A benzothiophene‐carboxamide is a potent inhibitor of IL‐1β induced VCAM‐1 gene expression in human endothelial cells

FEBS Letters

Felts, Katherine A.¹  Mackman, Nigel³  Parry, Graham C.N.³  McKenzie, Thomas C.²  Cobb, Ronald R.¹ 

[1] Department of Biology, Tanabe Research Laboratories, 4540 Towne Centre Court, San Diego, CA 92121, USA;Department of Chemistry, Tanabe Research Laboratories, 4540 Towne Centre Court, San Diego, CA 92121, USA;Departments of Immunology and Vascular Biology, The Scripps Research Institute, La Jolla, CA 92037, USA

关键词: VCAM-1;    Inhibition;    Transcription;    Nuclear factor κB;    Benzothiopene-carboxamide;    ICAM-1;    intercellular adhesion molecule-1;    VCAM-1;    vascular cell adhesion molecule-1;    HUVEC;    human umbilical vein endothelial cells;    IL-1β;    interleukin-1β;    TNF-α;    tumor necrosis factor-α;    NF-κB;    nuclear factor-κB;    RT/PCR;    reverse transcriptase/polymerase chain reaction;    EMSA;    electrophoretic mobility shift assay;    TPCK;    N-tosyl-Phe-chloromethylketone;   

DOI  :  10.1016/0014-5793(96)00202-5

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Vascular endothelial cells respond to cytokines such as IL-1β or TNF-α by undergoing a number of functional alterations. Among these alterations is the induction of cell surface adhesion molecules, including VCAM-1. In this report, we investigated the effects of a 3-alkoxybenzo[β]thiopene-2-carboximide (BZT) on the cytokine induction of VCAM-1 expression and activation of the transcription factor NF-κB in human endothelial cells. BZT blocked the IL-1β induced cell surface expression of VCAM-1 in human endothelial cells but did not prevent nuclear translocation of NF-κB. This study demonstrates that BZT is a potent inhibitor of VCAM-1 expression in human endothelial cells.

【 授权许可】

Unknown