Estrogen Receptor Assays
Background of Estrogen Receptor
Estrogen receptors (ERs) are a group of proteins belonging to the superfamily class of nuclear receptors. Activated by the hormone estrogen, ERs can translocate into the nucleus and bind to DNA to regulate the activity of different genes. Due to their involvement in the regulation of many complex physiological processes in humans, ERs have been used for the prevention and treatment of a variety of pathological conditions, such as cancer, metabolic and cardiovascular diseases, neurodegeneration, inflammation, and osteoporosis.
Fig.1. Mechanisms for regulating ERα and ERβ expression. (Hua, 2018)
Distribution and Function of Estrogen Receptors
Estrogen receptors alpha (ERα) and beta (ERβ) are nuclear transcription factors that are widely expressed in multiple cells and tissues. These proteins control key physiological functions of various organ systems such as reproductive, skeletal, cardiovascular, and central nervous systems by regulating the transcription of specific target genes.
Subtypes and Mechanisms of Estrogen Receptor
Two classes of ERs exist, including estrogen receptors alpha (ERα) and estrogen receptors beta (ERβ). The main functions of the ERα are homeostasis and metabolic regulation of the mammary gland, uterus, and bone, while the ERβ focuses on the central nervous and immune systems.
| Receptor | Gene | Mechanism | Agonists | Antagonists |
| Estrogen receptor 1 | ESR1 |
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| Estrogen receptor 2 | ESR2 |
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Published Data
| Paper Title | Estrogen receptor signaling mechanisms |
| Journal | Advances in protein chemistry and structural biology |
| Published | 2019 |
| Abstract | Estrogen is responsible for controlling the function of the female reproductive system and the development of secondary sex characteristics. Estrogen controls gene expression by binding to the estrogen receptor (ER) to activate transcriptional processes and/or signaling events. These processes can function through direct nuclear interactions, indirect non-nuclear interactions, or a combination of both. Furthermore, the effects of estrogen on gene expression are all controlled by complex mechanisms that are highly regulated. In this article, we describe our knowledge of estrogen-mediated regulation of gene expression and biosynthesis of estrogen, and describe the main mechanisms by which estrogen controls gene transcription in different tissues and cell types. We also describe the crosstalk mechanism between nuclear and membrane estrogen receptor-activated signaling cascades. Finally, we discuss natural compounds capable of targeting specific estrogen receptors and their implications for human health and medical treatment. |
| Result |
Estrogen receptors have been shown to be involved in a variety of biological and physiological processes. These processes involve complex mechanisms and involve the direct binding of specific DNA sequences by the genomic nucleus, or the activation of intracellular cascades leading to non-genomic control of transcription. Since the first discovery of a membrane receptor, multiple mechanisms of action have been discovered and characterized. These processes involve a large number of intracellular kinases, transcription and growth factors, membrane receptors, as well as coregulators. The obtained findings contribute to the development of therapeutic strategies for diseases involving estrogen receptors and a range of endocrine diseases. A better understanding of the receptor's role in disease is needed in future studies. We will also focus on strategies for the prevention and treatment of diseases affected by estrogen and other steroid hormones.
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Fig.2. Association of theca and granulosa cells in estrogen synthesis. (Fuentes & Silveyra, 2019)
References
- Hua, H.; et al. Mechanisms for estrogen receptor expression in human cancer. Experimental hematology & oncology. 2018, 7(1): 1-11.
- Fuentes, N.; Silveyra, P. Estrogen receptor signaling mechanisms. Advances in protein chemistry and structural biology. 2019, 116: 135-170.
