Research Progress in Estrogen-related Receptor Gamma (ERRγ) Agonists and Inverse Agonists


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Abstract

Estrogen-related receptor gamma (ERRγ), one of three members of the ERR family, is an inducible transcription factor. ERRγ has dual functions in different tissues. The decreased expression of ERRγ in the brain, stomach, prostate, and fat cells can cause neuropsychological dysfunction, gastric cancer, prostate cancer, and obesity. However, when ERRγ is present in the liver, pancreas, and thyroid follicular cells, ERRγ overexpression is related to liver cancer, type II diabetes, oxidative liver injury, and anaplastic thyroid carcinoma. Signaling pathway studies have confirmed that ERRγ agonists or inverse agonists can regulate ERRγ expression to treat related diseases. The collision between residue Phe435 and the modulator is a key factor determining the activation or inhibition of ERRγ. Although more than 20 agonists and inverse agonists of ERRγ have been reported, no clinical studies have been found in the literature. This review summarizes the important relationship between ERRγ-related signaling pathways and diseases, research progress, and the structure-activity relationship of modulators. These findings provide guidance for further study on new ERRγ modulators.

About the authors

Yong Zheng

School of Chemistry & Chemical Engineering, Qilu University of Technology, Shandong Academy of Sciences

Email: info@benthamscience.net

Yongli Du

School of Chemistry & Chemical Engineering, Qilu University of Technology, Shandong Academy of Sciences,

Author for correspondence.
Email: info@benthamscience.net

Haibin Zhang

School of Chemistry & Chemical Engineering, Qilu University of Technology, Shandong Academy of Sciences

Email: info@benthamscience.net

Huiting Lv

School of Chemistry & Chemical Engineering, Qilu University of Technology, Shandong Academy of Sciences

Email: info@benthamscience.net

Zhijia Yan

School of Chemistry & Chemical Engineering, Qilu University of Technology, Shandong Academy of Sciences

Email: info@benthamscience.net

Ning Dong

School of Chemistry & Chemical Engineering, Qilu University of Technology, Shandong Academy of Sciences

Email: info@benthamscience.net

Qunyi Li

Department of Pharmacy, Huashan Hospital, Fudan University

Email: info@benthamscience.net

Tianxiao Wang

Department of Pharmacy, Huashan Hospital, Fudan University

Email: info@benthamscience.net

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