Abstract
Human Immunodeficiency Virus type 1 Reverse Transcriptase (HIV-1 RT) is one of the most important targets for treatment of Acquired Immune Deficiency Syndrome (AIDS). It catalyzes the reverse transcription of HIV-RNA into a double stranded DNA, and the knowledge of its substrate specificity and catalytic mechanism has guided the development of several inhibitors widely used on current HIV/AIDS therapy. However, mutations in HIV-1 RT structure can lead to the emergence of drug-resistant virus strains. The goal of this review is to summarize relevant structural features of HIV-1 RT and its inhibitors in such a way that this cost-effective target in the development of new antiretroviral drugs is particularly highlighted.
Keywords: Reverse transcriptase, nucleoside, nucleotide, non-nucleoside, DNA, RNA, antiretroviral, AIDS
Current Medicinal Chemistry
Title: HIV-1 Reverse Transcriptase: A Therapeutical Target in the Spotlight
Volume: 13 Issue: 3
Author(s): H. C. Castro, N. I.V. Loureiro, M. Pujol-Luz, A. M.T. Souza, M. G. Albuquerque, D. O. Santos, L. M. Cabral, I. C. Frugulhetti and C. R. Rodrigues
Affiliation:
Keywords: Reverse transcriptase, nucleoside, nucleotide, non-nucleoside, DNA, RNA, antiretroviral, AIDS
Abstract: Human Immunodeficiency Virus type 1 Reverse Transcriptase (HIV-1 RT) is one of the most important targets for treatment of Acquired Immune Deficiency Syndrome (AIDS). It catalyzes the reverse transcription of HIV-RNA into a double stranded DNA, and the knowledge of its substrate specificity and catalytic mechanism has guided the development of several inhibitors widely used on current HIV/AIDS therapy. However, mutations in HIV-1 RT structure can lead to the emergence of drug-resistant virus strains. The goal of this review is to summarize relevant structural features of HIV-1 RT and its inhibitors in such a way that this cost-effective target in the development of new antiretroviral drugs is particularly highlighted.
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Castro C. H., Loureiro I.V. N., Pujol-Luz M., Souza M.T. A., Albuquerque G. M., Santos O. D., Cabral M. L., Frugulhetti C. I. and Rodrigues R. C., HIV-1 Reverse Transcriptase: A Therapeutical Target in the Spotlight, Current Medicinal Chemistry 2006; 13 (3) . https://dx.doi.org/10.2174/092986706775476089
DOI https://dx.doi.org/10.2174/092986706775476089 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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