Dataset Information

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

ABSTRACT: 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.

SUBMITTER: Sun Y

PROVIDER: S-EPMC3653934 | biostudies-literature | 2013

REPOSITORIES: biostudies-literature

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

Sun Yiyi Y Zang Zhihe Z Zhong Ling L Wu Min M Su Qing Q Gao Xiurong X Zan Wang W Lin Dong D Zhao Yan Y Zhang Zhonglin Z

PloS one 20130514 5

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 develop ...[more]

PMID: 23691032

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Dataset Information

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

Publications

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

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