Identification of adiponectin receptor agonist utilizing a fluorescence polarization based high throughput assay.

Adiponectin, the adipose-derived hormone, plays an important role in the suppression of metabolic disorders that can result in type 2 diabetes, obesity, and atherosclerosis. It has been shown that up-regulation of adiponectin or adiponectin receptor has a number of therapeutic benefits. Given that i...

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Autores principales:	Yiyi Sun, Zhihe Zang, Ling Zhong, Min Wu, Qing Su, Xiurong Gao, Wang Zan, Dong Lin, Yan Zhao, Zhonglin Zhang
Formato:	article
Lenguaje:	EN
Publicado:	Public Library of Science (PLoS) 2013
Materias:	Medicine R Science Q
Acceso en línea:	https://doaj.org/article/46d1e5eb95024aab8493a46e430b0493
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spelling	oai:doaj.org-article:46d1e5eb95024aab8493a46e430b04932021-11-18T07:45:51ZIdentification of adiponectin receptor agonist utilizing a fluorescence polarization based high throughput assay.1932-620310.1371/journal.pone.0063354https://doaj.org/article/46d1e5eb95024aab8493a46e430b04932013-01-01T00:00:00Zhttps://www.ncbi.nlm.nih.gov/pmc/articles/pmid/23691032/?tool=EBIhttps://doaj.org/toc/1932-6203Adiponectin, the adipose-derived hormone, plays an important role in the suppression of metabolic disorders that can result in type 2 diabetes, obesity, and atherosclerosis. It has been shown that up-regulation of adiponectin or adiponectin receptor has a number of therapeutic benefits. Given that it is hard to convert the full size adiponectin protein into a viable drug, adiponectin receptor agonists could be designed or identified using high-throughput screening. Here, we report on the development of a two-step screening process to identify adiponectin agonists. First step, we developed a high throughput screening assay based on fluorescence polarization to identify adiponectin ligands. The fluorescence polarization assay reported here could be adapted to screening against larger small molecular compound libraries. A natural product library containing 10,000 compounds was screened and 9 hits were selected for validation. These compounds have been taken for the second-step in vitro tests to confirm their agonistic activity. The most active adiponectin receptor 1 agonists are matairesinol, arctiin, (-)-arctigenin and gramine. The most active adiponectin receptor 2 agonists are parthenolide, taxifoliol, deoxyschizandrin, and syringin. These compounds may be useful drug candidates for hypoadiponectin related diseases.Yiyi SunZhihe ZangLing ZhongMin WuQing SuXiurong GaoWang ZanDong LinYan ZhaoZhonglin ZhangPublic Library of Science (PLoS)articleMedicineRScienceQENPLoS ONE, Vol 8, Iss 5, p e63354 (2013)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine R Science Q
spellingShingle	Medicine R Science Q Yiyi Sun Zhihe Zang Ling Zhong Min Wu Qing Su Xiurong Gao Wang Zan Dong Lin Yan Zhao Zhonglin Zhang Identification of adiponectin receptor agonist utilizing a fluorescence polarization based high throughput assay.
description	Adiponectin, the adipose-derived hormone, plays an important role in the suppression of metabolic disorders that can result in type 2 diabetes, obesity, and atherosclerosis. It has been shown that up-regulation of adiponectin or adiponectin receptor has a number of therapeutic benefits. Given that it is hard to convert the full size adiponectin protein into a viable drug, adiponectin receptor agonists could be designed or identified using high-throughput screening. Here, we report on the development of a two-step screening process to identify adiponectin agonists. First step, we developed a high throughput screening assay based on fluorescence polarization to identify adiponectin ligands. The fluorescence polarization assay reported here could be adapted to screening against larger small molecular compound libraries. A natural product library containing 10,000 compounds was screened and 9 hits were selected for validation. These compounds have been taken for the second-step in vitro tests to confirm their agonistic activity. The most active adiponectin receptor 1 agonists are matairesinol, arctiin, (-)-arctigenin and gramine. The most active adiponectin receptor 2 agonists are parthenolide, taxifoliol, deoxyschizandrin, and syringin. These compounds may be useful drug candidates for hypoadiponectin related diseases.
format	article
author	Yiyi Sun Zhihe Zang Ling Zhong Min Wu Qing Su Xiurong Gao Wang Zan Dong Lin Yan Zhao Zhonglin Zhang
author_facet	Yiyi Sun Zhihe Zang Ling Zhong Min Wu Qing Su Xiurong Gao Wang Zan Dong Lin Yan Zhao Zhonglin Zhang
author_sort	Yiyi Sun
title	Identification of adiponectin receptor agonist utilizing a fluorescence polarization based high throughput assay.
title_short	Identification of adiponectin receptor agonist utilizing a fluorescence polarization based high throughput assay.
title_full	Identification of adiponectin receptor agonist utilizing a fluorescence polarization based high throughput assay.
title_fullStr	Identification of adiponectin receptor agonist utilizing a fluorescence polarization based high throughput assay.
title_full_unstemmed	Identification of adiponectin receptor agonist utilizing a fluorescence polarization based high throughput assay.
title_sort	identification of adiponectin receptor agonist utilizing a fluorescence polarization based high throughput assay.
publisher	Public Library of Science (PLoS)
publishDate	2013
url	https://doaj.org/article/46d1e5eb95024aab8493a46e430b0493
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Identification of adiponectin receptor agonist utilizing a fluorescence polarization based high throughput assay.

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