Target Information

Target General Infomation
Target ID
T98933
Former ID
TTDR01227
Target Name
Thyroid hormone receptor beta-1
Gene Name
THRB
Synonyms
Nuclear receptor subfamily 1 group A member 2; Thyroid hormone receptor beta; c-erbA-2; c-erbA-beta; THRB
Target Type
Successful
Disease Hyperlipidaemia [ICD9: 272.0-272.4; ICD10: E78]
Hyperthyroidism [ICD9: 242; ICD10: E05]
Hypothyroidism [ICD9: 244; ICD10: E03]
High cholesterol levels in blood [ICD10: E78.0]
Lipid metabolism disorder [ICD10: E75-E78]
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
T98933
UniProt ID
P10828
Sequence
MTPNSMTENGLTAWDKPKHCPDREHDWKLVGMSEACLHRKSHSERRSTLKNEQSSPHLIQ
TTWTSSIFHLDHDDVNDQSVSSAQTFQTEEKKCKGYIPSYLDKDELCVVCGDKATGYHYR
CITCEGCKGFFRRTIQKNLHPSYSCKYEGKCVIDKVTRNQCQECRFKKCIYVGMATDLVL
DDSKRLAKRKLIEENREKRRREELQKSIGHKPEPTDEEWELIKTVTEAHVATNAQGSHWK
QKRKFLPEDIGQAPIVNAPEGGKVDLEAFSHFTKIITPAITRVVDFAKKLPMFCELPCED
QIILLKGCCMEIMSLRAAVRYDPESETLTLNGEMAVTRGQLKNGGLGVVSDAIFDLGMSL
SSFNLDDTEVALLQAVLLMSSDRPGLACVERIEKYQDSFLLAFEHYINYRKHHVTHFWPK
LLMKVTDLRMIGACHASRFLHMKVECPTELFPPLFLEVFED
Drugs and Mode of Action
Drug(s) Dextrothyroxine Sodium Drug Info Approved High cholesterol levels in blood [1]
BCT303 Drug Info Phase 2 Hypothyroidism [2]
MB-07811 Drug Info Phase 2 Hyperlipidaemia [3]
Axitirome Drug Info Phase 1 Hyperlipidaemia [4]
MGL-3196 Drug Info Phase 1 Hyperlipidaemia [5]
ZYT-1 Drug Info Phase 1 Lipid metabolism disorder [6]
tiratricol Drug Info Clinical trial Wound healing [7]
Inhibitor (3,5-Dibromo-4-butoxy-phenyl)-acetic acid Drug Info [8]
(3,5-Dibromo-4-hexyloxy-phenyl)-acetic acid Drug Info [8]
(3,5-Dibromo-4-pentyloxy-phenyl)-acetic acid Drug Info [8]
(4-hexylphenyl)(oxiran-2-yl)methanone Drug Info [9]
(E)-1-(4-heptylphenyl)but-2-en-1-one Drug Info [9]
(Z)-4-(4-hexylphenylamino)-4-oxobut-2-enoic acid Drug Info [9]
1-(4-(Hexyloxy)phenyl)-3-morpholinopropan-1-one Drug Info [10]
1-(4-heptylphenyl)prop-2-en-1-one Drug Info [9]
1-(4-hexylphenyl)-3-(propylamino)propan-1-one Drug Info [9]
1-(4-hexylphenyl)-3-morpholinopropan-1-one Drug Info [9]
1-(4-HEXYLPHENYL)PROP-2-EN-1-ONE Drug Info [11]
1-(4-octylphenyl)prop-2-en-1-one Drug Info [9]
2-hexylphenyl acrylate Drug Info [9]
3-(3,5-Dibromo-4-hexyloxy-phenyl)-propionic acid Drug Info [8]
3-(4-(benzyloxy)-3,5-dibromophenyl)propanoic acid Drug Info [12]
3-(dibutylamino)-1-(4-hexylphenyl)propan-1-one Drug Info [9]
3-(dimethylamino)-1-(4-heptylphenyl)propan-1-one Drug Info [10]
3-(dimethylamino)-1-(4-hexylphenyl)propan-1-one Drug Info [9]
3-bromo-1-(4-hexylphenyl)propan-1-one Drug Info [9]
4-(3-(Dimethylamino)propanoyl)-N-hexylbenzamide Drug Info [10]
4-(4-hexylphenyl)-4-oxobut-2-enoic acid Drug Info [9]
4-hexylphenyl propiolate Drug Info [9]
Cacodylate Ion Drug Info [13]
Detrothyronine Drug Info [14]
GC-24 Drug Info [13]
Modulator Axitirome Drug Info [4]
BCT303 Drug Info [15]
Dextrothyroxine Sodium Drug Info [16]
MB-07811 Drug Info [17]
ZYT-1 Drug Info [15]
Agonist MGL-3196 Drug Info [5]
rT3 Drug Info [18]
tiratricol Drug Info [18]
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 SIDS Susceptibility Pathways
Hematopoietic Stem Cell Differentiation
Nuclear Receptors
References
REF 1Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 2Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800037654)
REF 3ClinicalTrials.gov (NCT00879112) Study of MB07811 in Subjects With Hypercholesterolemia. U.S. National Institutes of Health.
REF 4Bacterial biosensors for screening isoform-selective ligands for human thyroid receptors alpha-1 and beta-1. FEBS Open Bio. 2012; 2: 247-253.
REF 5Lipid lowering in healthy volunteers treated with multiple doses of MGL-3196, a liver-targeted thyroid hormone receptor-beta agonist. Atherosclerosis. 2013 Oct;230(2):373-80.
REF 6ClinicalTrials.gov (NCT01543269) A Clinical Study to Evaluate the Safety,Tolerability and PK of ZYT1, Following Oral Administration in Healthy Volunteers. U.S. National Institutes of Health.
REF 7(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 8J 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 9J 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 10J Med Chem. 2009 Jul 9;52(13):3892-901.Improvement of pharmacological properties of irreversible thyroid receptor coactivator binding inhibitors.
REF 11The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
REF 12Bioorg 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 13How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.
REF 14Bioorg 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 15Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
REF 16Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services.
REF 17(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. (Target id: 589).
REF 18Binding 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.

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