Related Experiment Video

Updated: Apr 16, 2026

In Vivo Inhibition of MicroRNA to Decrease Tumor Growth in Mice
07:02

In Vivo Inhibition of MicroRNA to Decrease Tumor Growth in Mice

Published on: August 23, 2019

7.9K

Targeting the thyroid-stimulating hormone receptor with small molecule ligands and antibodies

Terry F Davies1, Rauf Latif

  • 1Icahn School of Medicine at Mount Sinai and the James J. Peters VA Medical Center, Thyroid Research Unit , 1 Gustave L Levy Place, New York, NY 10029 , USA +1 212 241 7975 ; +1 212 428 6748 ; terry.davies@mssm.edu.

Expert Opinion on Therapeutic Targets
|March 14, 2015
PubMed
Abstract

Insights

Targeting the thyroid-stimulating hormone receptor (TSHR) offers new therapeutic strategies. Allosteric ligands and TSHR antibodies can selectively modulate TSHR pathways for disease control.

Area of Science:

  • Endocrinology
  • Molecular Biology
  • Immunology

Background:

  • The thyroid-stimulating hormone receptor (TSHR) is crucial for thyroid function and hormone synthesis.
  • TSHR is implicated as a key autoantigen in Graves' disease and in thyroid cancer development.

Purpose of the Study:

  • To review the structure and function of TSHR.
  • To explore the therapeutic potential of small molecule ligands and TSHR antibodies.

Main Methods:

  • Literature review of TSHR structure and function.
  • Analysis of therapeutic strategies involving small molecules and antibodies targeting TSHR.

Main Results:

  • TSHR conformation can be stabilized by allosteric ligands.
  • Selective modulation of TSHR signaling pathways is achievable.

Conclusions:

  • Allosteric ligands and TSHR antibodies represent potential next-generation therapeutics.
  • These agents can control pathophysiological consequences mediated by TSHR in thyroid and extrathyroidal tissues.
Keywords:
Graves’ diseaseautoantibodiesglycoprotein-hormone receptorsmall molecule ligandsthyroid cancerthyroid-stimulating hormone receptor

More Related Videos

Pretargeted Radioimmunotherapy Based on the Inverse Electron Demand Diels-Alder Reaction09:44

Pretargeted Radioimmunotherapy Based on the Inverse Electron Demand Diels-Alder Reaction

Published on: January 29, 2019

10.7K
An Orthotopic Mouse Model of Anaplastic Thyroid Carcinoma07:01

An Orthotopic Mouse Model of Anaplastic Thyroid Carcinoma

Published on: April 17, 2013

21.8K

Related Concept Videos

Synthesis and Regulation of Thyroid Hormones01:20

Synthesis and Regulation of Thyroid Hormones

Low blood levels of the thyroid hormones — triiodothyronine (T3) and thyroxine (T4) — signal the hypothalamus to release the thyrotropin-releasing hormone (TRH). TRH then reaches the pituitary gland and stimulates the release of thyroid-stimulating hormone(TSH) into the bloodstream.
Upon reaching the thyroid gland, TSH stimulates the follicular cells' active uptake of iodide ions from the blood. The ions diffuse to the apical surface of the cells and are oxidized to iodine. The...
9.4K
Targeted Cancer Therapies02:57

Targeted Cancer Therapies

The targeted cancer therapies, also known as “molecular targeted therapies,” take advantage of the molecular and genetic differences between the cancer cells and the normal cells. It needs a thorough understanding of the cancer cells to develop drugs that can target specific molecular aspects that drive the growth, progression, and spread of cancer cells without affecting the growth and survival of other normal cells in the body.
There are several types of targeted therapies against...
9.2K
Transducer Mechanism: Enzyme-Linked Receptors01:27

Transducer Mechanism: Enzyme-Linked Receptors

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.
Major types that are helpful drug targets include:
5.1K
Targets for Drug Action: Overview01:26

Targets for Drug Action: Overview

Drugs target macromolecules to modify ongoing cellular processes. Primary drug targets include receptors, ion channels, transporters, and enzymes.
Receptors are either membrane-spanning or intracellular proteins, which upon binding a ligand, get activated and transmit the signal downstream to elicit a response. Drugs bind receptors, either mimicking the action of endogenous ligands or blocking the receptor activity to bring about a modified response. Nearly 35% of approved drugs target the G...
11.9K
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:
6.4K
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...
6.6K