TABLE 6

Inhibitors of ABCA1 and ABCG1 protein breakdown

Overview of compounds that inhibit ABCA1 and ABCG1 protein breakdown, 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
AcifranGPR109A agonistGaidarov et al., 2013
AcipimoxGPR109A agonistGaidarov et al., 2013
ALLNThiol-protease inhibitor=THP-1THP-1Arakawa and Yokoyama, 2002; Yokoyama, 2004
Calphostin CPKC inhibitorCHO-K1 ABCG1(+12)Gelissen et al., 2012
CHO-K1 ABCG1(−12)
DiphenoquinoneUnknown, probucol metaboliteTHP-1RAW264.7THP-1Arakawa et al., 2009; Lu et al., 2016; Yakushiji et al., 2016
RAW264.7RAW264.7
HEK293 apoA-I
Balb/3T3 HDL
MEFsHek293
=LiveraMEFs
Exendin-4GLP-1R agonist3T3-L1 adipocytes3T3-L1 adipocytes3T3-L1 adipocytesMostafa et al., 2015; Yin et al., 2016
glomerulibglomerulib
EzetimibeNPC1L1 inhibitorVSCMsGong et al., 2014; Kannisto et al., 2014
Liverc
Proximal small intestinec
Gö6976PKC inhibitorTHP-1THP-1Iwamoto et al., 2008
Gö6983PKC inhibitorTHP-1THP-1Iwamoto et al., 2008
Liverc
IMM-H007AMPK agonistTHP-1J774Huang et al., 2015
LiverdTHP-1
RCTc
LD211MC1-R agonistBMDMdBMDMdBMDMdRinne et al., 2017
 apoA-I
 HDL
LeupeptinThiol-protease inhibitor=THP-1Arakawa and Yokoyama, 2002
MK-0354GPR109A agonist=MDMd=MDMd=MDMdGaidarov et al., 2013
MK-1903GPR109A agonistMDMdMDMdMDMdGaidarov et al., 2013
MSG606MC1-R agonistBMDMdBMDMdBMDMdRinne et al., 2017
=Aortad=Aortad apoA-I
LiverdLiverd HDL
N-acetyl cysteineGlutathione synthase stimulatorJ774J774J774Machado et al., 2014
 apoA-I
 HDL
NiacinGPR109A agonistHepG2MDMdTHP-1Rubic et al., 2004; Siripurkpong and Na-Bangchang, 2009; Wu and Zhao, 2009; Yvan-Charvet et al., 2010a; Zhang et al., 2012; Gaidarov et al., 2013
3T3-L1 adipocytesHepG2
MM6sr3T3-L1 adipocytes
MDMdMM6sr
MonocytedMDMd
Livere
NicardipineCalcium channel blockerTHP-1Suzuki et al., 2004
RAW264.7
NifedipineCalcium channel blockerRAW264.7RAW264.7THP-1Suzuki et al., 2004; Ishii et al., 2010; Zhang et al., 2013b
Aorta sinusfRAW264.7
PMa apoA-I
 HDL
PD98059MEK1/2 inhibitorTHP-1THP-1CHOZhou et al., 2010; Mulay et al., 2013; Zhang et al., 2016
RAW264.7RAW264.7PMd
HuH7CHO HDL
CHOHEK293
Mouse primary macrop
PMd
PKC19-36PKC inhibitorCHO-K1 ABCG1(+12)Gelissen et al., 2012
CHO-K1 ABCG1(−12)
RottlerinPKC inhibitorTHP-1=THP-1Iwamoto et al., 2008
SpiroquinoneUnknown, probucol metaboliteTHP-1RAW264.7THP-1Yokoyama, 2004; Arakawa et al., 2009; Lu et al., 2016; Yakushiji et al., 2016
RAW264.7RAW264.7
HEK293 apoA-I
Balb/3T3= HDL
MEFsHek293
=LiveraMEFs
Tert-butylhydroquinoneSynthetic phenolic antioxidantTHP-1THP-1Lu et al., 2013
U0126MEK1/2 inhibitorRAW264.7THP-1RAW264.7Mogilenko et al., 2010; Zhou et al., 2010; Mulay et al., 2013; Xue et al., 2016; Zhang et al., 2016; Liu et al., 2019
HepG2RAW264.7 apoA-I
PMbMouse primary macrop HDL
JurkatPMdPM
PMg apoA-I
Jurkat HDL
Jurkat
 apoA-I
VerapamilCalcium channel blockerRAW264.7RAW264.7THP-1Suzuki et al., 2004
RAW264.7
VildagliptinGLP-1R agonist3T3-L1 adipocytes3T3-L1 adipocytes3T3-L1 adipocytesMostafa et al., 2015, 2016
  • ALLN, N-acetyl-leu-leu-norleucinal; GLP-1R, glucagon-like peptide-1 receptor; MDM, monocyte-derived macrophage; MEF, murine embryonic fibroblast; MEK, mitogen-activated protein kinase kinase; NPC1L1, Niemann-Pick C1-like 1; PM, peritoneal macrophages.

  • a New Zealand White rabbits.

  • b apoE−/− C75BL/6 diabetic mice.

  • c apoE−/− C75BL/6 mice.

  • d C75BL/6 mice.

  • e Golden Syrian Hamster.

  • f C3H/He mice.

  • g Sprague Dawley rats.