A new series of ERbeta (ERbeta) selective ligands has been prepared. One of the compounds 6, structurally related to the phytoestrogen apigenin 4, displays a binding preference for ERbeta over ERalpha of over 40-fold. In addition to its binding selectivity, 6 was able to potently induce metallothionein (an ERbeta specific response in human SAOS-2 cells) while demonstrating low potency in an ERalpha dependant ERE-tk luciferase assay in MCF-7 cells. Such receptor and cell selectivity could make 6 a useful molecular probe for better understanding the role of ERbeta in mammalian physiology.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.1016/s0960-894x(03)00394-9 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Exposure to zearalenone exacerbates the decrease in calcium transport via selective regulation to estrogen receptor α/β in estrogenic deficient model.
Sci China Life Sci
January 2025
State Key Laboratory of Animal Nutrition and Feeding, College of Animal Science and Technology, China Agricultural University, Beijing, 100193, China.
Leveraging nuclear receptor mediated transcriptional signaling for drug discovery: Historical insights and current advances.
Adv Protein Chem Struct Biol
January 2025
Department of Life Sciences, Kristu Jayanti College, Autonomous, Bengaluru, Karnataka, India. Electronic address:
Nuclear receptors (NRs) are ligand-activated transcription factors that regulate gene expression in response to physiological signals, such as hormones and other chemical messengers. These receptors either activate or repress the transcription of target genes, which in turn promotes or suppresses physiological processes governing growth, differentiation, and homeostasis. NRs bind to specific DNA sequences and, in response to ligand binding, either promote or hinder the assembly of the transcriptional machinery, thereby influencing gene expression at the transcriptional level.
View Article and Find Full Text PDFDietary phytoestrogens recalibrate socioemotional behavior in C57Bl/6J mice in a sex- and timing-dependent manner.
Horm Behav
January 2025
Department of Molecular Biomedical Sciences, College of Veterinary Medicine, North Carolina State University, Raleigh, NC, USA; Department of Psychiatry & Behavioral Neurobiology, Heersink School of Medicine, University of Alabama at Birmingham, Birmingham, AL, USA. Electronic address:
Estrogens are potent regulators of socioemotional behavior across species. Ubiquitous in human and animal diets, plant-derived phytoestrogens (PE) bind estrogen receptors. While prior work has examined the impact of PE exposure on socioemotional behavior, findings are inconsistent across studies.
View Article and Find Full Text PDFEndocrine-targeting therapies shift the breast microbiome to reduce estrogen receptor-α breast cancer risk.
Cell Rep Med
January 2025
Department of Surgery, Wake Forest University School of Medicine, Winston-Salem, NC 27157, USA; Department of Cancer Biology, Wake Forest University School of Medicine, Winston-Salem, NC 27157, USA; Atrium Health Wake Forest Baptist Comprehensive Cancer Center, Wake Forest University School of Medicine, Winston-Salem, NC 27157, USA. Electronic address:
Article Synopsis
- Research shows that breast tissue has a unique, changeable microbiome that can be influenced by endocrine-targeting therapies such as tamoxifen.
- Tamoxifen treatment was found to change the diversity of the breast microbiome and increase levels of certain beneficial bacteria, like Lactobacillus, in both mice and primates.
- Probiotic bacteria injections in lab mice not only reduced tumor formation but also affected gene expression related to metabolism, suggesting a link between breast microbiome changes and lower risk of estrogen receptor-positive breast cancer.
Exploring the Complex Mechanisms of Isoflavones: From Cell Bioavailability, to Cell Dynamics and Breast Cancer.
Phytother Res
December 2024
Université de Rennes, Inserm, EHESP, Irset (Institut de Recherche en Santé, Environnement et Travail) - UMR_S 1085, Rennes, France.
In Western countries, the increase in the consumption of soy-derived products raises the population's exposure to isoflavones. These molecules, present in many foods, have numerous effects on the body's cells, including regulation of the transcription and epigenetics, cell signaling, cell cycle, cell growth, apoptosis, and oxidative stress. However, despite the multitude of studies conducted, on these compounds, it remains difficult to draw definitive conclusions regarding their safety or dangerousness in the diet.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!