New targets and novel antiretrovirals
Abstract
Highly active antiretroviral therapy (HAART) has to date been based on use of a triple combination of drugs chosen from three classes of antiretrovirals (ARVs), nucleoside reverse transcriptase inhibitors (NRTIs), non-nucleoside reverse transcriptase inhibitors (NNRTIs) and protease inhibitors (PIs). These ARV classes target two of the three virally encoded enzymes necessary for viral replication after entry of HIV into the host cell. A greater understanding of the viral-host interactions necessary for new infection of CD4 cells has led to the development of compounds able to inhibit viral entry. The novel fusion inhibitor T-20 has entered clinical use and has a particular role in salvage therapy of patients with HIV strains resistant to present classes of ARVs. Co-receptor inhibitors have shown in vivo antiviral activity and are now entering phase III development. Integrase (IN), the third viral enzyme encoded by the pol gene, has remained an elusive target. Compounds with low toxicity and able to inhibit (IN) are now entering phase II clinical development. These new HIV treatment modalities represent a significant advance in and addition to our anti-HIV armamentarium. This review will outline the mechanisms of action of entry inhibitors and IN inhibitors and discuss the lead compounds within each class.
Southern African Journal of HIV Medicine Vol. 6 (4) 2005: pp. 49-51
The author(s) retain copyright on work published by AOSIS unless specified otherwise.
Licensing and publishing rights
Author(s) of work published by AOSIS are required to grant AOSIS the unlimited rights to publish the definitive work in any format, language and medium, for any lawful purpose. AOSIS requires journal authors to publish their work in open access under the Creative Commons Attribution 4.0 International (CC BY 4.0) licence.
Read more here: http://creativecommons.org/licenses/by/4.0/.
The authors retain the non-exclusive right to do anything they wish with the published article(s), provided attribution is given to the applicable journal with details of the original publication, as set out in the official citation of the article published in the journal. The retained right specifically includes the right to post the article on the authors’ or their institution’s websites or in institutional repositories.
Previously published work may have been published under a different licence. We advise the community that if they would like to reuse the work to consult the applicable licence at article level.
