Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDS00381

Target Information
NameThyroid hormone receptor alpha    
Type of targetSuccessful target    
SynonymsC-erbA-1    
C-erbA-alpha    
EAR-7    
EAR7    
DiseaseThyrotoxicosis [hyperthyroidism]
[ICD9: 242.9   ICD10: E05]
[1]
Drug(s)LevothyroxineApprovedHypothyroidism[2][3]
LiothyronineApprovedHypothyroidism[4][3]
BioChemical ClassZinc-finger    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP10827
PDB Structure1NAV; 2H79.    
FunctionNuclear hormone receptor. High affinity receptor for triiodothyronine.    
SequenceMEQKPSKVECGSDPEENSARSPDGKRKRKNGQCSLKTSMSGYIPSYLDKDEQCVVCGDKA TGYHYRCITCEGCKGFFRRTIQKNLHPTYSCKYDSCCVIDKITRNQCQLCRFKKCIAVGM AMDLVLDDSKRVAKRKLIEQNRERRRKEEMIRSLQQRPEPTPEEWDLIHIATEAHRSTNA QGSHWKQRRKFLPDDIGQSPIVSMPDGDKVDLEAFSEFTKIITPAITRVVDFAKKLPMFS ELPCEDQIILLKGCCMEIMSLRAAVRYDPESDTLTLSGEMAVKREQLKNGGLGVVSDAIF ELGKSLSAFNLDDTEVALLQAVLLMSTDRSGLLCVDKIEKSQEAYLLAFEHYVNHRKHNI PHFWPKLLMKEREVQSSILYKGAAAEGRPGGSLGVHPEGQQLLGMHVVQGPQVRQLEQQL GEAGSLQGPVLQHQSPKSPQQRLLELLHRSGILHARAVCGEDDSSEADSPSSSEEEPEVC EDLAGNAASP
Target ValidationClick to Find Target Validation Information.    
Inhibitor (3,5-Dibromo-4-hexyloxy-phenyl)-acetic acid[5]
(E)-1-[6]
(Z)-4-[6]
1- (4-hexylphenyl)-3-morpholinopropan-1-one[6]
3- (3,5-Dibromo-4-hexyloxy-phenyl)-propionic acid[5]
3- (4-[7]
3- (dibutylamino)-1-[6]
3- (dimethylamino)-1-[6]
3-bromo-1- (4-hexylphenyl)propan-1-one[6]
4- (4-hexylphenyl)-4-oxobut-2-enoic acid[6]
4-hexylphenyl propiolate[6]
Detrothyronine[8]
MB-07344[9]
AntagonistLevothyroxine[2][3]
Liothyronine[4][3]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Deletion of the thyroid hormone receptor alpha 1 prevents the structural alterations of the cerebellum induced by hypothyroidism. Proc Natl Acad Sci U S A. 2002 Mar 19;99(6):3985-9. Epub 2002 Mar 12. To Reference
Ref 2Thyroid hormone resistance and pituitary enlargement after thyroid ablation in a woman on levothyroxine treatment. Thyroid. 2008 Oct;18(10):1119-23. To Reference
Ref 3Thyroid hormone receptors in brain development and function. Nat Clin Pract Endocrinol Metab. 2007 Mar;3(3):249-59. To Reference
Ref 4Evaluation 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. To Reference
Ref 5J 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. To Reference
Ref 6J 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. To Reference
Ref 7Bioorg 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. To Reference
Ref 8Bioorg 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. To Reference
Ref 9J Med Chem. 2008 Nov 27;51(22):7075-93.Synthesis and biological evaluation of a series of liver-selective phosphonic acid thyroid hormone receptor agonists and their prodrugs. To Reference



 

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