Related Experiment Video
Updated: Aug 26, 2026

Rapid Screening of HIV Reverse Transcriptase and Integrase Inhibitors
Published on: April 9, 2014
Efavirenz is a potent nonnucleoside reverse transcriptase inhibitor of HIV type 1 replication in microglia in vitro
A V Albright1, S Erickson-Viitanen, M O'Connor
1Departments of Neurology and Microbiology, University of Pennsylvania Medical Center, Philadelphia, Pennsylvania 19104, USA.
Abstract:
The objective of this study was to determine whether reverse transcriptase inhibitors (RTIs) could decrease viral replication in microglia. Human microglia obtained from individuals undergoing temporal lobectomy were cultured and infected with HIV-1 isolates from the central nervous system (CNS) as previously described (Strizki JM, et al. J Virol 1996;70:7654-7662). These microglial cultures were treated with one of three nucleoside RTIs (NRTIs) or with efavirenz, a nonnucleoside RTI (NNRTI), at various time points before and during HIV-1 infection. The drug levels sufficient to provide > 90% inhibition of microglial HIV replication (IC90) were determined by comparison of p24(gag) release in the cultures among treated and untreated microglia. Infectious virus released from the infected cultures was also measured with U373-MAGI-CCR5 cells. Efavirenz, an NNRTI, blocked HIV-1(DS-br) infection of microglia with an IC(90) of 0.7-7 nM. This value is similar to the efavirenz IC(90) values for inhibition of laboratory and clinical isolates in lymphocytes, is 2-3 logs lower than the IC90 values of AZT and d4T, and is 1-2 logs lower than that of ddC in microglia. Efavirenz also inhibited infection with other neurotropic isolates, and with viruses isolated from other compartments that also replicated well in microglia. Thus, efavirenz is a potent inhibitor of HIV-1 infection in microglia. Furthermore, efavirenz IC(90) drug levels are present in the cerebrospinal fluid (CSF) of patients taking this once daily NNRTI.
More Related Videos
07:22A High-throughput Cre-Lox Activated Viral Membrane Fusion Assay to Identify Inhibitors of HIV-1 Viral Membrane Fusion
Published on: August 14, 2018
10:29Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
Published on: May 9, 2025
Related Concept Videos
Retrovirus Life Cycles
Retroviruses
Inhibitors of Viral Protein Synthesis
Inhibitors Of Virion Release
Antiviral Nucleoside Inhibitors
Inhibitors of Virion Maturation and Assembly