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#1 Drug to treat Heart disease?
How do human cells obtain cholesterol?
- Biosynthesis - synthesized w/in the cell
- Endocytosis of lipoproteins - LDL's deliver cholesterol by binding to the LDL receptor through apo B100
What do Statins do?
Inhibit cholesterol synthesis in all cells
During endocytosis, what binds to the LDL receptor?
During endocytosis, what does apolipoprotein B100 bind to?
What does mutations of either apo B100 or the LDL receptor do and what is this called?
- Prevent binding of LDLs to cells
- Familial Hypercholesterolemia
With high blood LDL concentration, what happens to storage, biosynthesis, and uptake?
- Down regulates synthesis
- Down regulates production
- Up regulates storage
What is the key regulatory enzyme in cholesterol biosynthesis?
HMG CoA reductase
What effect does insulin have on cholesterol?
It up regulates it
How does statins inhibit cholesterol biosynthesis?
- Statins mimic HMG CoA
- HMG CoA reductase is inhibited by statins and does it by mimicry
What are side effects of statins?
Myopathies (muscle pain)