Fungal Phenalenones Inhibit HIV-1 Integrase

被引：0
|
作者：
Kazuro Shiomi
Ryosuke Matsui
Miki Isozaki
Harumi Chiba
Takahiro Sugai
Yuichi Yamaguchi
Rokuro Masuma
Hiroshi Tomoda
Tomoko Chiba
Hua Yan
Yoshihiro Kitamura
Wataru Sugiura
Satoshi Ōmura
Haruo Tanaka
机构：
[1] School of Pharmaceutical Sciences Kitasato University,
[2] The Kitasato Institute,undefined
[3] Kitasato Institute for Life Sciences,undefined
[4] Kitasato University,undefined
[5] AIDS Research Center,undefined
[6] National Institute of Infectious Diseases,undefined
[7] Advanced Clinical Research Center,undefined
[8] Institute of Medical Science,undefined
[9] The University of Tokyo,undefined
来源：
The Journal of Antibiotics | 2005年 / 58卷
关键词：
enzyme inhibitor; HIV interase; AIDS; phenalenone;
D O I：
暂无
中图分类号：
学科分类号：
摘要：
A phenalenone compound, atrovenetinone methyl acetal, was isolated from a culture broth of Penicillium sp. FKI-1463 as an HIV-1 integrase inhibitor, and it showed anti-HIV activity in vitro. HIV-1 integrase inhibition and anti-HIV activity of two other natural phenalenones were also studied. Among the tested compounds, funalenone inhibited HIV-1 integrase with an IC50 value of 10 µM and showed the best selectivity (anti-HIV, IC50=1.7 µM; cytotoxicity, IC50=87 µM).
引用
收藏
页码：65 / 68
页数：3
相关论文
共 50 条
  • [41] Uneven Genetic Robustness of HIV-1 Integrase
    Rihn, Suzannah J.
    Hughes, Joseph
    Wilson, Sam J.
    Bieniasz, Paul D.
    JOURNAL OF VIROLOGY, 2015, 89 (01) : 552 - 567
  • [42] Strategies for identification of HIV-1 integrase inhibitors
    Ramcharan, Joseph
    Skalka, Anna Marie
    FUTURE VIROLOGY, 2006, 1 (06) : 717 - 731
  • [43] Design and discovery of HIV-1 integrase inhibitors
    Neamati, N
    Sunder, S
    Pommier, Y
    DRUG DISCOVERY TODAY, 1997, 2 (11) : 487 - 498
  • [44] HIV-1 integrase pharmacophore identification.
    Hong, HX
    Wang, SM
    Nicklause, MC
    Milne, GWA
    ABSTRACTS OF PAPERS OF THE AMERICAN CHEMICAL SOCIETY, 1997, 213 : 38 - COMP
  • [45] Screening and identification of inhibitors on HIV-1 integrase
    Zou Yuan
    Zhan Jin-Biao
    PROGRESS IN BIOCHEMISTRY AND BIOPHYSICS, 2007, 34 (09) : 965 - 970
  • [46] HIV-1 Integrase Multimerization as a Therapeutic Target
    Feng, Lei
    Larue, Ross C.
    Slaughter, Alison
    Kessl, Jacques J.
    Kvaratskhelia, Mamuka
    FUTURE OF HIV-1 THERAPEUTICS: RESISTANCE IS FUTILE?, 2015, 389 : 93 - 119
  • [47] HIV-1 integrase SUMOylation and viral replication
    Alessia Zamborlini
    Audrey Coiffic
    Guillaume Beauclair
    Olivier Delelis
    Joris Paris
    Fabien Magne
    Yashuiro Koh
    Marie-Lou Giron
    Joelle Tobaly-Tapiero
    Stephane Emiliani
    Alan Engelman
    Hugues de The
    Ali Saib
    Retrovirology, 8 (Suppl 2)
  • [48] Allosteric inhibition of HIV-1 integrase activity
    Engelman, Alan
    Kessl, Jacques J.
    Kvaratskhelia, Mamuka
    CURRENT OPINION IN CHEMICAL BIOLOGY, 2013, 17 (03) : 339 - 345
  • [49] Stereospecificity of reactions catalyzed by HIV-1 integrase
    Gerton, JL
    Herschlag, D
    Brown, PO
    JOURNAL OF BIOLOGICAL CHEMISTRY, 1999, 274 (47) : 33480 - 33487
  • [50] Integrase inhibitors in the treatment of HIV-1 infection
    Powderly, William G.
    JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY, 2010, 65 (12) : 2485 - 2488
12345