Question

What are transition state inhibitors? how do they work? please explain.

Answer 1

An enzyme reaction undergoes a transition state formation before the product is formed and released. During this state, substrate is bound to the enzyme and under modification, for the product to be formed. Inhibitors which mimic the transition state, are transition state analogues. Because of the structural similarity, these inhibitors bind the enzyme well. They occupy the site for substrates, rendering the enzyme inactive for catalysis. Such inhibitors have a higher binding affinity for the enzyme, than the original substrate. Example includes HIV protease inhibitor saquinavir.