Selective thyroid hormone receptor modulators
Thyroid hormone (TH) is known to have many beneficial effects on vital organs, but its extrapolation to be used therapeutically has been restricted by the fact that it does have concurrent adverse effects. Recent finding of various thyroid hormone receptors (TR) isoforms and their differential patte...
| Main Authors: | , , , , , , |
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| Format: | Article |
| Language: | English |
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Wolters Kluwer Medknow Publications
2013-01-01
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| Series: | Indian Journal of Endocrinology and Metabolism |
| Subjects: | |
| Online Access: | http://www.ijem.in/article.asp?issn=2230-8210;year=2013;volume=17;issue=2;spage=211;epage=218;aulast=Raparti |
| _version_ | 1818215568496394240 |
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| author | Girish Raparti Suyog Jain Karuna Ramteke Mangala Murthy Ravi Ghanghas Sunita Ramanand Jaiprakash Ramanand |
| author_facet | Girish Raparti Suyog Jain Karuna Ramteke Mangala Murthy Ravi Ghanghas Sunita Ramanand Jaiprakash Ramanand |
| author_sort | Girish Raparti |
| collection | DOAJ |
| description | Thyroid hormone (TH) is known to have many beneficial effects on vital organs, but its extrapolation to be used therapeutically has been restricted by the fact that it does have concurrent adverse effects. Recent finding of various thyroid hormone receptors (TR) isoforms and their differential pattern of tissue distribution has regained interest in possible use of TH analogues in therapeutics. These findings were followed by search of compounds with isoform-specific or tissue-specific action on TR. Studying the structure-activity relationship of TR led to the development of compounds like GC1 and KB141, which preferentially act on the β1 isoform of TR. More recently, eprotirome was developed and has been studied in humans. It has shown to be effective in dyslipidemia by the lipid-lowering action of TH in the liver and also in obesity. Another compound, 3,5-diiodothyropropionic acid (DITPA), binds to both α- and β-type TRs with relatively low affinity and has been shown to be effective in heart failure (HF). In postinfarction models of HF and in a pilot clinical study, DITPA increased cardiac performance without affecting the heart rate. TR antagonists like NH3 can be used in thyrotoxicosis and cardiac arrhythmias. However, further larger clinical trials on some of these promising compounds and development of newer compounds with increased selectivity is required to achieve higher precision of action and avoid adverse effects seen with TH. |
| first_indexed | 2024-12-12T06:38:09Z |
| format | Article |
| id | doaj.art-bbf61fe492664f9191021ce5d80e9bf4 |
| institution | Directory Open Access Journal |
| issn | 2230-8210 2230-9500 |
| language | English |
| last_indexed | 2024-12-12T06:38:09Z |
| publishDate | 2013-01-01 |
| publisher | Wolters Kluwer Medknow Publications |
| record_format | Article |
| series | Indian Journal of Endocrinology and Metabolism |
| spelling | doaj.art-bbf61fe492664f9191021ce5d80e9bf42022-12-22T00:34:25ZengWolters Kluwer Medknow PublicationsIndian Journal of Endocrinology and Metabolism2230-82102230-95002013-01-0117221121810.4103/2230-8210.109663Selective thyroid hormone receptor modulatorsGirish RapartiSuyog JainKaruna RamtekeMangala MurthyRavi GhanghasSunita RamanandJaiprakash RamanandThyroid hormone (TH) is known to have many beneficial effects on vital organs, but its extrapolation to be used therapeutically has been restricted by the fact that it does have concurrent adverse effects. Recent finding of various thyroid hormone receptors (TR) isoforms and their differential pattern of tissue distribution has regained interest in possible use of TH analogues in therapeutics. These findings were followed by search of compounds with isoform-specific or tissue-specific action on TR. Studying the structure-activity relationship of TR led to the development of compounds like GC1 and KB141, which preferentially act on the β1 isoform of TR. More recently, eprotirome was developed and has been studied in humans. It has shown to be effective in dyslipidemia by the lipid-lowering action of TH in the liver and also in obesity. Another compound, 3,5-diiodothyropropionic acid (DITPA), binds to both α- and β-type TRs with relatively low affinity and has been shown to be effective in heart failure (HF). In postinfarction models of HF and in a pilot clinical study, DITPA increased cardiac performance without affecting the heart rate. TR antagonists like NH3 can be used in thyrotoxicosis and cardiac arrhythmias. However, further larger clinical trials on some of these promising compounds and development of newer compounds with increased selectivity is required to achieve higher precision of action and avoid adverse effects seen with TH.http://www.ijem.in/article.asp?issn=2230-8210;year=2013;volume=17;issue=2;spage=211;epage=218;aulast=Raparti35-diiodothyropropionic acideprotiromeGC-1hypolipidemicselective thyroid hormone receptor modulatorsthyroid analogue |
| spellingShingle | Girish Raparti Suyog Jain Karuna Ramteke Mangala Murthy Ravi Ghanghas Sunita Ramanand Jaiprakash Ramanand Selective thyroid hormone receptor modulators Indian Journal of Endocrinology and Metabolism 3 5-diiodothyropropionic acid eprotirome GC-1 hypolipidemic selective thyroid hormone receptor modulators thyroid analogue |
| title | Selective thyroid hormone receptor modulators |
| title_full | Selective thyroid hormone receptor modulators |
| title_fullStr | Selective thyroid hormone receptor modulators |
| title_full_unstemmed | Selective thyroid hormone receptor modulators |
| title_short | Selective thyroid hormone receptor modulators |
| title_sort | selective thyroid hormone receptor modulators |
| topic | 3 5-diiodothyropropionic acid eprotirome GC-1 hypolipidemic selective thyroid hormone receptor modulators thyroid analogue |
| url | http://www.ijem.in/article.asp?issn=2230-8210;year=2013;volume=17;issue=2;spage=211;epage=218;aulast=Raparti |
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