Estrogen-related Receptor Related Drug Discovery Products
The Estrogen-related Receptor (ERR) family, a group of structurally related but functionally separate nuclear receptors, is made up of three members: ERR (ESRRRA), ERR (ESRRB), and ERR (ESRRC) (ESRRG). Despite their structural similarity to estrogen receptors (ERs), ERRs are categorized as orphan nuclear receptors since they do not bind endogenous ligands like estrogens. ERRs, on the other hand, are constitutively active and regulate target gene expression by binding to specific DNA sequences known as estrogen-related receptor response elements (ERREs). The ERR family has been linked to a variety of biological processes such as energy metabolism, cellular differentiation, and development.
Fig.1 Structure of ERRα.1
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Overview of Estrogen-related Receptor
These receptors play a vital role in regulating numerous biological processes, including energy metabolism, cellular differentiation, and development. ERR family members consist of ERRα (ESRRA), ERRβ (ESRRB), and ERRγ (ESRRG).
- ERRα (ESRRA):
The ERRα subtype is predominantly expressed in tissues with high energy demand, such as skeletal muscle, heart, and brown adipose tissue. ERRα is a significant regulator of mitochondrial biogenesis and function, thereby bolstering cellular energy capacity. In addition to its role in energy metabolism, ERRα has been implicated in later stages of development, particularly in skeletal muscle differentiation and adipogenesis.
- ERRβ (ESRRB):
ERRβ is essential for early embryonic development and is involved in the differentiation of pluripotent stem cells. It is expressed in various tissues, including the central nervous system, heart, and kidney. ERRβ has been linked to the regulation of genes implicated in oxidative phosphorylation, fatty acid oxidation, and electron transport chain function. Additionally, ERRβ has been shown to modulate the expression of genes involved in cellular differentiation and tissue development.
- ERRγ (ESRRG):
The ERRγ subtype is expressed in a tissue-specific manner, with high levels detected in the brain, heart, and kidney. ERRγ plays a crucial role in energy metabolism, particularly in modulating the expression of genes involved in glucose and lipid metabolism, and mitochondrial function. Furthermore, ERRγ is essential for early embryonic development and has been implicated in the regulation of genes associated with cellular differentiation and tissue development.
Pharmacological Targeting of Estrogen-related Receptors:
The development of synthetic compounds, such as inverse agonists and antagonists, capable of modulating ERR activity has emerged as a fecund area of investigation. The identification and optimization of these compounds hold promise for the amelioration of ERR-mediated pathologies, including cancer, metabolic diseases, and neurological conditions. Moreover, ongoing endeavors in medicinal chemistry aim to create novel ERR ligands with enhanced in vivo biodistribution, tissue selectivity, and structure-activity relationships, all of which are essential for druggability.
Reference
- From Wikipedia, by Boghog, Own work, CC BY-SA 4.0, without any modification, https://commons.wikimedia.org/wiki/File:1DFU_L27.png
