TABLE 8

Compounds increasing ABCA1/G1 expression or function by an unknown mechanism

Overview of compounds that increase ABCA1 or ABCG1 expression or function by a yet unknown mechanism, 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
1-Phenyl-2-Decanoylamino-3-morpholino-1-propanol	Glycosylceramide transferase inhibitor	↑↑	Skin fibroblasts^{^a}		—	↑	Skin fibroblasts^{^a}	Glaros et al., 2005
	Glycosylceramide transferase inhibitor	↑↑	Skin fibroblasts^{^a}		—	↑	MDM^{^a}	Glaros et al., 2005
Aclarubicin	Topoisomerase I and II inhibitor	↑↑	HepG2		—		—	Gao et al., 2008
Anacetrapib	CETP inhibitor		—		—	↑	THP-1	Yvan-Charvet et al., 2010a; Brodeur et al., 2017
						↑	BHK
						↑	ABCA1-expressing BHK
Daidzein	Mitochondrial aldehyde dehydrogenase inhibitor	↑↑	HepG2		—		—	Gao et al., 2008
Dalcetrapib	CETP inhibitor		—		—	↑	BHK	Brodeur et al., 2017
Dalcetrapib	CETP inhibitor		—		—	↑	ABCA1-expressing BHK	Brodeur et al., 2017
Ibrutinib	NLRP3 inflammasome inhibitor	↑	THP-1	=	THP-1		THP-1	Chen et al., 2018
						=	apoA-I
						↑	HDL
IMB2026791	Unknown		—		—	↑	THP-1	Liu et al., 2012
						↑	CHO-ABCA1
						↑	CHO
MCC950	NLRP3 inflammasome inhibitor	↑	THP-1	=	THP-1		THP-1	Chen et al., 2018
						=	apoA-I
						↑	HDL
Metformin	Antihyperglycemic agent	==	RAW264.7	↑↑	RAW264.7		RAW264.7	He et al., 2019
						=	apoA-I
						↑	HDL
N-butyldeoxynojirimycin	Glycosylceramide transferase inhibitor		—		—	=	Skin fibroblasts^{^a}	Glaros et al., 2005
Pratensein	Unknown	↑↑	HepG2		—		—	Gao et al., 2008
Pyrromycin	Microbial protein synthesis inhbitor	↑↑	HepG2		—		—	Gao et al., 2008
t-AUCB	Soluble epoxide hydrolase inhibitor	↑↑	Liver^{^b}	==	Liver^{^b}	↑	3T3-L1 adipocytes	Shen et al., 2015
						↑	Epididymal fatc
						↑	RCT^{^b}

Torcetrapib	CEPT inhibitor	↑	THP-1			↑	THP-1	Yvan-Charvet et al., 2007

BHK, baby hamster kidney cell; fatc., fat cell; MDM, monocyte-derived macrophage; NLRP3, nucleotide binding oligomerization domain receptor family, pyrin domain-containing protein 3; t-AUCB, trans-4-[4-(3-Adamanthan-1-yl-uneido)-cyclonexyloxy]-benzoic acid.
↵^a Human.
↵^b LXRα^−/− C75BL/6 mice.