QUESTION 1 Compound A is an inhibitor of the cysteine protease calpain. H (a) A Draw the structure of a natural substrat
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QUESTION 1 Compound A is an inhibitor of the cysteine protease calpain. H (a) A Draw the structure of a natural substrat
QUESTION 1 Compound A is an inhibitor of the cysteine protease calpain. H (a) A Draw the structure of a natural substrate of calpain that spans P3 to P1', identify the scissile bond, and give the mechanism by which it would be hydrolysed by the enzyme. [5 marks) (b) Label the P1, P2, P3 and P4 amino acid R groups on A. [1 mark] (C) What is the role of the C-terminal aldehyde of A in the mechanism of inhibition? [2 marks] (d) Discuss (in detail) the role of the macrocycle of A on the mechanism of inhibition. [4 marks) (e) Discuss all other features of A that contribute to the mechanism of inhibition. [3 marks] (6) What type of inhibitor is A and how might its effects be reversed? [2 marks]