2. Kinetics to characterize inhibition and activation

An effector modifies the rate of a reaction by combining with the enzyme alone [E] and/or with the enzyme/substrate complex [ES]. Some effectors are inhibitors, slowing down the rate of reaction, while others are activators, speeding it up.

This section covers Michaelian and allosteric single-substrate kinetics. Studying a multi-substrate enzyme means saturating it with substrates not under analysis. These classical characterizations are extremely important for understanding the mechanism of action of molecules marketed for the treatment of disease. These experiments must be mastered, as many therapeutic targets are enzymes.

In 2002, 47% of therapeutic molecules targeted enzymes