Target Information
Target General Infomation | |||||
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Target ID |
T79591
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Former ID |
TTDS00381
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Target Name |
Thyroid hormone receptor alpha
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Gene Name |
THRA
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Synonyms |
C-erbA-1; C-erbA-alpha; EAR-7; EAR7; THRA
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Target Type |
Successful
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Disease | Hypothyroidism of any etiology [ICD10: R68, T68] | ||||
Hypothyroidism [ICD9: 244; ICD10: E03] | |||||
High cholesterol levels in blood [ICD10: E78.0] | |||||
Wound healing [ICD10: T14.0-T14.1] | |||||
Function |
Nuclear hormone receptor that can act as a repressor or activator of transcription. High affinity receptor for thyroid hormones, including triiodothyronine and thyroxine.
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BioChemical Class |
Nuclear hormone receptor
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Target Validation |
T79591
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UniProt ID | |||||
Sequence |
MEQKPSKVECGSDPEENSARSPDGKRKRKNGQCSLKTSMSGYIPSYLDKDEQCVVCGDKA
TGYHYRCITCEGCKGFFRRTIQKNLHPTYSCKYDSCCVIDKITRNQCQLCRFKKCIAVGM AMDLVLDDSKRVAKRKLIEQNRERRRKEEMIRSLQQRPEPTPEEWDLIHIATEAHRSTNA QGSHWKQRRKFLPDDIGQSPIVSMPDGDKVDLEAFSEFTKIITPAITRVVDFAKKLPMFS ELPCEDQIILLKGCCMEIMSLRAAVRYDPESDTLTLSGEMAVKREQLKNGGLGVVSDAIF ELGKSLSAFNLDDTEVALLQAVLLMSTDRSGLLCVDKIEKSQEAYLLAFEHYVNHRKHNI PHFWPKLLMKEREVQSSILYKGAAAEGRPGGSLGVHPEGQQLLGMHVVQGPQVRQLEQQL GEAGSLQGPVLQHQSPKSPQQRLLELLHRSGILHARAVCGEDDSSEADSPSSSEEEPEVC EDLAGNAASP |
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Drugs and Mode of Action | |||||
Drug(s) | Dextrothyroxine Sodium | Drug Info | Approved | High cholesterol levels in blood | [551871] |
Levothyroxine | Drug Info | Approved | Hypothyroidism | [467866], [536138] | |
Liothyronine | Drug Info | Approved | Hypothyroidism of any etiology | [551871] | |
BCT303 | Drug Info | Phase 2 | Hypothyroidism | [549461] | |
tiratricol | Drug Info | Clinical trial | Wound healing | [539702] | |
Inhibitor | (3,5-Dibromo-4-hexyloxy-phenyl)-acetic acid | Drug Info | [527532] | ||
(E)-1-(4-heptylphenyl)but-2-en-1-one | Drug Info | [529081] | |||
(Z)-4-(4-hexylphenylamino)-4-oxobut-2-enoic acid | Drug Info | [529081] | |||
1-(4-hexylphenyl)-3-morpholinopropan-1-one | Drug Info | [529081] | |||
3-(3,5-Dibromo-4-hexyloxy-phenyl)-propionic acid | Drug Info | [527532] | |||
3-(4-(benzyloxy)-3,5-dibromophenyl)propanoic acid | Drug Info | [528640] | |||
3-(dibutylamino)-1-(4-hexylphenyl)propan-1-one | Drug Info | [529081] | |||
3-(dimethylamino)-1-(4-hexylphenyl)propan-1-one | Drug Info | [529081] | |||
3-bromo-1-(4-hexylphenyl)propan-1-one | Drug Info | [529081] | |||
4-(4-hexylphenyl)-4-oxobut-2-enoic acid | Drug Info | [529081] | |||
4-hexylphenyl propiolate | Drug Info | [529081] | |||
Detrothyronine | Drug Info | [527923] | |||
Modulator | BCT303 | Drug Info | [1572591] | ||
Dextrothyroxine Sodium | Drug Info | [556264] | |||
Antagonist | Levothyroxine | Drug Info | [536362], [536861] | ||
Liothyronine | Drug Info | [536362], [536494] | |||
Agonist | rT3 | Drug Info | [531482] | ||
tiratricol | Drug Info | [531482] | |||
Pathways | |||||
KEGG Pathway | Neuroactive ligand-receptor interaction | ||||
Thyroid hormone signaling pathway | |||||
Pathway Interaction Database | RXR and RAR heterodimerization with other nuclear receptor | ||||
Reactome | Nuclear Receptor transcription pathway | ||||
WikiPathways | Endochondral Ossification | ||||
Nuclear Receptors | |||||
References | |||||
Ref 467866 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 4627). | ||||
Ref 536138 | Current methodology to assess bioequivalence of levothyroxine sodium products is inadequate. AAPS J. 2005 Mar 30;7(1):E42-6. | ||||
Ref 539702 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2637). | ||||
Ref 527532 | J Med Chem. 2005 May 5;48(9):3114-7.Thyroid receptor ligands. 3. Design and synthesis of 3,5-dihalo-4-alkoxyphenylalkanoic acids as indirect antagonists of the thyroid hormone receptor. | ||||
Ref 527923 | Bioorg Med Chem Lett. 2006 Mar 1;16(5):1240-4. Epub 2005 Dec 9.Thyroid receptor ligands. Part 5: novel bicyclic agonist ligands selective for the thyroid hormone receptor beta. | ||||
Ref 528640 | Bioorg Med Chem Lett. 2007 Apr 1;17(7):2018-21. Epub 2007 Jan 13.Thyroid receptor ligands. Part 7: Indirect antagonists of the thyroid hormone receptor with improved affinity. | ||||
Ref 529081 | J Med Chem. 2007 Nov 1;50(22):5269-80. Epub 2007 Oct 5.Inhibitors of the interaction of a thyroid hormone receptor and coactivators: preliminary structure-activity relationships. | ||||
Ref 531482 | Binding of 3,5,3'-triiodothyronine (T3) and its analogs to the in vitro translational products of c-erbA protooncogenes: differences in the affinity of the alpha- and beta-forms for the acetic acid analog and failure of the human testis and kidney alpha-2 products to bind T3. Mol Endocrinol. 1990 Feb;4(2):227-34. | ||||
Ref 536362 | Thyroid hormone receptors in brain development and function. Nat Clin Pract Endocrinol Metab. 2007 Mar;3(3):249-59. | ||||
Ref 536494 | Evaluation of thyroid hormone action in a case of generalized resistance to thyroid hormone with chronic thyroiditis: discovery of a novel heterozygous missense mutation (G347A). Endocr J. 2007 Dec;54(5):727-32. Epub 2007 Sep 7. |
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