Proteins > Thyroid hormone receptor alpha
Page last updated: 2024-08-07 15:53:28
Thyroid hormone receptor alpha
A thyroid hormone receptor alpha that is encoded in the genome of human. [PRO:HJD, UniProtKB:P10827]
Synonyms
Nuclear receptor subfamily 1 group A member 1;
V-erbA-related protein 7;
EAR-7;
c-erbA-1;
c-erbA-alpha
Research
Bioassay Publications (29)
Timeframe | Studies on this Protein(%) | All Drugs % |
pre-1990 | 0 (0.00) | 18.7374 |
1990's | 1 (3.45) | 18.2507 |
2000's | 18 (62.07) | 29.6817 |
2010's | 7 (24.14) | 24.3611 |
2020's | 3 (10.34) | 2.80 |
Compounds (17)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
2D QSAR studies on thyroid hormone receptor ligands.Bioorganic & medicinal chemistry, , Jul-01, Volume: 15, Issue:13, 2007
Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1.Journal of medicinal chemistry, , Apr-24, Volume: 46, Issue:9, 2003
2D QSAR studies on thyroid hormone receptor ligands.Bioorganic & medicinal chemistry, , Jul-01, Volume: 15, Issue:13, 2007
Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1.Journal of medicinal chemistry, , Apr-24, Volume: 46, Issue:9, 2003
Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist.Journal of medicinal chemistry, , 05-26, Volume: 65, Issue:10, 2022
Discovery of (Journal of medicinal chemistry, , 07-28, Volume: 65, Issue:14, 2022
l-Thyroxin and the Nonclassical Thyroid Hormone TETRAC Are Potent Activators of PPARγ.Journal of medicinal chemistry, , 07-09, Volume: 63, Issue:13, 2020
Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor β agonist in clinical trials for the treatment of dysJournal of medicinal chemistry, , May-22, Volume: 57, Issue:10, 2014
Identification of the first inverse agonist of retinoid-related orphan receptor (ROR) with dual selectivity for RORβ and RORγt.Bioorganic & medicinal chemistry letters, , Nov-15, Volume: 24, Issue:22, 2014
Synthesis and pharmacological characterization of 1-benzyl-4-aminoindole-based thyroid hormone receptor β agonists.Bioorganic & medicinal chemistry, , Jan-01, Volume: 22, Issue:1, 2014
Design, synthesis, and structure-activity relationship (SAR) of N-[7-(4-hydroxyphenoxy)-6-methylindan-4-yl]malonamic acids as thyroid hormone receptor β (TRβ) selective agonists.Bioorganic & medicinal chemistry, , Feb-01, Volume: 21, Issue:3, 2013
Discovery of novel indane derivatives as liver-selective thyroid hormone receptor β (TRβ) agonists for the treatment of dyslipidemia.Bioorganic & medicinal chemistry, , Jun-01, Volume: 20, Issue:11, 2012
Characterization of thyroid hormone receptor alpha (TRalpha)-specific analogs with varying inner- and outer-ring substituents.Bioorganic & medicinal chemistry, , Jan-15, Volume: 16, Issue:2, 2008
Synthesis and biological evaluation of a series of liver-selective phosphonic acid thyroid hormone receptor agonists and their prodrugs.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index.Proceedings of the National Academy of Sciences of the United States of America, , Sep-25, Volume: 104, Issue:39, 2007
Thyroid receptor ligands. Part 8: Thyromimetics derived from N-acylated-alpha-amino acid derivatives displaying modulated pharmacological selectivity compared with KB-141.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 17, Issue:15, 2007
Thyroid receptor ligands. Part 4: 4'-amido bioisosteric ligands selective for the thyroid hormone receptor beta.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 16, Issue:4, 2006
Design and characterization of a thyroid hormone receptor alpha (TRalpha)-specific agonist.ACS chemical biology, , Oct-24, Volume: 1, Issue:9, 2006
A new class of high affinity thyromimetics containing a phenyl-naphthylene core.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 15, Issue:20, 2005
Thyroid receptor ligands. Part 2: Thyromimetics with improved selectivity for the thyroid hormone receptor beta.Bioorganic & medicinal chemistry letters, , Jul-05, Volume: 14, Issue:13, 2004
Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1.Journal of medicinal chemistry, , Apr-24, Volume: 46, Issue:9, 2003
Structural determinants of selective thyromimetics.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
Discovery of a novel series of 6-azauracil-based thyroid hormone receptor ligands: potent, TR beta subtype-selective thyromimetics.Bioorganic & medicinal chemistry letters, , Feb-10, Volume: 13, Issue:3, 2003
Rational design and synthesis of a novel thyroid hormone antagonist that blocks coactivator recruitment.Journal of medicinal chemistry, , Jul-18, Volume: 45, Issue:15, 2002
A designed antagonist of the thyroid hormone receptor.Bioorganic & medicinal chemistry letters, , Nov-05, Volume: 11, Issue:21, 2001
