The LDL receptor
. Arterioscler Thromb Vasc Biol 2009; 29: 431-438, doi: 10.1161/ ATVBAHA.108.179564.
Kootte et al., "Pro-atherogenic lipid changes and decreased hepatic LDL receptor
expression by tocilizumab in rheumatoid arthritis," Atherosclerosis, vol.
Furin-cleaved PCSK9 is unable to regulate the LDL receptor
compared to intact PCSK9 (13).
 Transient down-regulation of LDL receptors
in rats followed methylprednisolone administration, accounting for elevated LDL and TC.
Alternatively, the fully human monoclonal antibody PCSK9 inhibitors lower bad cholesterol by preventing PCKS9 from binding to the LDL receptors
in the liver.
Alternatively, the fully human monoclonal antibody PCSK9 inhibitors lower bad cholesterol by preventing PCKS9 from binding to and degrading the LDL receptors
in the liver resulting in more available to remove excess LDL cholesterol.
A nonsense mutation in the LDL receptor
gene leads to familial hypercholesterolemia in the Druze sect.
The drugs are antibodies that free up a protein on cells called the LDL receptor
, which lowers LDL by pulling it out of circulation.
It is thought that blocking the destructive capacity of PCSK9 can lead to more LDL receptors
on cells and lower cholesterol levels.
Invasive procedures such as lipid apheresis and liver transplant may be a last resort in patients who have no functional LDL receptors
and are not responding to pharmacological therapy.
Studies further reveal that it incre- ases LDL receptor
binding capacity in the liver and prevents elevation of total cholesterol and up-regu- lates hepatic LDL receptors
resulting in greater in- flux of plasma LDL cholesterol in the liver.
[13.] Graadt van Roggen J.F, van der Westhuyzen D.R., Coetzee G.A, Marais A.D, Steyn K., Langenhoven E., Kotze M.J., FH Afrikaner-3 LDL Receptor
mutation results in defective LDL receptors
and causes a mild form of familial hypercholesterolemia.