Target intelligence / Profile preview

HIV antiretroviral drug targets (ART targets)

Target
ART targets
Molecular classification
Enzyme, Receptor, Structural protein, Other
01

Overview

HIV antiretroviral drug targets refers to a collective group of viral and host proteins essential for the replication and survival of the Human Immunodeficiency Virus (HIV) (National HIV Curriculum, 2025). The primary viral targets include three essential enzymes: reverse transcriptase, which converts viral RNA into DNA; integrase, which inserts viral DNA into the host genome; and protease, which cleaves viral polyproteins into functional units for virion maturation (Patsnap Synapse, 2025; PubMed, 2016). Additionally, the viral envelope glycoproteins gp120 and gp41, along with the host cell receptors CD4 and CCR5, serve as critical targets for entry inhibitors that prevent the virus from infecting new cells (PMC, 2022; YouTube, 2024). Recent advancements have also established the HIV-1 capsid protein as a potent target, with inhibitors like lenacapavir disrupting multiple stages of the viral life cycle, including nuclear uptake and assembly (PMC, 2022; Drug Target Review, 2024). Drugs targeting these molecules are typically used in combination (cART) to suppress viral load, preserve immune function, and prevent the emergence of drug resistance (Aidsmap, 2024). Monitoring efficacy and safety involves tracking biomarkers such as plasma HIV-1 RNA levels and CD4+ T-cell counts, while managing challenges like metabolic side effects and long-term chronic inflammation (PMC, 2021; PMC, 2023).

Other names
HIV-1 drug targetsAntiretroviral therapy targetsHIV replication cycle proteinsHIV-1 enzymes and entry receptors
02

Mechanism of action

Inhibition of reverse transcription via chain termination or allosteric modulation; inhibition of viral DNA integration into the host genome; inhibition of proteolytic cleavage of viral polyproteins; blocking of viral attachment, co-receptor binding, or membrane fusion; and disruption of capsid-mediated nuclear uptake and virion assembly.

03

Biological functions

Viral replicationReverse transcriptionViral DNA integrationProteolysisViral entryCapsid assembly and disassemblyNuclear transport
04

Disease associations

InfectionAcquired Immunodeficiency Syndrome (AIDS)Multi-drug resistant HIV infection
05

Safety considerations

Development of drug resistance mutationsHepatotoxicityMetabolic dysfunction (dyslipidemia, insulin resistance)Weight gainHypersensitivity reactionsChronic immune activation and inflammationInjection site reactions
06

Interacting drugs

Tenofovir

16 more in the full profile.

07

Biomarkers

Plasma HIV-1 RNA (Viral load)CD4+ T-lymphocyte countHIV-1 genotypic and phenotypic resistance mutationsHLA-B*5701 alleleCCR5 tropismInterleukin-6 (IL-6)High-sensitivity C-reactive protein (hs-CRP)D-dimer

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