Target intelligence / Profile preview

HIV-1 reverse transcriptase (RT) (HIV-1 RT)

Target
HIV-1 RT
Molecular classification
Enzyme
01

Overview

HIV-1 reverse transcriptase (RT) is a multifunctional enzyme essential for the replication of the human immunodeficiency virus type 1 (HIV-1) [7, 16]. It catalyzes the conversion of the single-stranded viral RNA genome into double-stranded DNA, a process known as reverse transcription, which allows the viral genetic material to be integrated into the host cell's genome [6, 8]. RT is a heterodimer composed of p66 and p51 subunits and exhibits three enzymatic activities: RNA-dependent DNA polymerase, DNA-dependent DNA polymerase, and ribonuclease H (RNase H) [7, 9]. As a cornerstone of antiretroviral therapy (ART), RT is targeted by nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs) and non-nucleoside reverse transcriptase inhibitors (NNRTIs) [10, 19]. Abacavir is a potent NRTI that, after intracellular conversion to its active metabolite carbovir triphosphate, competes with natural dGTP for incorporation into the nascent DNA strand, resulting in premature chain termination and inhibition of viral replication [1, 5].

Other names
RNA-directed DNA polymerasePolp66/p51 heterodimerReverse transcriptase
02

Mechanism of action

Nucleoside reverse transcriptase inhibitor (NRTI); competitive inhibition of the polymerase active site and DNA chain termination [1, 5, 7].

03

Biological functions

Other
04

Disease associations

Infection
05

Safety considerations

Abacavir hypersensitivity syndromeDrug resistance mutationsCardiovascular risk (myocardial infarction)Mitochondrial toxicity
06

Interacting drugs

Abacavir

9 more in the full profile.

07

Biomarkers

HLA-B*5701HIV-1 RNA viral loadCD4+ T-cell countM184V mutationK65R mutation

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