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 language | English (US) |
|---|---|
| Title of host publication | Methods in Molecular Biology |
| Publisher | Humana Press Inc. |
| Pages | 431-443 |
| Number of pages | 13 |
| DOIs | |
| State | Published - Jan 1 2016 |
Publication series
| Name | Methods in Molecular Biology |
|---|---|
| Volume | 1366 |
| ISSN (Print) | 1064-3745 |
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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
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 proceeding › Chapter
}
TY - CHAP
T1 - Detection of endogenous selective estrogen receptor modulators such as 27-hydroxycholesterol
AU - Nelson, Erik R.
PY - 2016/1/1
Y1 - 2016/1/1
N2 - 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.
AB - 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.
KW - 27-Hydroxycholesterol
KW - Estradiol
KW - Estrogen receptor
KW - Gene expression
KW - MCF7 cell s
KW - Pharmacology
KW - Quantitative PCR
KW - Selective estrogen receptor modulator (SERM)
KW - Tamoxifen
UR - http://www.scopus.com/inward/record.url?scp=84947714479&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84947714479&partnerID=8YFLogxK
U2 - 10.1007/978-1-4939-3127-9_34
DO - 10.1007/978-1-4939-3127-9_34
M3 - Chapter
C2 - 26585155
AN - SCOPUS:84947714479
T3 - Methods in Molecular Biology
SP - 431
EP - 443
BT - Methods in Molecular Biology
PB - Humana Press Inc.
ER -