Abstract
Vascular endothelial cells respond to cytokines such as IL-1 beta or TNF-alpha 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[beta]thiophene-2-carboxamide (BZT) on the cytokine induction of VCAM-1 expression and activation of the transcription factor NF-kappa B in human endothelial cells. BZT blocked the IL-1 beta induced cell surface expression of VCAM-1 in human endothelial cells but did not prevent nuclear translocation of NF-kappa B. This study demonstrates that BZT is a potent inhibitor of VCAM-1 expression in human endothelial cells.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Base Sequence
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Biological Transport
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Cell Nucleus / metabolism
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Cells, Cultured
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Endothelium, Vascular / cytology
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Endothelium, Vascular / drug effects
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Endothelium, Vascular / metabolism*
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Gene Expression Regulation / drug effects*
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Humans
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Interleukin-1 / pharmacology*
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Molecular Sequence Data
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NF-kappa B / metabolism*
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Promoter Regions, Genetic
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RNA, Messenger / analysis
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Thiophenes / chemical synthesis
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Thiophenes / pharmacology*
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Tosylphenylalanyl Chloromethyl Ketone / pharmacology
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Umbilical Veins
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Vascular Cell Adhesion Molecule-1 / genetics*
Substances
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Interleukin-1
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NF-kappa B
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RNA, Messenger
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Thiophenes
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Vascular Cell Adhesion Molecule-1
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3-isopropoxy-5-methoxybenzo(b)thiophene-2-carboxamide
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Tosylphenylalanyl Chloromethyl Ketone