RRC ID |
36873
|
Author |
Watari A, Hashegawa M, Muangman T, Yagi K, Kondoh M.
|
Title |
Use of cell-based screening to identify small-molecule compounds that modulate claudin-4 expression.
|
Journal |
Biotechnol Lett
|
Abstract |
Claudins constitute a family of at least 27 proteins with four transmembrane domains, and play a pivotal role in maintaining tight-junctions seals in diverse epithelial tissues. The expression of claudin-4 often changes in intestinal tissues of inflammatory bowel disease and various human cancers. Therefore, claudin-4 is a promising target for treatment of these diseases. In our previous study, we established a reporter cell line to monitor claudin-4 expression on the basis of a functional claudin-4 promoter. Using this cell line, we have performed a cell-based screen of a library containing 2642 biologically active small-molecule compounds to identify modulators of claudin-4 expression. The screen identified 24 potential modulators of the claudin-4 promoter activity. Fourteen of these compounds (12 of them novel) induced endogenous claudin-4 expression. The identified compounds might serve as lead compounds targeting aberrant gene expression in inflammatory bowel disease.
|
Volume |
37(6)
|
Pages |
1177-85
|
Published |
2015-6-1
|
DOI |
10.1007/s10529-015-1791-7
|
PMID |
25700824
|
MeSH |
Cell Line
Claudin-4 / biosynthesis*
Cytological Techniques / methods*
Drug Evaluation, Preclinical / methods*
Gene Expression / drug effects*
Humans
Promoter Regions, Genetic
Transcriptional Activation*
|
IF |
1.977
|
Times Cited |
3
|
WOS Category
|
BIOTECHNOLOGY & APPLIED MICROBIOLOGY
|
Resource |
Human and Animal Cells |
MCF7(RCB1904) |