ArticleMolecular and cellular biology2004
Selective estrogen receptor modulators 4-hydroxytamoxifen and raloxifene impact the stability and function of SRC-1 and SRC-3 coactivator proteins.
Article in Molecular and cellular biology, 2004. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 35 papers.
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Who cites it
35 citing papers in PubMed, 85 citations in OpenAlex.
- Steroid receptor coactivator-3 regulates glucose metabolism in bladder cancer cells through coactivation of hypoxia inducible factor 1α.The Journal of biological chemistry · 2014Trial
- Steroid receptor coactivators: from basic research to translational opportunities.Endocrine reviews · 2026Review
- Steroid receptor coactivators in immunity - From function to emerging translational opportunities.The Journal of biological chemistry · 2026Review
- Critical Roles of SRC-3 in the Development and Progression of Breast Cancer, Rendering It a Prospective Clinical Target.Cancers · 2023Review
- Heat shock factor 1 (HSF1) specifically potentiates c-MYC-mediated transcription independently of the canonical heat shock response.Cell reports · 2023Article
- Mining toxicogenomic data for dose-responsive pathways: implications in advancing next-generation risk assessment.Frontiers in toxicology · 2023Article
- Oleuropein suppresses endometriosis progression and improves the fertility of mice with endometriosis.Journal of biomedical science · 2022Article
- Relationship between endocrine disruptors and obesity with a focus on bisphenol A: a narrative review.BioImpacts : BI · 2021Review
- Article
- The molecular, cellular and clinical consequences of targeting the estrogen receptor following estrogen deprivation therapy.Molecular and cellular endocrinology · 2015Review
- Nuclear receptor modulation--role of coregulators in selective estrogen receptor modulator (SERM) actions.Steroids · 2014Article
- Bufalin is a potent small-molecule inhibitor of the steroid receptor coactivators SRC-3 and SRC-1.Cancer research · 2014Article
- Importance of sex to pain and its amelioration; relevance of spinal estrogens and its membrane receptors.Frontiers in neuroendocrinology · 2012Review
- Steroid receptor coactivators, HER-2 and HER-3 expression is stimulated by tamoxifen treatment in DMBA-induced breast cancer.BMC cancer · 2012Article
- Steroid receptor coactivators 1, 2, and 3: critical regulators of nuclear receptor activity and steroid receptor modulator (SRM)-based cancer therapy.Molecular and cellular endocrinology · 2012Review
- The function of steroid receptor coactivator-1 in normal tissues and cancer.International journal of biological sciences · 2012Review
- Small molecule inhibition of the steroid receptor coactivators, SRC-3 and SRC-1.Molecular endocrinology (Baltimore, Md.) · 2011Article
- ERasing breast cancer resistance through the kinome.Nature medicine · 2011Article
- Progesterone and estradiol effects on SRC-1 and SRC-3 expression in human astrocytoma cell lines.Endocrine · 2010Article
- Resistance to antiestrogen arzoxifene is mediated by overexpression of cyclin D1.Molecular endocrinology (Baltimore, Md.) · 2009Article
Corrections and comments
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Proteasome-mediated protein degradation has been implicated in playing a role in nuclear receptor-mediated gene expression; inhibition of the proteasome impairs the transcriptional activity of estrogen receptor alpha (ERalpha) and most other nuclear receptors. This coincides with blockage of agonist-dependent degradation of the receptor and elevation of the steady-state levels of SRC family coactivators and CBP. Here, we examined the effects that different ERalpha ligands have on coactivator protein steady-state levels and demonstrate that the selective ER modulators (SERMs) 4-hydroxytamoxifen (4HT) and raloxifene are able to elevate SRC-1 and SRC-3 protein levels. Using the HeLa cell line, we show that this effect is ERalpha dependent. Consistent with the observed increase in coactivator protein levels, we were also able to observe an increase in the transcriptional activity of other nuclear receptors in SERM-treated cells. Information presented here demonstrates an unexpected consequence of SERM treatment, which could help further define the complex tissue responses to 4HT and raloxifene, and suggests that these ligands can have a broad biological action, stimulating the transcriptional activity of other nuclear receptors.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.