Reverse transcriptase inhibitors are antiretroviral agents that block reverse transcriptase, the viral enzyme that copies single-stranded RNA into proviral DNA during the replication cycle of HIV and other retroviruses. By halting this step, the drugs prevent integration of viral genetic material into the host genom…
Reverse transcriptase inhibitors are antiretroviral agents that block reverse transcriptase, the viral enzyme that copies single-stranded RNA into proviral DNA during the replication cycle of HIV and other retroviruses. By halting this step, the drugs prevent integration of viral genetic material into the host genome and suppress production of new virions. Two principal pharmacological classes are distinguished by mechanism. Nucleoside and nucleotide reverse transcriptase inhibitors are chain-terminating substrate analogues that, once phosphorylated, are incorporated into the growing DNA strand and stop further elongation; this same affinity for cellular polymerases underlies off-target effects such as the inhibition of telomerase. Non-nucleoside reverse transcriptase inhibitors instead bind allosterically near the enzyme's catalytic site, distorting its conformation. These agents form the backbone of combination antiretroviral therapy and highly active antiretroviral regimens, where multiple drug classes are paired to maximize viral suppression and limit resistance. Clinically relevant concerns addressed in the literature include the emergence of HIV drug resistance through reverse transcriptase mutations, adverse drug reactions, mitochondrial toxicity manifesting as lactic acidosis, and peripheral neuropathy. Structure-based docking and phytochemical screening continue to inform the search for novel reverse transcriptase and protease inhibitors.
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