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Updated: Sep 5, 2025

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors

Published on: May 9, 2025

HIV nucleoside reverse transcriptase inhibitors.

Franck Amblard¹, Dharmeshkumar Patel¹, Eleftherios Michailidis¹

¹Center for ViroScience and Cure, Laboratory of Biochemical Pharmacology, Department of Pediatrics, Emory University School of Medicine, and Children's Healthcare of Atlanta, 1760 Haygood Drive, Atlanta, GA, 30322, USA.

European Journal of Medicinal Chemistry

|July 6, 2022

Summary

This summary is machine-generated.

HIV remains a global challenge, but highly active antiretroviral therapy (HAART) manages the infection. This review covers nucleoside reverse transcriptase inhibitors (NRTIs), their mechanisms, resistance, and current use in long-acting regimens.

Keywords:

HIV Inhibitors Nucleoside Prodrug RT Reverse transcriptase

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Published on: January 30, 2019

Area of Science:

Virology
Infectious Diseases
Pharmacology

Background:

HIV/AIDS remains a significant global health burden over 40 years into the pandemic.
Highly active antiretroviral therapy (HAART) is crucial for managing and suppressing HIV infection.
Combinations of antiretroviral drugs, particularly those targeting HIV reverse transcriptase (RT), form the basis of current HIV treatment.

Purpose of the Study:

To provide a comprehensive review of nucleoside reverse transcriptase inhibitors (NRTIs) in HIV treatment.
To detail the history, mechanisms of action, and resistance patterns of various NRTI classes.
To discuss the current clinical applications of NRTIs, including emerging long-acting regimens.

Main Methods:

Literature review of scientific publications on HIV reverse transcriptase inhibitors.
Analysis of drug mechanisms, resistance pathways, and clinical trial data.
Synthesis of information on NRTI history, classification, and therapeutic use.

Main Results:

NRTIs are a cornerstone of HAART, acting through various mechanisms like chain termination and translocation inhibition.
Different classes of NRTIs, including chain terminators, delayed chain terminators, NRTTIs, and NcRTIs, have distinct properties.
Understanding NRTI resistance is critical for effective treatment strategies.
Long-acting NRTI regimens represent a significant advancement in HIV management.

Conclusions:

NRTIs are indispensable in managing HIV infection, with ongoing research into novel formulations and resistance mitigation.
The evolution of NRTIs has significantly improved patient outcomes and quality of life.
Future directions include optimizing long-acting NRTI therapies for sustained viral suppression and improved adherence.