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Updated: Aug 16, 2026

Quantitative Structure-Activity Relationship, Activity Prediction, and Molecular Dynamics of Non-nucleotide Reverse Transcriptase Inhibitors
Published on: May 9, 2025
Cardiomyopathy, nucleoside reverse transcriptase inhibitors and mitochondria are linked through AIDS and its therapy
1Department of Pathology, Emory University, 101 Woodruff Circle, WMB, Room 7117, Atlanta, GA 30322, USA. wlewis@emory.edu
Abstract:
Nucleoside reverse transcriptase inhibitors (NRTIs) in highly active antiretroviral therapy (HAART) bring serious side effects to light. Mitochondrial dysfunction, mtDNA replication defects and mtDNA depletion in target tissues are observed experimentally and clinical confirmation is present in some cases. Organ-specific pathological changes, particularly in the cardiovascular system, result from and are frequently attributed to HAART where NRTIs are included. Mechanisms of mitochondrial toxicity are incompletely understood, but could reasonably relate to inhibition of DNA polymerase-gamma (the enzyme responsible for mtDNA replication in eukaryotes) by pharmacologically active NRTI triphosphates. Cellular and biological implications of the pharmacologic events are addressed.
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