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CHE130A Quiz 4 W10 Key Hague

CHE130A Quiz 4 W10 Key Hague - bacteria 3(4pts Please...

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Quiz # 4 March 10, 2010 Chem 130A, Winter 2010 Last name_______________ First name________________ SN_____________ 1 . 2 . 1. (4 pts.) Below is an analogue of Deferasirox (marketed as Exjade ), designed as oral iron chelator, used to reduce chronic iron overload in patients who are receiving long-term blood transfusions for conditions such as beta-thalassemia and other chronic anemias. It is the first oral medication approved in the USA for this purpose. Please encircle 2 potential toxicophoric groups in this molecule. N N N HO OH HO O 3 . 2. (2pts.) Why would you want to design a drug that is an enzyme inhibitor? To block the biotransformation of substrates or formation of products or block a metabolic pathway in a foreign organism such as
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Unformatted text preview: bacteria. 3. (4pts.) Please explain the difference of enzyme inhibition using a transition state analog and a mechanism-based irreversible inhibitor. Transition state analogs mimic the transition state of substrates that the enzyme can bind tightly but cannot be processed along the reaction pathway. Mechanism-based irreversible inactivators are compounds that bear structural similarity to the natural substrates or products. It uses the catalytic machinery of the enzyme to reveal reactive groups that allows for binding and subsequent inactivation of the enzyme prior to escape from the active site....
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