Question

For what purposes would someone consider designing a small molecule enzyme inhibitor?

Answer 1

Enzyme is proteinaceous in nature and these biological molecules acts as catalyst to speed up the reaction by lowering the activation energy. Enzyme inhibitors are the molecules which can go and bind to the active site of the enzyme and can decrease its activity. Sometime it may bind away from the active site and alters the binding of the substrates to the active site.

When it comes to small enzyme inhibitors, they are important tools used in pharmaceutical industry for the pharmaceutical intervention in various human diseases. Most of the drugs what we are using are the inhibitors of specific enzyme targets. These will go and bind to those specific enzyme and will decrease their activity. They may be taken in the form of injection or oral tablets. Few examples for these small inhibitors are Acetazolamide which acts agaisnt carbonic anhydrase, Aspirin acts against Cyclooxygenase, Captopril acts against angiotensin.

These inhibitors are intentionally synthesized as small molecule compound, so that it can easily penetrate the cell and can escape from proteolytic degradation. But one disadvantage is reducing their size sometimes reduces their specificity also. small molecules offers us to pack them in suitable concentration for oral administration, and this small size only targets active site but not the whole enzyme and so dose also will be less.