title: Beauvericin and enniatins H, I and MK1688 are new potent inhibitors of human immunodeficiency virus type-1 integrase.
abstract: Some enniatins (ENs) reportedly exhibit antiretroviral activities in vivo. The potential inhibitory activities of cyclic hexadepsipeptides such as beauvericin (BEA) and ENs H, I and MK1688 were investigated in vitro against human immunodeficiency virus type-1 (HIV-1) integrase and Moloney murine leukemia virus reverse transcriptase. BEA, EN I and EN MK1688 exhibited strong inhibitory activities against HIV-1 integrase, whereas EN H showed relatively weak activity. None of the examined compounds showed anti-reverse transcriptase activity. BEA was the most effective inhibitor of the tested cyclic hexadepsipeptides in inhibiting HIV-1 integrase. These results indicate the potential of cyclic hexadepsipeptides as a new class of potent inhibitors of HIV-1 integrase.
authors.affiliation: Department of Biotechnology, BET Research Institute, Chung-Ang University, Anseong, Gyeonggi, South Korea.
authors.forename: Cha-Gyun
authors.initials: CG
authors.lastname: Shin
authors.forename: Dog-Gn
authors.initials: DG
authors.lastname: An
authors.forename: Hyuk-Hwan
authors.initials: HH
authors.lastname: Song
authors.forename: Chan
authors.initials: C
authors.lastname: Lee
mesh_terms: D019380:Anti-HIV Agents / Q000494:pharmacology*; D047630:Depsipeptides / Q000494:pharmacology*; D019427:HIV Integrase / Q000378:metabolism*; D015497:HIV-1 / Q000187:drug effects*; D019429:Integrase Inhibitors / Q000494:pharmacology*; D019426:Integrases / Q000378:metabolism; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D008979:Moloney murine leukemia virus / Q000187:drug effects; D014764:Viral Proteins / Q000037:antagonists & inhibitors
chemical_list: D019380:Anti-HIV Agents; D047630:Depsipeptides; D019429:Integrase Inhibitors; C543476:MK 1688; D014764:Viral Proteins; C100264:enniatins; C004456:beauvericin; D019427:HIV Integrase; D019426:Integrases; C514801:p31 integrase protein, Human immunodeficiency virus 1