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Recent Advance in the Design of Small Molecular Modulators of Estrogen-Related Receptors

[ Vol. 18 , Issue. 23 ]

Author(s):

Xiaoyun Lu, Lijie Peng, Man Lv and Ke ding   Pages 3421 - 3431 ( 11 )

Abstract:


The estrogen-related receptors (ERRs), comprising ERRα, ERRβ and ERRγ, are the members of the nuclear receptor superfamily, which have been functionally implicated in estrogen signal pathway in various patterns. However, no natural ligand of ERRs has been identified to data, so identification of the synthetic modulators (inverse agonist and agonist) of ERRs would be highly effective in the treatment of estrogen-related pathologies, such as diabetes, breast cancer and osteoporosis. This review summarizes the structures and biological functions of ERR subtypes, and the progress in designing the small molecular modulators of ERRs as well as the detailed description of available co-crystal structures of the LBD of ERRs in three distinct states: unligand, inverse agonist bound, and agonist bound.

Keywords:

Estrogen-related receptors (ERRs), ERRα, ERRγ, Modulators, Inverse agonist, Agonist, Biological Function, LBD, unligand, agonist bound, unligand, agonist bound

Affiliation:

Key Laboratory of Regenerative Biology and Institute of Chemical Biology, Guangzhou Institutes of Biomedicine and Health, Chinese Academy of Sciences, No 190, Kaiyuan Avenue, Science Park, Guangzhou, China.



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