Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDR01227

Target Information
NameThyroid hormone receptor beta-1    
Type of targetClinical trial target    
DiseaseHyperlipidemia
[ICD9: 272.0-272.4   ICD10: E78]
[1]
Obesity
[ICD9: 278   ICD10: E66]
[1]
Thyroid hormone resistance syndrome[2][3]
Thyrotoxicosis [hyperthyroidism]
[ICD9: 242.9   ICD10: E05]
[4]
BioChemical ClassZinc-finger    
PathwayNeuroactive ligand-receptor interaction
UniProt IDP10828
PDB Structure1BSX; 1N46; 1NAX; 1NQ0; 1NQ1; 1NQ2; 1NUO; 1Q4X; 1R6G; 1XZX; 1Y0X; 2J4A; 2NLL; 2PIN; 3D57; 3GWS; 3IMY; 3JZC.    
FunctionHigh affinity receptor for triiodothyronine.    
SequenceMTPNSMTENGLTAWDKPKHCPDREHDWKLVGMSEACLHRKSHSERRSTLKNEQSSPHLIQ TTWTSSIFHLDHDDVNDQSVSSAQTFQTEEKKCKGYIPSYLDKDELCVVCGDKATGYHYR CITCEGCKGFFRRTIQKNLHPSYSCKYEGKCVIDKVTRNQCQECRFKKCIYVGMATDLVL DDSKRLAKRKLIEENREKRRREELQKSIGHKPEPTDEEWELIKTVTEAHVATNAQGSHWK QKRKFLPEDIGQAPIVNAPEGGKVDLEAFSHFTKIITPAITRVVDFAKKLPMFCELPCED QIILLKGCCMEIMSLRAAVRYDPESETLTLNGEMAVTRGQLKNGGLGVVSDAIFDLGMSL SSFNLDDTEVALLQAVLLMSSDRPGLACVERIEKYQDSFLLAFEHYINYRKHHVTHFWPK LLMKVTDLRMIGACHASRFLHMKVECPTELFPPLFLEVFED
Target ValidationClick to Find Target Validation Information.    
Inhibitor (3,5-Dibromo-4-butoxy-phenyl)-acetic acid[5]
(3,5-Dibromo-4-hexyloxy-phenyl)-acetic acid[5]
(3,5-Dibromo-4-pentyloxy-phenyl)-acetic acid[5]
(4-hexylphenyl)[6]
(E)-1-[6]
(Z)-4-[6]
1- (4-[7]
1- (4-HEXYLPHENYL)PROP-2-EN-1-ONE[8]
1- (4-heptylphenyl)prop-2-en-1-one[6]
1- (4-hexylphenyl)-3-[6]
1- (4-hexylphenyl)-3-morpholinopropan-1-one[6]
1- (4-octylphenyl)prop-2-en-1-one[6]
2-hexylphenyl acrylate[6]
3- (3,5-Dibromo-4-hexyloxy-phenyl)-propionic acid[5]
3- (4-[9]
3- (dibutylamino)-1-[6]
3- (dimethylamino)-1-[7]
3- (dimethylamino)-1-[6]
3-bromo-1- (4-hexylphenyl)propan-1-one[6]
4- (3-[7]
4- (4-hexylphenyl)-4-oxobut-2-enoic acid[6]
4-hexylphenyl propiolate[6]
Cacodylate Ion[10]
Detrothyronine[11]
GC-24[10]
MB-07344[12]
AgonistGC-1[1]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1The thyroid hormone receptor-beta-selective agonist GC-1 differentially affects plasma lipids and cardiac activity. Endocrinology. 2000 Sep;141(9):3057-64. To Reference
Ref 2A mouse model of resistance to thyroid hormone produced by somatic gene transfer of a mutant thyroid hormone receptor. Mol Endocrinol. 1996 Jan;10(1):100-6. To Reference
Ref 3Enhanced levels of wild-type versus mutant thyroid hormone receptor beta 1 messenger RNA in fibroblasts from heterozygotes of kindred S with thyroid hormone resistance. Thyroid. 1996 Jun;6(3):189-94. To Reference
Ref 4Deletion 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 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 7J Med Chem. 2009 Jul 9;52(13):3892-901.Improvement of pharmacological properties of irreversible thyroid receptor coactivator binding inhibitors. To Reference
Ref 8Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. To Reference
Ref 9Bioorg 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 10Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 11Bioorg 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 12J 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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