A high-throughput screen for inhibitors of the prolyl isomerase, Pin1, identifies a seaweed polyphenol that reduces adipose cell differentiation. Mori, T., Hidaka, M., Ikuji, H., Yoshizawa, I., Toyohara, H., Okuda, T., Uchida, C., Asano, T., Yotsu-Yamashita, M., & Uchida, T. Bioscience, Biotechnology and Biochemistry, 2014. abstract bibtex © 2014 Japan Society for Bioscience, Biotechnology, and Agrochemistry. 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.
@article{
title = {A high-throughput screen for inhibitors of the prolyl isomerase, Pin1, identifies a seaweed polyphenol that reduces adipose cell differentiation},
type = {article},
year = {2014},
identifiers = {[object Object]},
keywords = {Adipose cell,High-throughput screen,Obesity,Prolyl isomerase,Seaweed polyphenol},
volume = {78},
id = {fdb49483-05f5-361d-8e58-ddba93b42d15},
created = {2018-02-28T22:42:48.647Z},
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last_modified = {2018-02-28T22:42:48.647Z},
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abstract = {© 2014 Japan Society for Bioscience, Biotechnology, and Agrochemistry. 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.},
bibtype = {article},
author = {Mori, T. and Hidaka, M. and Ikuji, H. and Yoshizawa, I. and Toyohara, H. and Okuda, T. and Uchida, C. and Asano, T. and Yotsu-Yamashita, M. and Uchida, T.},
journal = {Bioscience, Biotechnology and Biochemistry},
number = {5}
}
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