HIV-1 reverse transcriptase: a therapeutical target in the spotlight

• Published in: Current medicinal chemistry Vol. 13; no. 3; p. 313
• Main Authors: Castro, H C, Loureiro, N I V, Pujol-Luz, M, Souza, A M T, Albuquerque, M G, Santos, D O, Cabral, L M, Frugulhetti, I C, Rodrigues, C R
• Format: Journal Article
• Language: English
• Published: United Arab Emirates 01-02-2006
• Subjects: Drug Resistance, Viral; HIV Infections - drug therapy; HIV Reverse Transcriptase - chemistry; HIV Reverse Transcriptase - drug effects; HIV Reverse Transcriptase - genetics; HIV-1 - enzymology; HIV-1 - genetics; HIV-1 - physiology; Humans; Models, Molecular; Protein Conformation; Reverse Transcriptase Inhibitors - pharmacology; Reverse Transcriptase Inhibitors - therapeutic use; Virus Replication
• ISSN: 0929-8673
• DOI: 10.2174/092986706775476089

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.