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Reverse Transcriptase Inhibitors (RTIs)

Reverse transcriptase inhibitors (RTIs) are the antiretroviral class of drugs used in the management and treatment of HIV. These drugs block the replication of virus by inhibiting the reverse transcription of viral RNA into DNA. Within the class of reverse transcriptase inhibitors, there are two subclasses of drugs. The first class includes the nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs), and the second class includes the non-nucleoside reverse transcriptase inhibitors (NNRTIs). The NRTIs were the first class of antiretroviral drugs to be approved by the FDA. NRTIs are taken as prodrugs and must be taken into the host cell and phosphorylated before they become active. Once inside the host cell, cellular kinases will activate the drug. The drug exerts its effect through its structure by competing with natural deoxynucleotides. NRTIs lack a 3’-hydroxyl group at the 2’-deoxyribosyl moiety and will have either a nucleoside or nucleotide as a base. Due to the missing 3’-hydroxyl group, the NRTI prevents the formation of a 3’-5’-phosphodiester bond in growing DNA chains and can thus prevent replication of the virus.

NNRTIs are the second class of reverse transcriptase inhibitors. The primary mechanism of action is through the binding of the NNRTI to the reverse transcriptase and the creation of a hydrophobic pocket proximal to the active site. This pocket creates a new spatial configuration of the substrate-binding site which reduces the overall polymerase activity. By creating a different configuration, DNA synthesis becomes slow overall. Because of the non-competitive inhibitor action of NNRTI, it is not effective against HIV-2 reverse transcriptase. BioVision is proud to offer >10 reverse transcriptase inhibitors (NRTIs and NNRTIs) for research.

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