Question

decrease the toxic side effects of the anti-malarial drug primaquine, it is oftern 7. (4 points) In order to delivered via a macromolecular pro-drug system (as conjugated to serum albumin). CH,O CH,O HN Serum albumin HN. s- H NH3 ne Provide a mechanism how the active drug can be released at the sites of action.

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Answer 1

It is evident from comparision between the prodrug and primaquine that the sequestered for controlled release by attachment to cysteine residue through an amide bond. However, the cysteine proteases found in the active site of drug action procced by binding to the thiol group of cysteines requiring a possible first attack of cysteine reductases to cleave the disulfide linkages. Then, cysteine reductases are activated by NAD cofactors in the blood. This double cleavage inadverently releases the drug in its active form.