27. Some of the drugs used to treat HIV patients are competitive inhibitors of t

Question

27. Some of the drugs used to treat HIV patients are competitive inhibitors of the HIV reverse transcriptase enzyme. Unfortunately, the high mutation rate of HIV means that the virus rapidly acquires mutations with amino acid changes that make them resistant to these competitive inhibitors. Where in the reverse transcriptase enzyme would such amino acid changes most likely occur in drug-resistant viruses? A. in or near the active site B. at an allosteric site C. at a cofactor binding site D. in regions of the protein that determine packaging into the virus capsid E. Such mutations could occur anywhere with equal probability

Explanation / Answer

Ans. Option A.

It will occur in or near the active site of the reverse transcriptase enzyme because competitive inhibitors are closely resemble the enzyme's normal substrate, because of their structure competitive inhibitors binds reversibly to the enzyme's active site. They form an enzyme-inhibitor[EI] complex which is equivalent to the enzyme-substrate[ES] complex. Thats why mutation occurs in or near the active site of the enzyme to make it resistant from the competitive inhibitors.

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