A high-affinity subtype-selective agonist ligand for the thyroid hormone receptor.Chemistry & biology, , Volume: 5, Issue:6, 1998
Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor β agonist in clinical trials for the treatment of dysJournal of medicinal chemistry, , May-22, Volume: 57, Issue:10, 2014
Selective thyromimetics using receptor and tissue selectivity approaches: prospects for dyslipidemia.Journal of medicinal chemistry, , Jun-28, Volume: 55, Issue:12, 2012
Synthesis and biological evaluation of a series of liver-selective phosphonic acid thyroid hormone receptor agonists and their prodrugs.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Structural determinants of selective thyromimetics.Journal of medicinal chemistry, , Jul-03, Volume: 46, Issue:14, 2003
Rational design and synthesis of a novel thyroid hormone antagonist that blocks coactivator recruitment.Journal of medicinal chemistry, , Jul-18, Volume: 45, Issue:15, 2002
A high-affinity subtype-selective agonist ligand for the thyroid hormone receptor.Chemistry & biology, , Volume: 5, Issue:6, 1998
Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor β agonist in clinical trials for the treatment of dysJournal of medicinal chemistry, , May-22, Volume: 57, Issue:10, 2014
Selective thyromimetics using receptor and tissue selectivity approaches: prospects for dyslipidemia.Journal of medicinal chemistry, , Jun-28, Volume: 55, Issue:12, 2012
Synthesis and biological evaluation of a series of liver-selective phosphonic acid thyroid hormone receptor agonists and their prodrugs.Journal of medicinal chemistry, , Nov-27, Volume: 51, Issue:22, 2008
Design and synthesis of novel 3-hydroxy-cyclobut-3-ene-1,2-dione derivatives as thyroid hormone receptor beta (TR-beta) selective ligands.Bioorganic & medicinal chemistry letters, , Jul-15, Volume: 18, Issue:14, 2008
Thyroid receptor ligands. Part 8: Thyromimetics derived from N-acylated-alpha-amino acid derivatives displaying modulated pharmacological selectivity compared with KB-141.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 17, Issue:15, 2007
2D QSAR studies on thyroid hormone receptor ligands.Bioorganic & medicinal chemistry, , Jul-01, Volume: 15, Issue:13, 2007
Targeting thyroid hormone receptor-beta agonists to the liver reduces cholesterol and triglycerides and improves the therapeutic index.Proceedings of the National Academy of Sciences of the United States of America, , Sep-25, Volume: 104, Issue:39, 2007
Thyroid receptor ligands. Part 4: 4'-amido bioisosteric ligands selective for the thyroid hormone receptor beta.Bioorganic & medicinal chemistry letters, , Feb-15, Volume: 16, Issue:4, 2006
A new class of high affinity thyromimetics containing a phenyl-naphthylene core.Bioorganic & medicinal chemistry letters, , Oct-15, Volume: 15, Issue:20, 2005
Thyroid receptor ligands. Part 2: Thyromimetics with improved selectivity for the thyroid hormone receptor beta.Bioorganic & medicinal chemistry letters, , Jul-05, Volume: 14, Issue:13, 2004
Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1.Journal of medicinal chemistry, , Apr-24, Volume: 46, Issue:9, 2003
Thyroid receptor ligands. 3. Design and synthesis of 3,5-dihalo-4-alkoxyphenylalkanoic acids as indirect antagonists of the thyroid hormone receptor.Journal of medicinal chemistry, , May-05, Volume: 48, Issue:9, 2005
Synthesis and preliminary characterization of a novel antiarrhythmic compound (KB130015) with an improved toxicity profile compared with amiodarone.Journal of medicinal chemistry, , Jan-31, Volume: 45, Issue:3, 2002
2D QSAR studies on thyroid hormone receptor ligands.Bioorganic & medicinal chemistry, , Jul-01, Volume: 15, Issue:13, 2007
Thyroid receptor ligands. Part 8: Thyromimetics derived from N-acylated-alpha-amino acid derivatives displaying modulated pharmacological selectivity compared with KB-141.Bioorganic & medicinal chemistry letters, , Aug-01, Volume: 17, Issue:15, 2007
Thyroid receptor ligands. Part 2: Thyromimetics with improved selectivity for the thyroid hormone receptor beta.Bioorganic & medicinal chemistry letters, , Jul-05, Volume: 14, Issue:13, 2004
Thyroid receptor ligands. 1. Agonist ligands selective for the thyroid receptor beta1.Journal of medicinal chemistry, , Apr-24, Volume: 46, Issue:9, 2003
Discovery of a Highly Selective and H435R-Sensitive Thyroid Hormone Receptor β Agonist.Journal of medicinal chemistry, , 05-26, Volume: 65, Issue:10, 2022
Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a Highly Selective Thyroid Hormone Receptor β agonist in clinical trials for the treatment of dysJournal of medicinal chemistry, , May-22, Volume: 57, Issue:10, 2014
Enables
This protein enables 12 target(s):
Target | Category | Definition |
