Recent advances in the identification of Tat-mediated transactivation inhibitors: progressing toward a functional cure of HIV. (March 2016)

• Record Type: Journal Article
• Authors: Tabarrini, Oriana; Desantis, Jenny; Massari, Serena
• Is Part Of: Future medicinal chemistry. Volume 8:Number 4(2016)
• Page Start: 421
• Page End: 442
• Publication Date: 2016-03
• Subjects: CDK inhibitors -- dCA -- didehydrocortistatine A -- functional cure -- HIV latency -- HIV reservoir -- HIV transcription inhibitors -- PPI -- TAR ligands -- Tat inhibitors -- transactivation; Pharmaceutical chemistry -- Periodicals; 615.19005
• DOI: 10.4155/fmc.16.3
• Languages: English
• ISSNs: 1756-8919

Abstract

The current anti-HIV combination therapy does not eradicate the virus that persists mainly in quiescent infected CD4 + T cells as a latent integrated provirus that resumes after therapy interruption. The Tat-mediated transactivation (TMT) is a critical step in the HIV replication cycle that could give the opportunity to reduce the size of latent reservoirs. More than two decades of research led to the identification of various TMT inhibitors. While none of them met the criteria to reach the market, the search for a suitable TMT inhibitor is still actively pursued. Really promising compounds, including one in a Phase III clinical trial, have been recently identified, thus warranting an update.