title: Recent advances in the identification of Tat-mediated transactivation inhibitors: progressing toward a functional cure of HIV.
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.
authors.affiliation: Department of Pharmaceutical Sciences, University of Perugia, Via del Liceo 1, 06123 Perugia, Italy.
authors.forename: Oriana
authors.initials: O
authors.lastname: Tabarrini
authors.affiliation: Department of Pharmaceutical Sciences, University of Perugia, Via del Liceo 1, 06123 Perugia, Italy.
authors.forename: Jenny
authors.initials: J
authors.lastname: Desantis
authors.affiliation: Department of Pharmaceutical Sciences, University of Perugia, Via del Liceo 1, 06123 Perugia, Italy.
authors.forename: Serena
authors.initials: S
authors.lastname: Massari
mesh_terms: D019380:Anti-HIV Agents / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use*; D015658:HIV Infections / Q000188:drug therapy* / Q000821:virology; D015497:HIV-1 / Q000187:drug effects* / Q000235:genetics* / Q000254:growth & development; D006801:Humans; D015533:Transcriptional Activation / Q000187:drug effects*; D014779:Virus Replication / Q000187:drug effects / Q000235:genetics; D054322:tat Gene Products, Human Immunodeficiency Virus / Q000378:metabolism*
chemical_list: D019380:Anti-HIV Agents; D054322:tat Gene Products, Human Immunodeficiency Virus
keywords: CDK inhibitors; HIV latency; HIV reservoir; HIV transcription inhibitors; PPI; TAR ligands; Tat inhibitors; dCA; didehydrocortistatine A; functional cure; transactivation