AZT-resistant HIV-1 reverse transcriptase: Difference between revisions
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The RNase H activity of [[reverse transcriptase]] is not currently well known. Because so much is known about the activity of polymerase, this is typically the target for [[reverse transcriptase]] inhibitors. | The RNase H activity of [[reverse transcriptase]] is not currently well known. Because so much is known about the activity of polymerase, this is typically the target for [[reverse transcriptase]] inhibitors. | ||
==Inhibition of Reverse Transcriptase Activity== | ==Inhibition of Reverse Transcriptase Polymerase Activity== | ||
Approximately half of all anti-HIV drugs target the polymerase activity of [[reverse transcriptase]]. Azidothymidine (AZT) is one such medication that affects [[reverse transcriptase]]. AZT is classified as a Nucleoside analog Reverse Transcriptase Inhibitor (NRTI), meaning that it is a nucleoside analog which impacts the polymerase activity of the enzyme. AZT is specifically a thymidine analog and AZT-sensitive HIV binds azidothymidine triphosphate (AZTTP) almost as efficiently as DNA thymidine triphosphate (dTTP). When reverse transcriptase binds AZTTP, the polymerase activity is halted because AZTTP lacks a 3'-OH for the next nucleotide to bind to. Without completion of polymerase activity, the virus is unable to use its RNA as a template for DNA and incorporate its genetic information into the host genome. Preventing reverse transcriptase from creating viral [[DNA]] can greatly impact the progression of the virus by slowing viral replication. This is complicated by the fact that many strains of [[HIV]] are able to develop resistance to AZT and other NRTIs. | Approximately half of all anti-HIV drugs target the polymerase activity of [[reverse transcriptase]]. Azidothymidine (AZT) is one such medication that affects [[reverse transcriptase]]. AZT is classified as a Nucleoside analog Reverse Transcriptase Inhibitor (NRTI), meaning that it is a nucleoside analog which impacts the polymerase activity of the enzyme. AZT is specifically a thymidine analog and AZT-sensitive HIV binds azidothymidine triphosphate (AZTTP) almost as efficiently as DNA thymidine triphosphate (dTTP). When reverse transcriptase binds AZTTP, the polymerase activity is halted because AZTTP lacks a 3'-OH for the next nucleotide to bind to. Without completion of polymerase activity, the virus is unable to use its RNA as a template for DNA and incorporate its genetic information into the host genome. Preventing reverse transcriptase from creating viral [[DNA]] can greatly impact the progression of the virus by slowing viral replication. This is complicated by the fact that many strains of [[HIV]] are able to develop resistance to AZT and other NRTIs. | ||
