Me HN Ме. NH NH2 N. N. IC50 31nM IC50 AG > 1.8 kcal mol-1 N. 12nM R R R s-cis s-trans СOMT СOMT H2N H2N Gln120 Gln120 Me NH HNH: N N……HN/ Ser119 ' HN Ser119 N R R No hydrogen-bonds between water molecule and protein
Catalysis and Enzymatic Reactions
Catalysis is the kind of chemical reaction in which the rate (speed) of a reaction is enhanced by the catalyst which is not consumed during the process of reaction and afterward it is removed when the catalyst is not used to make up the impurity in the product. The enzymatic reaction is the reaction that is catalyzed via enzymes.
Lock And Key Model
The lock-and-key model is used to describe the catalytic enzyme activity, based on the interaction between enzyme and substrate. This model considers the lock as an enzyme and the key as a substrate to explain this model. The concept of how a unique distinct key only can have the access to open a particular lock resembles how the specific substrate can only fit into the particular active site of the enzyme. This is significant in understanding the intermolecular interaction between proteins and plays a vital role in drug interaction.
The figure below shows two COMT inhibitors (4 and 5). Inhibitor 4 exists in two conformations in bulk solution. The complex formed between COMT and inhibitors 4 and 5 is also shown in the figure. Explain why structure 5 (IC50 12nM) is a more effective inhibitor than structure 4 (IC50 31 nM), and explain why the difference in binding affinity is small.
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