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Biosci Biotechnol Biochem. 2014;78(5):832-8. doi: 10.1080/09168451.2014.905189. Epub 2014 Apr 17.

A high-throughput screen for inhibitors of the prolyl isomerase, Pin1, identifies a seaweed polyphenol that reduces adipose cell differentiation.

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  • 1a Molecular Enzymology, Department of Molecular Cell Science, Graduate School of Agricultural Science , Tohoku University , Sendai , Japan.

Abstract

The peptidyl prolyl cis/trans isomerase Pin1 enhances the uptake of triglycerides and the differentiation of fibroblasts into adipose cells in response to insulin stimulation. Pin1 downregulation could be a potential approach to prevent and treat obesity-related disorders. In order to identify an inhibitor of Pin1 that exhibited minimal cytotoxicity, we established a high-throughput screen for Pin1 inhibitors and used this method to identify an inhibitor from 1,056 crude fractions of two natural product libraries. The candidate, a phlorotannin called 974-B, was isolated from the seaweed, Ecklonia kurome. 974-B inhibited the differentiation of mouse embryonic fibroblasts and 3T3-L1 cells into adipose cells without inducing cytotoxicity. We discovered the Pin1 inhibitor, 974-B, from the seaweed, E. kurome, and showed that it blocks the differentiation of fibroblasts into adipose cells, suggesting that 974-B could be a lead drug candidate for obesity-related disorders.

KEYWORDS:

adipose cell; high-throughput screen; obesity; prolyl isomerase; seaweed polyphenol

PMID:
25035986
[PubMed - indexed for MEDLINE]
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