HIV nucleoside reverse transcriptase inhibitors

Franck Amblard; Dharmeshkumar Patel; Eleftherios Michailidis; Steven J Coats; Mahesh Kasthuri; Nicolas Biteau; Zahira Tber; Maryam Ehteshami; Raymond F Schinazi

doi:10.1016/j.ejmech.2022.114554

HIV nucleoside reverse transcriptase inhibitors

Eur J Med Chem. 2022 Oct 5:240:114554. doi: 10.1016/j.ejmech.2022.114554. Epub 2022 Jun 20.

Authors

Franck Amblard¹, Dharmeshkumar Patel¹, Eleftherios Michailidis¹, Steven J Coats¹, Mahesh Kasthuri¹, Nicolas Biteau¹, Zahira Tber¹, Maryam Ehteshami¹, Raymond F Schinazi²

Affiliations

¹ Center 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.
² Center 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. Electronic address: rschina@emory.edu.

PMID: 35792384
DOI: 10.1016/j.ejmech.2022.114554

Abstract

More than 40 years into the pandemic, HIV remains a global burden and as of now, there is no cure in sight. Fortunately, highly active antiretroviral therapy (HAART) has been developed to manage and suppress HIV infection. Combinations of two to three drugs targeting key viral proteins, including compounds inhibiting HIV reverse transcriptase (RT), have become the cornerstone of HIV treatment. This review discusses nucleoside reverse transcriptase inhibitors (NRTIs), including chain terminators, delayed chain terminators, nucleoside reverse transcriptase translocation inhibitors (NRTTIs), and nucleotide competing RT inhibitors (NcRTIs); focusing on their history, mechanism of action, resistance, and current clinical application, including long-acting regimens.

Keywords: HIV; Inhibitors; Nucleoside; Prodrug; RT; Reverse transcriptase.

Publication types

Review

MeSH terms

Anti-HIV Agents* / pharmacology
Anti-HIV Agents* / therapeutic use
Antiretroviral Therapy, Highly Active
Drug Resistance, Viral
HIV Infections* / drug therapy
HIV Reverse Transcriptase / metabolism
Humans
Nucleosides / pharmacology
Nucleosides / therapeutic use
Reverse Transcriptase Inhibitors / pharmacology

Substances

Anti-HIV Agents
Nucleosides
Reverse Transcriptase Inhibitors
HIV Reverse Transcriptase