transcription cis-regulatory region binding | molecular function | Binding to a specific sequence of DNA that is part of a regulatory region that controls transcription of that section of the DNA. The transcribed region might be described as a gene, cistron, or operon. [GOC:txnOH] |
DNA-binding transcription factor activity, RNA polymerase II-specific | molecular function | A DNA-binding transcription factor activity that modulates the transcription of specific gene sets transcribed by RNA polymerase II. [GOC:txnOH-2018] |
DNA-binding transcription factor activity | molecular function | A transcription regulator activity that modulates transcription of gene sets via selective and non-covalent binding to a specific double-stranded genomic DNA sequence (sometimes referred to as a motif) within a cis-regulatory region. Regulatory regions include promoters (proximal and distal) and enhancers. Genes are transcriptional units, and include bacterial operons. [GOC:txnOH-2018] |
nuclear receptor activity | molecular function | A DNA-binding transcription factor activity regulated by binding to a ligand that modulates the transcription of specific gene sets transcribed by RNA polymerase II. Nuclear receptor ligands are usually lipid-based (such as a steroid hormone) and the binding of the ligand to its receptor often occurs in the cytosol, which leads to its translocation to the nucleus. [GOC:txnOH-2018, PMID:23457262] |
protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
zinc ion binding | molecular function | Binding to a zinc ion (Zn). [GOC:ai] |
TBP-class protein binding | molecular function | Binding to a member of the class of TATA-binding proteins (TBP), including any of the TBP-related factors (TRFs). [GOC:jl, GOC:txnOH, http://www.mblab.gla.ac.uk/, PMID:16858867] |
protein domain specific binding | molecular function | Binding to a specific domain of a protein. [GOC:go_curators] |
chromatin DNA binding | molecular function | Binding to DNA that is assembled into chromatin. [GOC:mah] |
thyroid hormone binding | molecular function | Binding to thyroxine (T4) or triiodothyronine (T3), tyrosine-based hormones produced by the thyroid gland. [GOC:rph] |
general transcription initiation factor binding | molecular function | Binding to a general transcription initiation factor, a protein that contributes to transcription start site selection and transcription initiation. [GOC:txnOH-2018] |
RNA polymerase II cis-regulatory region sequence-specific DNA binding | molecular function | Binding to a specific upstream regulatory DNA sequence (transcription factor recognition sequence or binding site) located in cis relative to the transcription start site (i.e., on the same strand of DNA) of a gene transcribed by RNA polymerase II. [GOC:txnOH-2018] |
Located In
This protein is located in 3 target(s):
Target | Category | Definition |
nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
cytosol | cellular component | The part of the cytoplasm that does not contain organelles but which does contain other particulate matter, such as protein complexes. [GOC:hjd, GOC:jl] |
Active In
This protein is active in 1 target(s):
Target | Category | Definition |
nucleus | cellular component | A membrane-bounded organelle of eukaryotic cells in which chromosomes are housed and replicated. In most cells, the nucleus contains all of the cell's chromosomes except the organellar chromosomes, and is the site of RNA synthesis and processing. In some species, or in specialized cell types, RNA metabolism or DNA replication may be absent. [GOC:go_curators] |
Part Of
This protein is part of 2 target(s):
Target | Category | Definition |
chromatin | cellular component | The ordered and organized complex of DNA, protein, and sometimes RNA, that forms the chromosome. [GOC:elh, PMID:20404130] |
RNA polymerase II transcription regulator complex | cellular component | A transcription factor complex that acts at a regulatory region of a gene transcribed by RNA polymerase II. [GOC:tb] |
Involved In
This protein is involved in 25 target(s):
Target | Category | Definition |
cartilage condensation | biological process | The condensation of mesenchymal cells that have been committed to differentiate into chondrocytes. [ISBN:0878932437] |
ossification | biological process | The formation of bone or of a bony substance, or the conversion of fibrous tissue or of cartilage into bone or a bony substance. [GOC:mtg_mpo, PMID:17572649] |
regulation of thyroid hormone mediated signaling pathway | biological process | Any process that modulates the frequency, rate or extent of a thyroid hormone mediated signaling pathway. [GOC:hjd] |
regulation of transcription by RNA polymerase II | biological process | Any process that modulates the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH] |
