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
Current Pharmaceutical Design
Title:Recent Advance in the Design of Small Molecular Modulators of Estrogen-Related Receptors
Volume: 18 Issue: 23
Author(s): Xiaoyun Lu, Lijie Peng, Man Lv and Ke ding
Affiliation:
Keywords: Estrogen-related receptors (ERRs), ERRα, ERRγ, Modulators, Inverse agonist, Agonist, Biological Function, LBD, unligand, agonist bound, unligand, agonist bound
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.
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Cite this article as:
Lu Xiaoyun, Peng Lijie, Lv Man and ding Ke, Recent Advance in the Design of Small Molecular Modulators of Estrogen-Related Receptors, Current Pharmaceutical Design 2012; 18 (23) . https://dx.doi.org/10.2174/138161212801227113
DOI https://dx.doi.org/10.2174/138161212801227113 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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