Inhibitory Effect of 4-(2-aminoethyl)-benzenesulfonyl Fluoride, a Serine Protease Inhibitor, on Pi3k Inhibitor-induced Chop Expression.
From: Department of Pharmacotherapy Graduate School of Biomedical Sciences, Hiroshima University, 1-2-3 Kasumi, Minami-ku, Hiroshima 734-8551, Japan.
European journal of pharmacology
- Publish Date: Jan 2007
- ISSN: 0014-2999
- Volume: 554
- Issue: 1
- Pages: 8-11
- Medium: Print
- Language: English
- Citation (JAMA): Hosoi Toru, Hyoda Kanae, Okuma Yasunobu, et al. Inhibitory Effect of 4-(2-aminoethyl)-benzenesulfonyl Fluoride, a Serine Protease Inhibitor, on Pi3k Inhibitor-induced Chop Expression.. Eur. J. Pharmacol. Jan 2007;554:8-11
Abstract
Endoplasmic reticulum stress contributes to several diseases such as neurodegenerative disorders and diabetes. In the previous report, we found that phosphatidylinositol 3-kinase (PI3K) down-regulation is important for inducing CHOP expression, an endoplasmic reticulum stress-induced transcription factor. In the present study, we investigated the effect of 4-(2-aminoethyl)-benzenesulfonyl fluoride (AEBSF), a serine protease inhibitor, on PI3K inhibitor-induced CHOP expression. We found that AEBSF completely inhibited PI3K inhibitor-induced CHOP expression at both mRNA and protein levels. It is suggested that AEBSF is an important drug from a pharmacological point of view and the results may have important implications for understanding endoplasmic reticulum stress-related diseases.
Mesh Headings (Keywords): 1-Phosphatidylinositol 3-Kinase, Animals, Cells, Cultured, Endoplasmic Reticulum, Gene Expression Regulation, Mice, RNA, Messenger, Serine Endopeptidases, Serine Proteinase Inhibitors, Sulfones, Transcription Factor CHOP
Check for Full Text / PubMed Unique Identifier (PMID): 17109853
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