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Related Concept Videos

Drug-Receptor Interaction: Agonist01:25

Drug-Receptor Interaction: Agonist

Agonists are drugs that interact with specific receptors in the body to produce a biological response. When an agonist binds to a receptor, it activates or enhances the receptor's function, leading to physiological effects. The interaction between agonist drugs and receptors is crucial for their therapeutic action in various medical treatments.
Agonists can bind to receptors in different ways. Some agonists bind directly to the receptor's active site, mimicking the endogenous ligand's action.
Gonadal and Placental Hormones01:24

Gonadal and Placental Hormones

The gonads, namely the testes in males and the ovaries in females, are pivotal in producing gonadal hormones that orchestrate the intricate processes of sexual development and reproduction.
In males, testosterone is the primary gonadal androgen. It plays a central role in the maturation of male reproductive organs — the penis and testes. Additionally, testosterone is instrumental in the development of secondary sexual characteristics — a deep voice as well as facial and pubic hair growth — and...
Spare Receptors01:30

Spare Receptors

Some receptors remain unoccupied even when an agonist produces a maximal response. Such empty ones are called spare receptors. In presence of spare receptors the maximum effect of an agonist drug is achieved with fewer than 100% of the receptors being occupied. To determine the presence of spare receptors, scientists often compare the concentration of the drug needed to produce 50% of the maximum effect (EC50) with the concentration of the drug needed to occupy 50% of the receptors (Kd). If the...
Target Cell Response to Hormones01:22

Target Cell Response to Hormones

Hormones intricately bind to receptors on the surface or within target cells, initiating a cascade of cellular responses.
Notably, the cellular response can be regulated by altering the number of receptors expressed in the cell. For example, prolonged exposure to elevated hormone levels results in a gradual decline or down-regulation in the number of receptors for that specific hormone on the cell surface. Conversely, in response to low hormone levels, cells may use up-regulation, producing an...
The Two-State Receptor Model01:29

The Two-State Receptor Model

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.
The binding affinity of a drug determines its interaction with one...
Transducer Mechanism: Nuclear Receptors01:31

Transducer Mechanism: Nuclear Receptors

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.
About 48 different soluble family members of nuclear receptors are identified that can be divided into two main classes:

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Related Experiment Video

Updated: May 31, 2026

In Vitro Imaging and Quantification of the Drug Targeting Efficiency of Fluorescently Labeled GnRH Analogues
10:36

In Vitro Imaging and Quantification of the Drug Targeting Efficiency of Fluorescently Labeled GnRH Analogues

Published on: March 21, 2017

Are circulating gonadotropin isoforms naturally occurring biased agonists? Basic and therapeutic implications.

Brian J Arey1, Francisco J López

  • 1Metabolic and Cardiovascular Drug Discovery, Research and Development, Bristol-Myers Squibb Co., 311 Pennington-Rocky Hill Rd., Mail Stop- 21-1.08, Hopewell, NJ 08543, USA. brian.arey@bms.com

Reviews in Endocrine & Metabolic Disorders
|June 28, 2011
PubMed
Summary

Researchers discovered small molecules that mimic the complex signaling of reproductive hormones like luteinizing hormone (LH) and follicle-stimulating hormone (FSH). This breakthrough paves the way for new, orally available fertility disorder treatments.

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Last Updated: May 31, 2026

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Published on: March 21, 2017

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Reproductive Techniques for Ovarian Monitoring and Control in Amphibians
04:37

Reproductive Techniques for Ovarian Monitoring and Control in Amphibians

Published on: May 12, 2019

Area of Science:

  • Reproductive endocrinology
  • Molecular pharmacology
  • Glycoprotein signaling

Background:

  • Gonadotropins (LH, hCG, FSH) are crucial for reproduction and have been used therapeutically for infertility.
  • Developing selective small molecules to modulate gonadotropin receptors has been challenging.
  • Gonadotropins are glycoproteins with varying glycosylation, impacting their biological activity and signaling.

Purpose of the Study:

  • To investigate the biased agonism of glycosylated gonadotropin variants.
  • To identify novel small molecules that mimic the distinct signaling properties of gonadotropin isoforms.
  • To explore new therapeutic strategies for reproductive disorders.

Main Methods:

  • Analysis of glycosylated variants of LH, hCG, and FSH.
  • Characterization of G protein-coupled receptor signaling pathways.
  • Identification and synthesis of small molecule allosteric modulators.

Main Results:

  • Glycosylated gonadotropin isoforms exhibit biased agonism, transducing distinct signals at the receptor level.
  • Newly developed synthetic allosteric compounds effectively mimic this biased signaling.
  • These small molecules offer potential for orally available, drug-like therapies.

Conclusions:

  • Biased agonism is a key mechanism in gonadotropin signaling.
  • Small molecule modulators can replicate the pleiotropic signaling of endogenous gonadotropins.
  • This research opens avenues for novel treatments for reproductive disorders.