E.3 Chemistry of Statins

Question 1

Why is cholesterol important ?

Answer 1

Important for the biosynthesis and cell membrane structure

Question 2

What can an excess of cholesterol lead to?

Answer 2

CVD

Question 3

How are fatty molecules (cholesterol transported around the body), and where do they transport the fatty acid molecules to?

Answer 3

Fatty acid molecules are transported in the blood via LDL and HDLs?

LDLs transport cholesterol to the cells (bad)
HDL transport cholesterol from the cells to the liver (good)

Mortality increases when levels of LDLs are high in the body and levels of HDLs are low

Question 4

When cholesterol caused fatty plaque in the arteries, what conditions can this lead to?

Answer 4

Artherosclerosis, clot formation, stroke, and heart attack

Question 5

How do statins work overall?

Answer 5

They inhibit cholesterol synthesis, in particular, HMG CoA reductase ( HMG CoA——–> mevalonate)

Question 6

What is the co-factor involved in the synthesis of mevalonate?

Answer 6

NADPH and this is being reduced

Question 7

What type of inhibitor is a stain?

Answer 7

A competitive inhibitor

Question 8

In HMG CoA, what is the active site?

Answer 8

Lysine charge pincer