title: Recent progress in the development of inhibitors of human immunodeficiency virus (HIV) integrase for the management of HIV infection.
abstract: Current therapy of acquired immune deficiency syndrome (AIDS) involves the use of a combination of at least three antiviral drugs to inhibit Human immunodeficiency virus 1 and 2 (HIV-1 and 2, in short HIV) replication via targeting of viral reverse transcriptase and protease. However, all anti-HIV drugs give rise to the new retroviral resistant strains. Therefore, new therapeutic agents against the emerging resistant HIV strains without secondary effects are very much needed. In HIV infection, the integration of viral DNA obtained from RNA genome into the chromosome of the host cell by viral integrase (IN) is essential for an effective viral replication. Moreover, no cellular IN has been found in the cells suggesting that viral IN appears to be one of the best candidates for the development of an antiviral drug. In recent years, promising results have proved that IN inhibitors are useful for treatment of retroviral infections. In this review, we briefly introduce IN and summarize potential inhibitors of IN, which are classified into several groups according to their origin and chemical structure. The resistance to the IN inhibitors is also discussed. Currently, several IN inhibitors are either being used in the clinical treatment or tested in clinical trials. Nevertheless, a great effort must be made to elicit wide knowledge with respect to the design of better viral inhibitors and the synthesis of new chemical derivatives with an anti-HIV activity.
authors.affiliation: School of Dentistry, Chung Shang Medical University, Taichung, Taiwan.
authors.forename: S S
authors.initials: SS
authors.lastname: Lin
authors.forename: F
authors.initials: F
authors.lastname: Xu
authors.forename: P H
authors.initials: PH
authors.lastname: Liao
authors.forename: C C
authors.initials: CC
authors.lastname: Yang
mesh_terms: D000818:Animals; D015658:HIV Infections / Q000188:drug therapy* / Q000821:virology; D019427:HIV Integrase / Q000378:metabolism; D019428:HIV Integrase Inhibitors / Q000494:pharmacology*; D015497:HIV-1 / Q000187:drug effects / Q000201:enzymology*; D006801:Humans
chemical_list: D019428:HIV Integrase Inhibitors; D019427:HIV Integrase