Problem 6 (10 pts) diacyl glycerolphospholipids The scheme illustrates the biosy
ID: 151249 • Letter: P
Question
Problem 6 (10 pts) diacyl glycerolphospholipids The scheme illustrates the biosynthetic pathway for the formation of prostacyclin and thromboxane A2 (prostanoids involved in vasodilation and vasoconstriction mechanisms). onyenase arachidonic acid prostaglandin G Many drug discovery efforts to identify SHPETE new therapeutics for asthma (chronic obstructed lung disease) focus on vasodilation and vasoconstriction mechanisms synthase Prostacyclin Thromboxane A2 P receptors TP receptors a) Propose a druggable upstream target that could have a favorable therapeutic effect on asthma. (Explain) b) Propose a druggable that could have a favorable therapeutic effect on asthma. (Explain) c) Which target would likely lead to the development of a drug with a better safety profile and fewer side effects. (Explain)Explanation / Answer
a.
Leukotrienes work as bronchoconstriction. In asthma, patients need to take bronchodilator to open or dilate the airway so that he can easily overcome the asthmatic problem.
therefore the enzyme "Lipooxygenase" responsible for the synthesis of 5-HPETE from Arachidonic acid can be a best druggable upstream target with less no. of side effects.
b.
Receptor for Thromboxane A2 and down-regulation of synthesis of leukotrienes can be the most druggable downstream targets for the treatment of asthma with lesser number of side effects.
c.
As I have mentioned bronchoconstrictor as main problematic chemicals for Asthmatic Patients, we need to increase the synthesis of bronchodilators such as prostacyclins ( vasodilators) and down-regulation of synthesis of vasoconstrictors.