↑	THP-1	↑	THP-1	↑	THP-1	Nishimaki-Mogami et al., 2008
HX630	RXR agonist		↑	RAW264.7	↑	THP-1	↑	THP-1	Nishimaki-Mogami et al., 2008
LG101305	RXR agonist		↑	RAW264.7		—	↑	RAW264.7	Claudel et al., 2001
LG268	RXR agonist		↑	Small intestine^{^d}		—	↑	THP-1	Chawla et al., 2001
LG268	RXR agonist		↑	PM		—	↑	THP-1	Chawla et al., 2001
Methoprene	RXR agonist		↑	Astrocyte	↑	Astrocyte		Astrocyte	Repa et al., 2000; Chen et al., 2011b
							↑	apoA-I
							↑	HDL
PA024	RXR agonist		↑	THP-1	↑	THP-1	↑	THP-1	Nishimaki-Mogami et al., 2008
PA024	RXR agonist		↑	RAW264.7	↑	THP-1	↑	THP-1	Nishimaki-Mogami et al., 2008
Tri-butylin chloride	RXRα agonist		↑↑	RAW264.7	↑↑	Primary mouse astrocyte cells	↑	RAW264.7	Cui et al., 2011; Sun et al., 2015
			↑↑	Primary mouse astrocyte cells	↑↑	Cortex^{^c}
			↑↑	Cortex^{^c}
RAR agonists
AM580	RARα agonist			—	↑	THP-1		—	Ayaori et al., 2012
TTNPB	Synthetic RAR agonist	↑		THP-1	↑	THP-1	↑	RAW264.7	Costet et al., 2003; Chen et al., 2011b; Ayaori et al., 2012
		↑		HEK293	↓	Astrocytes	↓	Astrocytes
		↓		Astrocytes	=	Liver^{^d}
		=		Liver^{^d}
		↑		PM^{^d}

BLEC, bovine lens epithelial cells; PM, peritoneal macrophages.
↵^a Lrp1^flox/flox; αCamKII-Cre^−/− mice.
↵^b Lrp1^flox/flox; αCamKII-Cre^+/− mice.
↵^c APPSWE/PSE1_∆E mice.
↵^d C75BL/6/A129Sv mice.