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

Author(s): Xiaoyun Lu, Lijie Peng, Man Lv, Ke ding

Journal Name: Current Pharmaceutical Design

Volume 18 , Issue 23 , 2012

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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

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Article Details

Year: 2012
Page: [3421 - 3431]
Pages: 11
DOI: 10.2174/138161212801227113
Price: $65

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