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Transducer Mechanism: Nuclear Receptors01:31

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Nuclear receptors, or NRs, are unique transcription factors that regulate gene transcription and affect the cellular pathways involved in reproduction, development, or metabolism. Their ability to be stimulated by small lipophilic ligands and control vital cellular processes makes them ideal drug targets. Nearly 10-15% of currently prescribed drugs target these receptors.
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Transducer Mechanism: Enzyme-Linked Receptors01:27

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Enzyme-linked receptors are cell-surface receptors acting as an enzyme or associating with an enzyme intracellularly. They make excellent drug targets. Drugs can bind to the extracellular ligand-binding domain or directly affect their enzymatic domain and alter their activity.
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The Two-State Receptor Model01:29

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The two-state receptor model explains a drug's interaction with receptors, such as G protein-coupled receptors and ligand-gated ion channels, to induce or inhibit a biological response. When no natural ligands are present, a receptor exists in an equilibrium of inactive (Ri) and active (Ra) conformations. The inactive form does not produce a response, while the active form generates a basal effect known as constitutive activity.
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Dose-Response Relationship: Selectivity and Specificity01:25

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Drugs exert their therapeutic effects by interacting with receptors, enzymes, or ion channels that are present throughout the human body. The strength and duration of the interaction between a drug and its target receptor are characterized by the selectivity and specificity of the drug. Selectivity refers to a drug's strong preference for its intended target over other targets. For instance, isoprenaline, a non-selective β-adrenergic agonist, interacts with both β1- and...
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Mitogens and their receptors play a crucial role in controlling the progression of the cell cycle. However, the loss of mitogenic control over cell division leads to tumor formation. Therefore, mitogens and mitogen receptors play an important role in cancer research. For instance, the epidermal growth factor (EGF) - a type of mitogen and its transmembrane receptor (EGFR), decides the fate of the cell's proliferation. When EGF binds to EGFR, a member of the ErbB family of tyrosine kinase...
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Internal Receptors01:31

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Many cellular signals are hydrophilic and therefore cannot pass through the plasma membrane. However, small or hydrophobic signaling molecules can cross the hydrophobic core of the plasma membrane and bind to internal, or intracellular, receptors that reside within the cell. Many mammalian steroid hormones use this mechanism of cell signaling, as does nitric oxide (NO) gas.
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Updated: Dec 17, 2025

Profiling of Estrogen-regulated MicroRNAs in Breast Cancer Cells
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Selective estrogen receptor modulators (SERMS): keys to understanding their function.

James H Liu1

  • 1Departments of Obstetrics and Gynecology and Reproductive Biology, University Hospitals MacDonald Women's Hospital, Case Western Reserve University School of Medicine, Cleveland, OH.

Menopause (New York, N.Y.)
|June 25, 2020
PubMed
Summary
This summary is machine-generated.

Selective estrogen receptor modulators (SERMs) offer vital therapeutic options for various conditions. This review clarifies SERM mechanisms and clinical uses in breast cancer, osteoporosis, and menopause symptom management.

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Area of Science:

  • Pharmacology and Therapeutics
  • Endocrinology
  • Oncology

Background:

  • Selective estrogen receptor modulators (SERMs) are crucial in modern medicine.
  • Understanding SERM mechanisms is limited among clinicians.
  • SERMs target estrogen-responsive tissues like breast, bone, and brain.

Purpose of the Study:

  • To elucidate the pharmacodynamics of SERMs.
  • To review clinical applications of FDA-approved SERMs.
  • To discuss SERMs in development and natural phytoestrogens.

Main Methods:

  • Literature review of SERM pharmacodynamics.
  • Analysis of clinical trial data for approved SERMs.
  • Synthesis of information on emerging SERMs and phytoestrogens.

Main Results:

  • SERMs exhibit tissue-specific agonist and antagonist activities.
  • FDA-approved SERMs are effective for vasomotor symptoms, osteoporosis, genitourinary syndrome of menopause, infertility, and breast cancer.
  • Ongoing research explores novel SERMs and natural alternatives.

Conclusions:

  • SERMs represent a significant therapeutic class with diverse applications.
  • Further research is needed to fully understand SERM action and optimize their use.
  • SERMs and phytoestrogens hold promise for managing hormone-related conditions.