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Cited by 71Estrogen and related hormone effectsSynthesis and biological activityComputational Drug Discovery Methods

Estrogen receptor ligands: a review (2013-2015)

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Farzaneh, Shabnam, Zarghi, Afshin·2016·Scientia Pharmaceutica
DOI 10.3390/scipharm84030409PMC PMC5064234
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Abstract

Estrogen receptors (ERs) are a group of compounds named for their importance in both menstrual and estrous reproductive cycles. They are involved in the regulation of various processes ranging from tissue growth maintenance to reproduction. Their action is mediated through ER nuclear receptors. Two subtypes of the estrogen receptor, ERα and ERβ, exist and exhibit distinct cellular and tissue distribution patterns. In humans, both receptor subtypes are expressed in many cells and tissues, and they control key physiological functions in various organ systems. Estrogens attract great attention due to their wide applications in female reproductive functions and treatment of some estrogen-dependent cancers and osteoporosis. This paper provides a general review of ER ligands published in international journals patented between 2013 and 2015. The broad physiological profile of estrogens has attracted the attention of many researchers to develop new estrogen ligands as therapeutic molecules for various clinical purposes. After the discovery of the ERβ receptor, subtype-selective ligands could be used to elicit beneficial estrogen-like activities and reduce adverse side effects, based on the different distributions and relative levels of the two ER subtypes in different estrogen target tissues. Therefore, recent literature has focused on selective estrogen ligands as highly promising agents for the treatment of some types of cancer, as well as for cardiovascular, inflammatory, and neurodegenerative diseases. Estrogen receptors are nuclear transcription factors that are involved in the regulation of many complex physiological functions in humans. Selective estrogen ligands are highly promising targets for treatment of some types of cancer, as well as for cardiovascular, inflammatory and neurodegenerative diseases. Extensive structure-activity relationship studies of ER ligands based on small molecules indicate that many different structural scaffolds may provide high-affinity compounds, provided that some basic structural requirements are present.

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  • Estrogen receptors are found on most cell types and exposure of male cells to estrogenic media (e.g., phenol red) can lead to estrogen-receptor-dependent influences on cell proliferation, differentiation, and metabolism.

    “Estrogen receptors are found on most cell types and exposure of male cells to estrogenic media (e.g. phenol red structurally resembles some nonsteroidal estrogens) can lead to estrogen-receptor-dependent influences on cell proliferation, differentiation, and metabolism (Berthois et al., 1986; Farzaneh and Zarghi, 2016).”

    From In Vitro research Reproducibility: Keeping up High Standards (2019) · cites this paper as Farzaneh and Zarghi, 2016

    The Introduction (§1.1; page unavailable) says estrogen receptors are expressed in many human cells and tissues, including male reproductive organs. The cancer discussion (§1.2.1; page unavailable) describes estrogen-receptor-related effects on proliferation. Our copy does not support the more specific claim about exposing male cells to phenol-red-containing media or effects on their differentiation and metabolism. (LLM, conf=0.85)

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Authors
Farzaneh, S., & Zarghi, A.
Affiliations
Shahid Beheshti University (IR)
Corresponding author
Zarghi, Afshin
ORCID
Venue
Scientia Pharmaceutica
Publisher
MDPI AG
Published
2016-04-13
Volume
84
Issue
3
Pages
409-427
ISSN
  • 0036-8709 (ISSN-L)
  • 2218-0532
DOI
10.3390/scipharm84030409
PMC
PMC5064234
OpenAlex
W2524575831
Cited by
71
References
0
Citations by year
2025: 3 · 2024: 8 · 2023: 6 · 2022: 8 · 2021: 11 · 2020: 9 · 2019: 11 · 2018: 7 · 2017: 3
FWCI
0.92
Type
journal article
Language
en
Open access
Licence
Locations
  • Scientia Pharmaceutica (publishedVersion, cc-by)
  • PubMed Central (publishedVersion, cc-by)
  • PubMed (publishedVersion)
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Genetics › Estrogen and related hormone effects
  • Physical Sciences › Chemistry › Organic Chemistry › Synthesis and biological activity
  • Physical Sciences › Computer Science › Computational Theory and Mathematics › Computational Drug Discovery Methods
Keywords
estrogen receptor ligands, estrogen receptor alpha, estrogen receptor beta, selective estrogen receptor modulators, structure-activity relationship, estrogen-dependent cancer, estrogen therapy, patents, cardiovascular disease, neurodegenerative diseases, inflammatory diseases, estrogen target tissues

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