| Most metabolism is catalyzed by biological catalysts - enzymes. Their catalytic activities are apparent at body temperature, and they are strictly regulated by several mechanisms. Both covalent and noncovalent modifications are involved in this regulation and allow for efficient metabolic control. Enzyme activity can be inhibited (or activated) by synthetic compounds (drugs), exogenous compounds (toxins), as well as endogenous compounds (allosteric effectors). Kinetic analyses of enzymatic reaction are beneficial for evaluating the biological role of enzymes and for elucidating their reaction mechanisms. In addition, assays of enzymes in blood are useful for diagnosis of some diseases. Uncontrolled enzymatic activity, however, sometimes causes serious diseases. In such cases, appropriate inhibitors are quite useful for therapeutic purposes.
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- In a multi-step sequence of enzymatic reactions, where is the most effective site for controlling the flux of substrate through the pathway. What effect will an inhibitor of a rate-limiting enzyme have on the concentration of substrates in a multi-step pathway?
- Most drugs are designed to inhibit specific enzymes in biological systems. The drug, Prozac, has had a profound effect on the medical treatment of depression. Review the history of development of Prozac, illustrating the importance of specificity in the mechanism of drug action.
- Discuss some examples of reversible and irreversible enzyme inhibitors used in medical practice.
- Knock-out mice are mice that lack a specific gene. Discuss the impact of KO-mice on the direction of drug development in the pharmaceutical industry.
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