Chemistry:Thyromimetic

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Thyromimetic drugs are synthetic agonists of the thyroid hormone receptor's isoforms TR α1, TRα2, TRβ1, or TRβ2, mimicking some or all of the effects of endogenously produced thyroid hormones that regulate metabolism.[1][2] Some thyromimetic drugs are selective for various of these receptors over others, enabling more targeted effects and reducing toxicity. Thyromimetics selective for TRβ—including eprotirome,[3] sobetirome,[4] resmetirom,[5] and the prodrug VK2809—have been investigated for the treatment of non-alcoholic fatty liver disease, dyslipidemia, and other metabolic and neurodegenerative diseases.[6]

References

  1. ↑ Unnikrishnan, A. G.; Baruah, Manash; Kalra, Sanjay (December 2012). "Thyromimetics: What does the future hold?". Indian Journal of Endocrinology and Metabolism 16 (Suppl 2): S159–S161. doi:10.4103/2230-8210.104029. ISSN 2230-8210. PMID 23565368. 
  2. ↑ Devereaux, Jordan; Ferrara, Skylar J.; Scanlan, Thomas S. (2018) (in en). Quantification of Thyromimetic Sobetirome Concentration in Biological Tissue Samples. Methods in Molecular Biology. 1801. Springer. 193–206. doi:10.1007/978-1-4939-7902-8_16. ISBN 978-1-4939-7901-1. https://link.springer.com/protocol/10.1007/978-1-4939-7902-8_16. 
  3. ↑ Saponaro, Federica; Sestito, Simona; Runfola, Massimiliano; Rapposelli, Simona; Chiellini, Grazia (2020). "Selective Thyroid Hormone Receptor-Beta (TRβ) Agonists: New Perspectives for the Treatment of Metabolic and Neurodegenerative Disorders". Frontiers in Medicine 7. doi:10.3389/fmed.2020.00331. ISSN 2296-858X. 
  4. ↑ Tancevski, Ivan; Demetz, Egon; Eller, Philipp (1 January 2011). "Sobetirome: A Selective Thyromimetic for the Treatment of Dyslipidemia". Recent Patents on Cardiovascular Drug Discovery 6 (1): 16–19. doi:10.2174/157489011794578473. https://www.ingentaconnect.com/content/ben/prc/2011/00000006/00000001/art00003. 
  5. ↑ Alkhouri, Naim (1 February 2020). "Thyromimetics as emerging therapeutic agents for nonalcoholic steatohepatitis: rationale for the development of resmetirom (MGL-3196)" (in en). Expert Opinion on Investigational Drugs 29 (2): 99–101. doi:10.1080/13543784.2020.1708899. ISSN 1354-3784. https://www.tandfonline.com/doi/full/10.1080/13543784.2020.1708899. 
  6. ↑ Saponaro, Federica; Sestito, Simona; Runfola, Massimiliano; Rapposelli, Simona; Chiellini, Grazia (9 July 2020). "Selective Thyroid Hormone Receptor-Beta (TRβ) Agonists: New Perspectives for the Treatment of Metabolic and Neurodegenerative Disorders". Frontiers in Medicine 7: 331. doi:10.3389/fmed.2020.00331. ISSN 2296-858X. PMID 32733906. 

Further reading

  • Yehuda-Shnaidman, Einav; Kalderon, Bella; Bar-Tana, Jacob (2014). "Thyroid Hormone, Thyromimetics, and Metabolic Efficiency". Endocrine Reviews 35 (1): 35–58. doi:10.1210/er.2013-1006. 



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