TCPOBOP, Androstane receptor (mCAR) agonist

Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

The estrogen receptor also known as ESR is a nuclear hormone receptor that functions as a transcription factor. It plays an important role in the regulation of gene expression. There are two main isoforms of the estrogen receptor: ER-alpha and ER-beta which have different tissue distributions and functions. The molecular mass of ER-alpha is approximately 66 kDa while ER-beta is about 59 kDa. Estrogen receptors are widely expressed in tissues such as the breast uterus bone liver and the central nervous system.

Biological function summary

Estrogen receptors mediate the effects of estrogens which include regulating reproductive and non-reproductive systems. They form a complex with DNA by binding to specific estrogen-responsive elements which elicits transcriptional activation or repression of target genes. These receptors interact with coactivators and corepressors to influence gene transcription often assembling into a larger receptor complex to facilitate diverse cellular functions.

Pathways

Estrogen receptors are integral in the estrogen signaling pathway and interact with various cellular processes such as cell growth differentiation and homeostasis. In the PI3K/AKT signaling pathway they can cross-talk with growth factor receptors offering an intersection with proteins such as HER2. This crosstalk impacts cellular behaviors associated with reproduction and cancer progression showcasing how vascular and hormonal signaling pathways interlink.

Estrogen receptors have significant relevance to breast cancer and osteoporosis. In breast cancer the expression of estrogen receptors drives proliferation of cancer cells and they are often evaluated to guide endocrine therapy decisions. The receptor’s interaction with proteins like CRHR2 and CRHBP in these contexts may influence stress and cortisol-related pathways in tumorigenesis and bone density regulation. Treatment strategies targeting estrogen receptors can help manage these diseases by interrupting their proliferative signaling.