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.
Highlights
Estrogens are a group of compounds named for their importance in both menstrual and estrous reproductive cycles
Selective estrogen receptor modulators (SERMs), structurally, are various compounds that interact with intracellular estrogen receptors in different target organs as Estrogen receptors (ERs) agonists or antagonists [1]
Ideal selective estrogen receptor modulators (SERMs) would possess antagonist activity in the mammary gland and uterus, and agonist activity in other target tissues that benefit from estrogen-like actions such as the cardiovascular, skeletal, and central nervous systems [2]
Summary
Estrogens are a group of compounds named for their importance in both menstrual and estrous reproductive cycles 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 such as reproductive, skeletal, cardiovascular, and central nervous systems. ERβ is predominant in the prostate (epithelium), bladder, ovary (granulosa cells), colon, adipose tissue, and immune system Both subtypes are markedly expressed in the cardiovascular and central nervous systems. Ideal SERMs would possess antagonist activity in the mammary gland and uterus, and agonist activity in other target tissues that benefit from estrogen-like actions such as the cardiovascular, skeletal, and central nervous systems [2]. 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 the different estrogen target tissues mentioned above [3]
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