Detection of endogenous selective estrogen receptor modulators such as 27-hydroxycholesterol

Research output: Chapter in Book/Report/Conference proceedingChapter

Abstract

The estrogen receptors (ERs) belong to the nuclear receptor superfamily, and as such act as ligand inducible transcription factors, mediating the effects of estrogens. However, their pharmacology is complex, having the ability to be differentially activated by ligands. Such ligands possess the ability to behave as either ER-agonists or ER-antagonists, depending on the cellular and tissue context, and have been termed Selective Estrogen Receptor Modulators (SERMs). Several SERMs have been identified with clinical relevance such as tamoxifen and raloxifene. Recently, 27-hydroxycholesterol has been characterized as the first identified endogenous SERM leading to the notion that other endogenous SERMs may exist, each having potential pathophysiological functions. This, coupled with the historic pharmaceutical interest as well as growing concern over chemicals in the environment with the ability to behave like SERMs, has increased the demand for assays to detect SERM-like activity. Here, we describe a common, straightforward in vitro assay investigating the induction of classic ER-target genes in MCF7 breast cancer cells, allowing one to identify ligands with SERM-like activity.

Original languageEnglish (US)
Title of host publicationMethods in Molecular Biology
PublisherHumana Press Inc.
Pages431-443
Number of pages13
DOIs
StatePublished - Jan 1 2016

Publication series

NameMethods in Molecular Biology
Volume1366
ISSN (Print)1064-3745

Fingerprint

Selective Estrogen Receptor Modulators
Ligands
Estrogen Receptors
Estrogens
Tamoxifen
Cytoplasmic and Nuclear Receptors
27-hydroxycholesterol
Transcription Factors
Pharmacology
Breast Neoplasms
Pharmaceutical Preparations

Keywords

  • 27-Hydroxycholesterol
  • Estradiol
  • Estrogen receptor
  • Gene expression
  • MCF7 cell s
  • Pharmacology
  • Quantitative PCR
  • Selective estrogen receptor modulator (SERM)
  • Tamoxifen

ASJC Scopus subject areas

  • Molecular Biology
  • Genetics

Cite this

Nelson, E. R. (2016). Detection of endogenous selective estrogen receptor modulators such as 27-hydroxycholesterol. In Methods in Molecular Biology (pp. 431-443). (Methods in Molecular Biology; Vol. 1366). Humana Press Inc.. https://doi.org/10.1007/978-1-4939-3127-9_34

Detection of endogenous selective estrogen receptor modulators such as 27-hydroxycholesterol. / Nelson, Erik R.

Methods in Molecular Biology. Humana Press Inc., 2016. p. 431-443 (Methods in Molecular Biology; Vol. 1366).

Research output: Chapter in Book/Report/Conference proceedingChapter

Nelson, ER 2016, Detection of endogenous selective estrogen receptor modulators such as 27-hydroxycholesterol. in Methods in Molecular Biology. Methods in Molecular Biology, vol. 1366, Humana Press Inc., pp. 431-443. https://doi.org/10.1007/978-1-4939-3127-9_34
Nelson ER. Detection of endogenous selective estrogen receptor modulators such as 27-hydroxycholesterol. In Methods in Molecular Biology. Humana Press Inc. 2016. p. 431-443. (Methods in Molecular Biology). https://doi.org/10.1007/978-1-4939-3127-9_34
Nelson, Erik R. / Detection of endogenous selective estrogen receptor modulators such as 27-hydroxycholesterol. Methods in Molecular Biology. Humana Press Inc., 2016. pp. 431-443 (Methods in Molecular Biology).
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