메뉴 건너뛰기




Volumn 14, Issue 17, 2004, Pages 4483-4486

Anti-HIV activity of some synthetic lignanolides and intermediates

Author keywords

Anti HIV 1; HIV 1 promoter activation; HIV 1 Tat protein; Synthetic lignanolides; Transcription factor NF B

Indexed keywords

ANTI HUMAN IMMUNODEFICIENCY VIRUS AGENT; IMMUNOGLOBULIN ENHANCER BINDING PROTEIN; LIGNAN DERIVATIVE; MACROLIDE; TRANSACTIVATOR PROTEIN; TRANSCRIPTION FACTOR;

EID: 3843105997     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2004.06.047     Document Type: Article
Times cited : (16)

References (27)
  • 10
    • 3843077829 scopus 로고    scopus 로고
    • note
    • TAR is a cis-activating stem-loop RNA structure called transactivating response element present in the HIV-1 LTR promoter. Through interaction with TAR, Tat recruits a host cell protein kinase complex, p-TEFb (CDK9 and CycT) that binds to the loop region of TAR. As a consequence of the p-TEFb recruitment to the HIV-1 promoter complex, the C-terminal domain (CTD) of the RNA polymerase II is phosphorylated increasing the efficiency of transcription elongation
  • 15
    • 3843110446 scopus 로고    scopus 로고
    • note
    • 2, 1 mM DTT, 1% Triton X-100, and 7% glycerol and luciferase activity was measured using an Autolumat LB 953 (EG & G Berthold, USA) following the instructions of the luciferase assay kit (Promega, Madison, WI, USA). TNFα induces an average of 15-20 fold induction of the luciferase activity compared to nonstimulated cells and this represent the index of transactivation that is represented in our experiment as the maximum levels of TNFα-induced NF- κ B activation (100%).
  • 16
    • 3843099644 scopus 로고    scopus 로고
    • note
    • 5 cells/mL), seeded the day before the assay, were treated either with the CDK9 inhibitor DRB, as a positive control, or with three doses of the compounds tested. After 12 h, the cells were washed twice with PBS and the luciferase activity measured as indicated for 5.1 cells
  • 18
    • 3843105058 scopus 로고    scopus 로고
    • note
    • 5 cells/mL) were seeded the day before the assay, and then stimulated with doxycycline (1 μg/mL) in the presence or absence of the compounds for 6 h. Then, the cells were washed twice in PBS, lysed and the luciferase activity measured as described
  • 19
    • 3843076717 scopus 로고    scopus 로고
    • in preparation
    • García et al., in preparation
    • García1
  • 24
    • 3843135467 scopus 로고    scopus 로고
    • note
    • 6 cells/mL were treated with the compounds for 24 h or 48 h at 37°C. Then, collected, resuspended in PBS and analysed by flow cytometry after Propidium Iodide staining to determine the cell death percentage. All the results, showed as % of cell death or CC50 values, were calculated by GraphPad software
  • 25
    • 3843115925 scopus 로고    scopus 로고
    • note
    • 50 values, calculated by GraphPad software


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.