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.

CompoundPrimary ActionABCA1ABCG1Cholesterol EffluxReference
1-Phenyl-2-Decanoylamino-3-morpholino-1-propanolGlycosylceramide transferase inhibitorSkin fibroblastsaSkin fibroblastsaGlaros et al., 2005
AclarubicinTopoisomerase I and II inhibitorHepG2Gao et al., 2008
AnacetrapibCETP inhibitorTHP-1Yvan-Charvet et al., 2010a; Brodeur et al., 2017
ABCA1-expressing BHK
DaidzeinMitochondrial aldehyde dehydrogenase inhibitorHepG2Gao et al., 2008
DalcetrapibCETP inhibitorBHKBrodeur et al., 2017
ABCA1-expressing BHK
IbrutinibNLRP3 inflammasome inhibitorTHP-1=THP-1THP-1Chen et al., 2018
= apoA-I
IMB2026791UnknownTHP-1Liu et al., 2012
MCC950NLRP3 inflammasome inhibitorTHP-1=THP-1THP-1Chen et al., 2018
= apoA-I
MetforminAntihyperglycemic agent==RAW264.7RAW264.7RAW264.7He et al., 2019
= apoA-I
N-butyldeoxynojirimycinGlycosylceramide transferase inhibitor=Skin fibroblastsaGlaros et al., 2005
PratenseinUnknownHepG2Gao et al., 2008
PyrromycinMicrobial protein synthesis inhbitorHepG2Gao et al., 2008
t-AUCBSoluble epoxide hydrolase inhibitorLiverb==Liverb3T3-L1 adipocytesShen et al., 2015
Epididymal fatc
TorcetrapibCEPT inhibitorTHP-1THP-1Yvan-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.