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Raloxifene is an antagonist of the estrogen receptor and is used for the treatment of hormone-dependent breast cancer. i. What class of antagonist does raloxifene

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Raloxifene is an antagonist of the estrogen receptor and is used for the treatment of hormone-dependent breast cancer. i. What class of antagonist does raloxifene belong to? Give reasons for your answer. ii. Describe the mode of action of raloxifene and discuss why it displays antagonistic rather than agonistic receptor activity. Include carefully draw structures and schemes in your answer. iii. Compare the structure of raloxifene with tamoxifen and outline if structural differences influence their modes of antagonistic action. Part (b) [35 Marks] HIV protease inhibitors such as saquinavir can stabilise the transition state of aspartic proteases. i. Identify and draw the transition-state isostere contained within saquinavir. ii. Discuss the structural development of saquinavir by Roche and its overall mechanism of HIV protease inhibition. Include carefully draw structures and schemes in your answer. Part (c) [35 Marks] i. Discuss the use and mode of action of the DNA-targeting drug, bleomycin. ii. Compare the mechanism of anticancer action of cyclophosphamide and cisplatin. Include carefully draw structures and schemes in your

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