Title
Anacetrapib reduces (V)LDL-cholesterol by inhibition of CETP activity and reduction of plasma PCSK9
Author
van der Tuin, S.J.
Kühnast, S.
Berbée, J.
Verschuren, L.
Pieterman, E.J.
Havekes, L.M.
van der Hoorn, J.W.
Rensen, P.C.
Jukema, J.W.
Princen, H.M.
Willems van Dijk, K.
Wang, Y.
Publication year
2015
Abstract
Recently, we showed in APOE*3-Leiden.CETP mice that anacetrapib attenuated atherosclerosis development by reducing (V)LDL-C rather than by raising HDL-C. Here, we investigated the mechanism by which anacetrapib reduces (V)LDL-C and whether this effect was dependent on the inhibition of CETP. APOE*3-Leiden.CETP mice were fed a Western type diet alone or supplemented with anacetrapib (30 mg/kg body weight/d). Microarray analyses of livers revealed down-regulation of the cholesterol biosynthesis pathway (P
Subject
ELSS - Earth, Life and Social Sciences
Life
Healthy Living
Biomedical Innovation
CETP
Cholesterol
Metabolism
Drug therapy
Hypolipidemic drugs
LDL
Metabolism
Lipids
Lipoproteins
PCSK9
Anacetrapib
Apolipoprotein B
Cholesterol ester transfer protein
Low density lipoprotein receptor
Proprotein convertase subtilisin kexin type 9
RNA
Serine proteinase
Sterol regulatory element binding protein 1
Sterol regulatory element binding protein 2
Triacylglycerol
Unclassified drug
Very low density lipoprotein cholesterol
Animal experiment
Animal tissue
Atherosclerosis
Cholesterol synthesis
Controlled study
Down regulation
Drug mechanism
Enzyme blood level
Female
Liver
Microarray analysis
Mouse
Nonhuman
Polymerase chain reaction
Protein expression
RNA isolation
Western diet
MHR - Metabolic Health Research MSB - Microbiology and Systems Biology
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http://resolver.tudelft.nl/uuid:8bc55533-9411-4f87-9b5e-cb65682f7b62
DOI
https://doi.org/10.1194/jlr.m057794
TNO identifier
528177
Source
Journal of Lipid Research, 56 (56), 2085-2093
Document type
article