A benzothiophene-carboxamide is a potent inhibitor of IL-1beta induced VCAM-1 gene expression in human endothelial cells.
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.
Cobb
R R
RR
Department of Biology, Tanabe Research Laboratories, San Diego, CA 92121, USA.
Felts
K A
KA
McKenzie
T C
TC
Parry
G C
GC
Mackman
N
N
D001483:Base Sequence; D001692:Biological Transport; D002467:Cell Nucleus / Q000378:metabolism; D002478:Cells, Cultured; D004730:Endothelium, Vascular / Q000166:cytology / Q000187:drug effects / Q000378:metabolism*; D005786:Gene Expression Regulation / Q000187:drug effects*; D006801:Humans; D007375:Interleukin-1 / Q000494:pharmacology*; D008969:Molecular Sequence Data; D016328:NF-kappa B / Q000378:metabolism*; D011401:Promoter Regions, Genetic; D012333:RNA, Messenger / Q000032:analysis; D013876:Thiophenes / Q000138:chemical synthesis / Q000494:pharmacology*; D014108:Tosylphenylalanyl Chloromethyl Ketone / Q000494:pharmacology; D014471:Umbilical Veins; D019010:Vascular Cell Adhesion Molecule-1 / Q000235:genetics*
D007375:Interleukin-1; D016328:NF-kappa B; D012333:RNA, Messenger; D013876:Thiophenes; D019010:Vascular Cell Adhesion Molecule-1; C098969:3-isopropoxy-5-methoxybenzo(b)thiophene-2-carboxamide; D014108:Tosylphenylalanyl Chloromethyl Ketone