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Inhibitors of HIV-1 Tat-Mediated Transactivation

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The transactivation responsive (TAR) RNA is the 5'-leader sequence of the HIV-1 mRNA genome and interacts with the Tat protein during transcription. Tat and the positive transcription elongation factor (PTEFb) complex bind to TAR to promote efficient transcription of the full-length HIV genome. In the absence of the TAR█Tat█P-TEFb interaction, viral transcription is inefficient, which makes this RNA-protein complex an important target for therapeutic intervention of HIV replication. Inhibitors of HIV-1 transactivation mainly target: 1) TAR RNA, 2) Tat protein and 3) Tat█P-TEFb complex. 1) Compounds against TAR RNA are the most numerous: besides cationic peptides, which were initially developed, recent advances in TAR binding inhibitors include oligonucleotide based-agents and small molecules. Specific research efforts are currently underway to increase cellular uptake. 2) By targeting the Tat protein, both transactivation and other Tatmediated intra/extracellular functions are affected. Various biopolymeric drugs are reported to effectively inhibit Tat activity. In addition, Tat-targeted antibodies have recently been developed. 3) Intracellular proteins have been discovered to disrupt Tat█P-TEFb interaction, raising the chance of inhibiting HIV-1 transcription via novel mechanisms.

Keywords: HIV-1; Inhibitors; P-TEFb; TAR RNA; Tat; Transactivation

Document Type: Research Article


Affiliations: Department of Histology, Microbiology and Medicinal Biotechnologies, University of Padova, via Gabelli 63, 35123 Padova, Italy.

Publication date: May 1, 2006

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.

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