Proteins > Thyroid hormone receptor beta
Page last updated: 2024-08-07 15:53:35
Thyroid hormone receptor beta
A thyroid hormone receptor beta that is encoded in the genome of human. [PRO:DNx, UniProtKB:P10828]
Synonyms
Nuclear receptor subfamily 1 group A member 2;
c-erbA-2;
c-erbA-beta
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 | 19 (65.52) | 29.6817 |
2010's | 6 (20.69) | 24.3611 |
2020's | 3 (10.34) | 2.80 |
Compounds (17)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
QSAR study of selective ligands for the thyroid hormone receptor beta.Bioorganic & medicinal chemistry, , Aug-01, Volume: 15, Issue:15, 2007
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
QSAR study of selective ligands for the thyroid hormone receptor beta.Bioorganic & medicinal chemistry, , Aug-01, Volume: 15, Issue:15, 2007
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 (Journal of medicinal chemistry, , 07-28, Volume: 65, Issue:14, 2022
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
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
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
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
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
QSAR study of selective ligands for the thyroid hormone receptor beta.Bioorganic & medicinal chemistry, , Aug-01, Volume: 15, Issue:15, 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
QSAR study of selective ligands for the thyroid hormone receptor beta.Bioorganic & medicinal chemistry, , Aug-01, Volume: 15, Issue:15, 2007
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
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
QSAR study of selective ligands for the thyroid hormone receptor beta.Bioorganic & medicinal chemistry, , Aug-01, Volume: 15, Issue:15, 2007
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
QSAR study of selective ligands for the thyroid hormone receptor beta.Bioorganic & medicinal chemistry, , Aug-01, Volume: 15, Issue:15, 2007
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 |
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] |
transcription coactivator binding | molecular function | Binding to a transcription coactivator, a protein involved in positive regulation of transcription via protein-protein interactions with transcription factors and other proteins that positively regulate transcription. Transcription coactivators do not bind DNA directly, but rather mediate protein-protein interactions between activating transcription factors and the basal transcription machinery. [GOC:krc] |
DNA binding | molecular function | Any molecular function by which a gene product interacts selectively and non-covalently with DNA (deoxyribonucleic acid). [GOC:dph, GOC:jl, GOC:tb, GOC:vw] |
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] |
enzyme binding | molecular function | Binding to an enzyme, a protein with catalytic activity. [GOC:jl] |
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] |
sequence-specific double-stranded DNA binding | molecular function | Binding to double-stranded DNA of a specific nucleotide composition, e.g. GC-rich DNA binding, or with a specific sequence motif or type of DNA, e.g. promotor binding or rDNA binding. [GOC:dos, GOC:sl] |
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 2 target(s):
Target | Category | Definition |
nucleoplasm | cellular component | That part of the nuclear content other than the chromosomes or the nucleolus. [GOC:ma, ISBN:0124325653] |
nuclear body | cellular component | Extra-nucleolar nuclear domains usually visualized by confocal microscopy and fluorescent antibodies to specific proteins. [GOC:ma, PMID:10330182] |
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 |
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] |
chromatin | cellular component | The ordered and organized complex of DNA, protein, and sometimes RNA, that forms the chromosome. [GOC:elh, PMID:20404130] |
Involved In
This protein is involved in 16 target(s):
Target | Category | Definition |
positive regulation of thyroid hormone mediated signaling pathway | biological process | Any process that increases the frequency, rate or extent of thyroid hormone mediated signaling pathway. [GOC:hjd] |
DNA-templated transcription | biological process | The synthesis of an RNA transcript from a DNA template. [GOC:jl, GOC:txnOH] |
sensory perception of sound | biological process | The series of events required for an organism to receive an auditory stimulus, convert it to a molecular signal, and recognize and characterize the signal. Sonic stimuli are detected in the form of vibrations and are processed to form a sound. [GOC:ai] |
negative regulation of female receptivity | biological process | Any process that stops, prevents or reduces the receptiveness of a female to male advances. [GOC:bf, PMID:11092827] |
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] |
mRNA transcription by RNA polymerase II | biological process | The cellular synthesis of messenger RNA (mRNA) from a DNA template by RNA polymerase II, originating at an RNA polymerase II promoter. [GOC:jl, ISBN:0321000382] |
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] |
retinal cone cell development | biological process | Development of a cone cell, one of the sensory cells in the eye that reacts to the presence of light. Cone cells contain the photopigment iodopsin or cyanopsin and are responsible for photopic (daylight) vision. [ISBN:0198506732] |
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] |
cellular response to thyroid hormone stimulus | biological process | A change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a thyroid hormone stimulus. [GOC:sjw, PMID:9916872] |
retinal cone cell apoptotic process | biological process | Any apoptotic process in a retinal cone cell, one of the two photoreceptor cell types of the vertebrate retina. [CL:0000573, GOC:jc] |
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] |
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] |
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] |