Novel HIV-1 non-nucleoside reverse transcriptase inhibitors: A combinatorial approach
- Authors: Valuev-Elliston V.T.1, Kochetkov S.N.1
-
Affiliations:
- Engelhardt Institute of Molecular Biology
- Issue: Vol 82, No 13 (2017)
- Pages: 1716-1743
- Section: Review
- URL: https://journals.rcsi.science/0006-2979/article/view/151558
- DOI: https://doi.org/10.1134/S0006297917130107
- ID: 151558
Cite item
Abstract
Highly active antiretroviral therapy (HAART) is one of the most effective means for fighting against HIV-infec- tion. HAART primarily targets HIV-1 reverse transcriptase (RT), and 14 of 28 compounds approved by the FDA as anti- HIV drugs act on this enzyme. HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) hold a special place among HIV RT inhibitors owing to their high specificity and unique mode of action. Nonetheless, these drugs show a tendency to decrease their efficacy due to high HIV-1 variability and formation of resistant virus strains tolerant to clinically applied HIV NNRTIs. A combinatorial approach based on varying substituents within various fragments of the parent molecule that results in development of highly potent compounds is one of the approaches aimed at designing novel HIV NNRTIs. Generation of HIV NNRTIs based on pyrimidine derivatives explicitly exemplifies this approach, which is discussed in this review.
Keywords
About the authors
V. T. Valuev-Elliston
Engelhardt Institute of Molecular Biology
Author for correspondence.
Email: gansfaust@mail.ru
Russian Federation, Moscow, 119991
S. N. Kochetkov
Engelhardt Institute of Molecular Biology
Email: gansfaust@mail.ru
Russian Federation, Moscow, 119991