Target intelligence / Profile preview

Reverse transcriptase (specifically, HIV-1 reverse transcriptase) (RT)

Target
RT
Molecular classification
Enzyme, RNA-dependent DNA polymerase, Ribonuclease H
01

Overview

HIV-1 reverse transcriptase is a multifunctional enzyme essential for HIV replication, possessing both RNA-dependent and DNA-dependent DNA polymerase activities, as well as intrinsic ribonuclease H activity. During the HIV life cycle, this enzyme converts viral single-stranded RNA into double-stranded DNA, enabling integration into the host genome and continued viral propagation. Its central function has made it a primary target for antiretroviral drug development; both nucleoside/nucleotide analogs (NRTIs) and non-nucleoside inhibitors (NNRTIs) inhibit reverse transcriptase, forming the backbone of standard HIV treatment regimens. Drug resistance and toxicity remain clinically important challenges for therapies targeting this enzyme.

Other names
HIV-1 reverse transcriptaseHIV reverse transcriptaseRT (abbreviation)
02

Mechanism of action

Nucleoside/nucleotide reverse transcriptase inhibitors: Incorporated into viral DNA by HIV-1 reverse transcriptase, causing premature DNA chain termination, halting viral replication. Non-nucleoside reverse transcriptase inhibitors: Bind non-competitively to reverse transcriptase at an allosteric site, inducing conformational changes that inhibit enzyme function.

03

Biological functions

Reverse transcriptionRNA-dependent DNA polymerizationDNA-dependent DNA polymerizationRibonuclease H activityEssential for replication of retroviral genomes
04

Disease associations

Infection
05

Safety considerations

Mitochondrial toxicityPeripheral neuropathy, bone marrow suppressionResistance
06

Interacting drugs

Abacavir

13 more in the full profile.

07

Biomarkers

Viral load (HIV RNA copies/mL)HIV genotyping

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