Target intelligence / Profile preview

Human immunodeficiency virus reverse transcriptase enzyme (HIV RT)

Target
HIV RT
Molecular classification
Enzyme, Polymerase, Ribonuclease H (RNase H), Viral enzyme
01

Overview

Human immunodeficiency virus reverse transcriptase enzyme (HIV RT) is a multifunctional viral enzyme essential for the replication of HIV. It exhibits both RNA-dependent and DNA-dependent DNA polymerase activities, as well as ribonuclease H (RNase H) activity. These functions allow HIV RT to convert the single-stranded viral RNA genome into double-stranded DNA, which can then be integrated into the host cell genome. Structurally, HIV RT is a heterodimer composed of p66 and p51 subunits, with the polymerase and RNase H active sites residing on p66. It is the primary molecular target of multiple classes of antiretroviral drugs used in HIV therapy, including NRTIs and NNRTIs. Inhibition of HIV RT prevents viral replication and is central to current HIV/AIDS treatment strategies[1][2][3][4][5].

Other names
HIV reverse transcriptaseHIV-1 reverse transcriptaseRTRetroviral reverse transcriptase
02

Mechanism of action

Inhibition of RNA-dependent DNA polymerase activity (NRTIs/NNRTIs) Chain termination of viral DNA synthesis (NRTIs) Allosteric inhibition of reverse transcriptase structure (NNRTIs) Inhibition of RNase H enzymatic activity (RNase H inhibitors)

03

Biological functions

Viral genome replicationReverse transcription (RNA-dependent DNA polymerase activity)DNA-dependent DNA polymerase activityRNA hydrolysis (RNase H activity)
04

Disease associations

Infection, specifically Human immunodeficiency virus (HIV) infection and Acquired immunodeficiency syndrome (AIDS)
05

Safety considerations

Drug resistance due to mutations in RT genemitochondrial toxicity (especially with older NRTIs)hypersensitivity reactions (e.g., abacavir)hepatotoxicitycentral nervous system side effects (e.g., efavirenz)lipodystrophylactic acidosis
06

Interacting drugs

zidovudine (AZT)

13 more in the full profile.

07

Biomarkers

HIV viral load in plasma (surrogate of RT activity and replication)HIV genotypic resistance mutations in RT gene

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