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Related Concept Videos

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.
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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 iodine is then...
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Related Experiment Video

Updated: May 10, 2026

In vivo Characterization of Endocrine Disrupting Chemical Effects via Thyroid Hormone Action Indicator Mouse
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Published on: October 6, 2023

Selective thyroid hormone receptor modulators.

Girish Raparti1, Suyog Jain, Karuna Ramteke

  • 1Department of Pharmacology, Government Medical College, Miraj, Maharashtra, India.

Indian Journal of Endocrinology and Metabolism
|June 19, 2013
PubMed
Summary

Thyroid hormone (TH) analogues offer therapeutic potential by targeting specific receptors, showing promise for conditions like dyslipidemia and heart failure. Further research is needed to enhance selectivity and minimize adverse effects for safer clinical applications.

Keywords:
35-diiodothyropropionic acidGC-1eprotiromehypolipidemicselective thyroid hormone receptor modulatorsthyroid analogue

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Area of Science:

  • Endocrinology
  • Pharmacology
  • Cardiovascular Medicine

Background:

  • Thyroid hormone (TH) exerts beneficial effects on organs but therapeutic use is limited by adverse effects.
  • Discovery of thyroid hormone receptor (TR) isoforms and their tissue distribution has renewed interest in TH analogues.
  • Targeting specific TR isoforms or tissues is key to developing safer TH-based therapies.

Purpose of the Study:

  • To explore the therapeutic potential of thyroid hormone analogues.
  • To review compounds targeting specific thyroid hormone receptor (TR) isoforms.
  • To assess the efficacy and safety of novel TH analogues in various conditions.

Main Methods:

  • Investigated structure-activity relationships of TR to develop isoform-specific compounds.
  • Reviewed studies on compounds like GC1, KB141, eprotirome, and DITPA.
  • Examined clinical data on eprotirome for dyslipidemia and obesity, and DITPA for heart failure.

Main Results:

  • Compounds GC1 and KB141 show preferential action on the TR β1 isoform.
  • Eprotirome demonstrated efficacy in treating dyslipidemia and obesity.
  • DITPA improved cardiac performance in heart failure models and a pilot study without increasing heart rate.

Conclusions:

  • TH analogues targeting specific TR isoforms show therapeutic promise for metabolic and cardiovascular diseases.
  • Compounds like eprotirome and DITPA offer potential benefits with improved safety profiles.
  • Further clinical trials and development of more selective compounds are essential for precise therapeutic action and minimizing adverse effects.