Target Information

Target General Infomation
Target ID
T79591
Former ID
TTDS00381
Target Name
Thyroid hormone receptor alpha
Gene Name
THRA
Synonyms
C-erbA-1; C-erbA-alpha; EAR-7; EAR7; THRA
Target Type
Successful
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.
BioChemical Class
Nuclear hormone receptor
Target Validation
T79591
UniProt ID
P10827
Sequence
MEQKPSKVECGSDPEENSARSPDGKRKRKNGQCSLKTSMSGYIPSYLDKDEQCVVCGDKA
TGYHYRCITCEGCKGFFRRTIQKNLHPTYSCKYDSCCVIDKITRNQCQLCRFKKCIAVGM
AMDLVLDDSKRVAKRKLIEQNRERRRKEEMIRSLQQRPEPTPEEWDLIHIATEAHRSTNA
QGSHWKQRRKFLPDDIGQSPIVSMPDGDKVDLEAFSEFTKIITPAITRVVDFAKKLPMFS
ELPCEDQIILLKGCCMEIMSLRAAVRYDPESDTLTLSGEMAVKREQLKNGGLGVVSDAIF
ELGKSLSAFNLDDTEVALLQAVLLMSTDRSGLLCVDKIEKSQEAYLLAFEHYVNHRKHNI
PHFWPKLLMKEREVQSSILYKGAAAEGRPGGSLGVHPEGQQLLGMHVVQGPQVRQLEQQL
GEAGSLQGPVLQHQSPKSPQQRLLELLHRSGILHARAVCGEDDSSEADSPSSSEEEPEVC
EDLAGNAASP
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 536138Current 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 549461Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800037654)
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref
Ref 527532J 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 527923Bioorg 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 528640Bioorg 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 529081J 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 531482Binding 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 536362Thyroid hormone receptors in brain development and function. Nat Clin Pract Endocrinol Metab. 2007 Mar;3(3):249-59.
Ref 536494Evaluation 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.
Ref 536861Thyroid hormone resistance and pituitary enlargement after thyroid ablation in a woman on levothyroxine treatment. Thyroid. 2008 Oct;18(10):1119-23.
Ref 556264Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
Ref 1572591Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.

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