(A) This schematic shows the genes discussed in relation to lipid
metabolism (highlighted by red font). Cholesterol and sterols are taken up from
the intestinal lumen via the Nieman Pick C1-like 1 (NPC1L1) transporter (blue,
lower left corner) and are then re-assembled into chylomicrons containing
apolipoprotein (APO) B48. The liver produces cholesterol through HMG-CoA
reductase (HMGCR; upper center), which is incorporated with triglycerides into
APOB100-containing VLDL. LPL (purple) hydrolyzes triglycerides into free fatty
acids (FFA), resulting in the formation of LDL and RLPs from VLDL and
chylomicrons, respectively, which can enter tissues. Most APOB-containing
lipoproteins are taken up via the hepatic LDL receptor (LDLR). Proprotein
convertase subtilisin/kexin type 9 (PCSK9) stimulates internalization and
degradation of the LDLR, thereby reducing cell surface expression of the LDLR.
Angiopoietin-like (ANGPL) 3, ANGPTL4, and APOC3 are endogenous inhibitors of
LPL. APOC3 can also suppress hepatic uptake of APOEcontaining lipoprotein
particles (found e.g., on VLDL and RLPs). (B) Diabetes enhances hepatic
production of APOC3. Elevated levels of APOC3 increase circulating levels of
triglyceride-rich lipoproteins (TRLs), resulting in accumulation of RLPs in the
artery wall and accelerated atherosclerosis, in part via increased macrophage
lipid loading. An antisense oligonucleotide (ASO) to APOC3 completely blocks
diabetes-accelerated atherosclerosis in a mouse model. Other emerging strategies
to block APOC3 include small interfering RNA (RNAi) and monoclonal antibodies.
Figure 2B is reproduced and modified from [80] with permission from the Journal of Clinical Investigation.