Nucleoside — Reverse Transcriptase Inhibitor
The Role and Mechanism of Nucleoside Reverse Transcriptase Inhibitors (NRTIs)
Nucleoside Reverse Transcriptase Inhibitors (NRTIs) are a foundational class of antiretroviral drugs used primarily in the treatment of HIV-1 infection. Often referred to as "nukes," these agents structurally mimic naturally occurring nucleosides (the building blocks of DNA) to interfere with the viral replication cycle. nucleoside reverse transcriptase inhibitor
Because NRTIs lack a 3'-hydroxyl group, once they are incorporated into the growing viral DNA strand, no further nucleotides can be added. This prematurely stops the conversion of viral RNA into DNA, preventing the virus from replicating. Commonly Used NRTIs The Role and Mechanism of Nucleoside Reverse Transcriptase
NRTIs function as "prodrugs," meaning they are inactive upon entry and require by host cell kinases to become active triphosphate metabolites. Once activated, their mechanism follows two critical steps: This prematurely stops the conversion of viral RNA
Clinically approved NRTIs are frequently used in combination therapies to improve efficacy and reduce the risk of drug resistance. Notable examples include:
They compete with endogenous deoxynucleotides (like dTTP or dCTP) for binding to the viral Reverse Transcriptase (RT) enzyme .
