Target Information
Target General Infomation | |||||
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Target ID |
T98933
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Former ID |
TTDR01227
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Target Name |
Thyroid hormone receptor beta-1
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Gene Name |
THRB
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Synonyms |
Nuclear receptor subfamily 1 group A member 2; Thyroid hormone receptor beta; c-erbA-2; c-erbA-beta; THRB
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Target Type |
Successful
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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.
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BioChemical Class |
Nuclear hormone receptor
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Target Validation |
T98933
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UniProt ID | |||||
Sequence |
MTPNSMTENGLTAWDKPKHCPDREHDWKLVGMSEACLHRKSHSERRSTLKNEQSSPHLIQ
TTWTSSIFHLDHDDVNDQSVSSAQTFQTEEKKCKGYIPSYLDKDELCVVCGDKATGYHYR CITCEGCKGFFRRTIQKNLHPSYSCKYEGKCVIDKVTRNQCQECRFKKCIYVGMATDLVL DDSKRLAKRKLIEENREKRRREELQKSIGHKPEPTDEEWELIKTVTEAHVATNAQGSHWK QKRKFLPEDIGQAPIVNAPEGGKVDLEAFSHFTKIITPAITRVVDFAKKLPMFCELPCED QIILLKGCCMEIMSLRAAVRYDPESETLTLNGEMAVTRGQLKNGGLGVVSDAIFDLGMSL SSFNLDDTEVALLQAVLLMSSDRPGLACVERIEKYQDSFLLAFEHYINYRKHHVTHFWPK LLMKVTDLRMIGACHASRFLHMKVECPTELFPPLFLEVFED |
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Drugs and Mode of Action | |||||
Drug(s) | Dextrothyroxine Sodium | Drug Info | Approved | High cholesterol levels in blood | [551871] |
BCT303 | Drug Info | Phase 2 | Hypothyroidism | [549461] | |
MB-07811 | Drug Info | Phase 2 | Hyperlipidaemia | [522631] | |
Axitirome | Drug Info | Phase 1 | Hyperlipidaemia | [544305] | |
MGL-3196 | Drug Info | Phase 1 | Hyperlipidaemia | [532494] | |
ZYT-1 | Drug Info | Phase 1 | Lipid metabolism disorder | [523811] | |
tiratricol | Drug Info | Clinical trial | Wound healing | [539702] | |
Inhibitor | (3,5-Dibromo-4-butoxy-phenyl)-acetic acid | Drug Info | [527532] | ||
(3,5-Dibromo-4-hexyloxy-phenyl)-acetic acid | Drug Info | [527532] | |||
(3,5-Dibromo-4-pentyloxy-phenyl)-acetic acid | Drug Info | [527532] | |||
(4-hexylphenyl)(oxiran-2-yl)methanone | Drug Info | [529081] | |||
(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-(Hexyloxy)phenyl)-3-morpholinopropan-1-one | Drug Info | [530166] | |||
1-(4-heptylphenyl)prop-2-en-1-one | Drug Info | [529081] | |||
1-(4-hexylphenyl)-3-(propylamino)propan-1-one | Drug Info | [529081] | |||
1-(4-hexylphenyl)-3-morpholinopropan-1-one | Drug Info | [529081] | |||
1-(4-HEXYLPHENYL)PROP-2-EN-1-ONE | Drug Info | [551374] | |||
1-(4-octylphenyl)prop-2-en-1-one | Drug Info | [529081] | |||
2-hexylphenyl acrylate | 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-heptylphenyl)propan-1-one | Drug Info | [530166] | |||
3-(dimethylamino)-1-(4-hexylphenyl)propan-1-one | Drug Info | [529081] | |||
3-bromo-1-(4-hexylphenyl)propan-1-one | Drug Info | [529081] | |||
4-(3-(Dimethylamino)propanoyl)-N-hexylbenzamide | Drug Info | [530166] | |||
4-(4-hexylphenyl)-4-oxobut-2-enoic acid | Drug Info | [529081] | |||
4-hexylphenyl propiolate | Drug Info | [529081] | |||
Cacodylate Ion | Drug Info | [551393] | |||
Detrothyronine | Drug Info | [527923] | |||
GC-24 | Drug Info | [551393] | |||
Modulator | Axitirome | Drug Info | [544305] | ||
BCT303 | Drug Info | [1572591] | |||
Dextrothyroxine Sodium | Drug Info | [556264] | |||
MB-07811 | Drug Info | [543886] | |||
ZYT-1 | Drug Info | [1572591] | |||
Agonist | MGL-3196 | Drug Info | [532494] | ||
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 | SIDS Susceptibility Pathways | ||||
Hematopoietic Stem Cell Differentiation | |||||
Nuclear Receptors | |||||
References | |||||
Ref 522631 | ClinicalTrials.gov (NCT00879112) Study of MB07811 in Subjects With Hypercholesterolemia. U.S. National Institutes of Health. | ||||
Ref 523811 | ClinicalTrials.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 532494 | Lipid 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 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 544305 | Bacterial biosensors for screening isoform-selective ligands for human thyroid receptors alpha-1 and beta-1. FEBS Open Bio. 2012; 2: 247-253. | ||||
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 530166 | J Med Chem. 2009 Jul 9;52(13):3892-901.Improvement of pharmacological properties of irreversible thyroid receptor coactivator binding inhibitors. | ||||
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 532494 | Lipid 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 543886 | (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). |
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