Nevirapine is a reversible non-competitive inhibitor of the AIDS virus reversed transcriptase. It is in the NNRTI (non-nucleoside reversed transcriptase inhibitors) class of medications. a.) What advantage over nucleoside based reversed transcriptase inhibitors like 3'-azidothymidine was anticipated for the non-nucleoside reversed transcriptase inhibitors? CH3 4 HINS 5 Nevirapine b.) What method was used to discover the initial lead compound possessing low potency reversed transcriptase inhibition activity? c.) Does nevirapine compete with the 2'-deoxynucleoside 5'-triphosphates for occupancy of the enzyme catalytic site?

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Nevirapine is a reversible non-competitive
inhibitor of the AIDS virus reversed transcriptase. It is in
the NNRTI (non-nucleoside reversed transcriptase
inhibitors) class of medications.
a.) What advantage over nucleoside based reversed
transcriptase inhibitors like 3'-azidothymidine was
anticipated for the non-nucleoside reversed
transcriptase inhibitors?
CH3
4
11
Nevirapine
b.) What method was used to discover the initial lead compound possessing low
potency reversed transcriptase inhibition activity?
c.) Does nevirapine compete with the 2'-deoxynucleoside 5'-triphosphates for
occupancy of the enzyme catalytic site?
d.) Do you predict that nevirapine binding will induce a conformational change in the
reversed transcriptase? Justify your answer.
e.) Will mutations within the catalytic site of AIDS virus reversed transcriptase that
decrease the efficacy of nucleoside based reversed transcriptase inhibitors similarly
decrease the efficacy of nevirapine?
Transcribed Image Text:Nevirapine is a reversible non-competitive inhibitor of the AIDS virus reversed transcriptase. It is in the NNRTI (non-nucleoside reversed transcriptase inhibitors) class of medications. a.) What advantage over nucleoside based reversed transcriptase inhibitors like 3'-azidothymidine was anticipated for the non-nucleoside reversed transcriptase inhibitors? CH3 4 11 Nevirapine b.) What method was used to discover the initial lead compound possessing low potency reversed transcriptase inhibition activity? c.) Does nevirapine compete with the 2'-deoxynucleoside 5'-triphosphates for occupancy of the enzyme catalytic site? d.) Do you predict that nevirapine binding will induce a conformational change in the reversed transcriptase? Justify your answer. e.) Will mutations within the catalytic site of AIDS virus reversed transcriptase that decrease the efficacy of nucleoside based reversed transcriptase inhibitors similarly decrease the efficacy of nevirapine?
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