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TREATMENT : HETEROCYCLIC INHIBITORS

 

Following the enzymes catalysis of protein break-up, it binds strongly to the substrate, and more weakly to the products. To accelerate the reaction, they bind to the transition state most strongly of all, lowering the energy of the transition state. The inhibitors being developed, bind well to the enzyme but cannot react further, and hence blocks the active site. The actual inhibitors are further complicated as HIV protease is a dimeric enzyme, which through experience suggests that more or less symmetrically placed heterocyclic rings, improve the binding. Crixivan and Norvir are two such inhibitors being developed.

 

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