Y Zhang Leukotrienes modulators

Question 1

What does phospholipase A2 do?

Answer 1

Takes FA from cell membranes and forms arachiodonic acid

Question 2

How are prostaglandins formed?

Answer 2

COX 1/COX 2 (cyclooxygenase) convert arachiodonic acid to prostaglandins

Question 3

How are leukotrienes formed?

Answer 3

5-LOX (lipoxygenase) converts arachiodonic acid to leukotrienes

Question 4

Which moeity is the pharmacophore?

Answer 4

Hydroxy-urea

Question 5

What are the important moeities for LTD4 receptor antagonist design?

Answer 5

Question 6

What is the structure of Montelukast?

Answer 6

Question 7

What is the active moeity in Zarfirlukast?

Answer 7

Sulfonamide

Question 8

What are structural differences in LTD4 vs LTB4 design?

Answer 8

Question 9

What is LTD4? CysLT1/2

What is LTB4? BLT4?

Answer 9

LTD4 and LTB4 are leukotrienes

CysLT1/2 and BLT4 are receptors for these ligands