transcription by RNA polymerase II | biological process | The synthesis of RNA from a DNA template by RNA polymerase II (RNAP II), originating at an RNA polymerase II promoter. Includes transcription of messenger RNA (mRNA) and certain small nuclear RNAs (snRNAs). [GOC:jl, GOC:txnOH, ISBN:0321000382] |
learning or memory | biological process | The acquisition and processing of information and/or the storage and retrieval of this information over time. [GOC:jid, PMID:8938125] |
regulation of heart contraction | biological process | Any process that modulates the frequency, rate or extent of heart contraction. Heart contraction is the process in which the heart decreases in volume in a characteristic way to propel blood through the body. [GOC:dph, GOC:go_curators, GOC:tb] |
female courtship behavior | biological process | The behavior of a female, for the purpose of attracting a sexual partner. [GOC:bf, GOC:pr] |
response to cold | biological process | Any process that results in a change in state or activity of a cell or an organism (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a cold stimulus, a temperature stimulus below the optimal temperature for that organism. [GOC:lr] |
hormone-mediated signaling pathway | biological process | The series of molecular signals mediated by the detection of a hormone. [GOC:sm] |
negative regulation of RNA polymerase II transcription preinitiation complex assembly | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of RNA polymerase II transcriptional preinitiation complex assembly. [GOC:go_curators] |
erythrocyte differentiation | biological process | The process in which a myeloid precursor cell acquires specializes features of an erythrocyte. [GOC:mah] |
thyroid gland development | biological process | The process whose specific outcome is the progression of the thyroid gland over time, from its formation to the mature structure. The thyroid gland is an endoderm-derived gland that produces thyroid hormone. [GOC:dgh] |
regulation of myeloid cell apoptotic process | biological process | Any process that modulates the frequency, rate, or extent of myeloid cell apoptotic process. [GOC:add, GOC:mtg_apoptosis] |
negative regulation of DNA-templated transcription | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of cellular DNA-templated transcription. [GOC:go_curators, GOC:txnOH] |
positive regulation of female receptivity | biological process | Any process that activates or increases the receptiveness of a female to male advances. [GOC:go_curators] |
regulation of lipid catabolic process | biological process | Any process that modulates the frequency, rate, or extent of the chemical reactions and pathways resulting in the breakdown of lipids. [GOC:ai] |
type I pneumocyte differentiation | biological process | The process in which a relatively unspecialized cell acquires specialized features of a type I pneumocyte. A type I pneumocyte is a flattened cell with greatly attenuated cytoplasm and a paucity of organelles. [GOC:dph, GOC:mtg_lung, ISBN:0721662544] |
positive regulation of cold-induced thermogenesis | biological process | Any process that activates or increases the frequency, rate or extent of cold-induced thermogenesis. [PMID:27876809] |
negative regulation of DNA-templated transcription initiation | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of DNA-templated transcription initiation. [GOC:mah, GOC:txnOH] |
thyroid hormone mediated signaling pathway | biological process | The series of molecular signals mediated by the detection of a thyroid hormone. [GOC:hjd] |
negative regulation of transcription by RNA polymerase II | biological process | Any process that stops, prevents, or reduces the frequency, rate or extent of transcription mediated by RNA polymerase II. [GOC:go_curators, GOC:txnOH] |
cell differentiation | biological process | The cellular developmental process in which a relatively unspecialized cell, e.g. embryonic or regenerative cell, acquires specialized structural and/or functional features that characterize a specific cell. Differentiation includes the processes involved in commitment of a cell to a specific fate and its subsequent development to the mature state. [ISBN:0198506732] |
positive regulation of transcription by RNA polymerase II | biological process | Any process that activates or increases the frequency, rate or extent of transcription from an RNA polymerase II promoter. [GOC:go_curators, GOC:txnOH] |
retinoic acid receptor signaling pathway | biological process | The series of molecular signals generated as a consequence of a retinoic acid receptor binding to one of its physiological ligands. [GOC:dgh] |