CETP inhibitors downregulate hepatic LDL receptor and PCSK9 expression in vitro and in vivo through a SREBP2 dependent mechanism

B Dong, AB Singh, C Fung, K Kan, J Liu - Atherosclerosis, 2014 - Elsevier
Background CETP inhibitors block the transfer of cholesteryl ester from HDL-C to VLDL-C
and LDL-C, thereby raising HDL-C and lowering LDL-C. In this study, we explored the effect
of CETP inhibitors on hepatic LDL receptor (LDLR) and PCSK9 expression and further
elucidated the underlying regulatory mechanism. Results We first examined the effect of
anacetrapib (ANA) and dalcetrapib (DAL) on LDLR and PCSK9 expression in hepatic cells
in vitro. ANA exhibited a dose-dependent inhibition on both LDLR and PCSK9 expression in …