Page last updated: 2024-08-07 15:35:19
Transthyretin
A transthyretin that is encoded in the genome of human. [PRO:DNx, UniProtKB:P02766]
Synonyms
ATTR;
Prealbumin;
TBPA
Research
Bioassay Publications (26)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 1 (3.85) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 6 (23.08) | 29.6817 |
| 2010's | 11 (42.31) | 24.3611 |
| 2020's | 8 (30.77) | 2.80 |
Compounds (70)
Drugs with Inhibition Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| bithionol | Homo sapiens (human) | IC50 | 2.7000 | 2 | 2 |
| danthron | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| diflunisal | Homo sapiens (human) | IC50 | 7.1000 | 4 | 4 |
| emodin | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| flufenamic acid | Homo sapiens (human) | IC50 | 2.9000 | 1 | 1 |
| 1,2,5,8-tetrahydroxy anthraquinone | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| triclosan | Homo sapiens (human) | IC50 | 53.5000 | 1 | 1 |
| thyroxine | Homo sapiens (human) | IC50 | 4.9626 | 2 | 3 |
| alizarin | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| purpurin | Homo sapiens (human) | IC50 | 12.0000 | 1 | 1 |
| 1,4-dihydroxyanthraquinone | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| isatin | Homo sapiens (human) | IC50 | 50.0000 | 1 | 1 |
| anthrarufin | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| dextrothyroxine | Homo sapiens (human) | IC50 | 7.1700 | 1 | 1 |
| rhein | Homo sapiens (human) | IC50 | 12.0000 | 1 | 1 |
| aloe emodin | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| chrysophanic acid | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| physcione | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| 2,4,6-triiodophenol | Homo sapiens (human) | IC50 | 3.2000 | 1 | 1 |
| n-methylisatin | Homo sapiens (human) | IC50 | 6.3000 | 1 | 1 |
| diacerein | Homo sapiens (human) | IC50 | 5.4000 | 1 | 1 |
| 18-crown-6 | Homo sapiens (human) | IC50 | 15.0000 | 2 | 2 |
| daunorubicin | Homo sapiens (human) | IC50 | 100.0000 | 1 | 1 |
| triclabendazole | Homo sapiens (human) | IC50 | 3.5000 | 1 | 1 |
| 9,10-anthraquinone 2-carboxylic acid | Homo sapiens (human) | IC50 | 28.0000 | 1 | 1 |
| 3,3',5,5'-tetrachlorobiphenyl-4,4'-diol | Homo sapiens (human) | IC50 | 1.5874 | 1 | 2 |
| glabridin | Homo sapiens (human) | IC50 | 6.4000 | 1 | 1 |
| tolcapone | Homo sapiens (human) | IC50 | 16.6000 | 2 | 2 |
| luteolin | Homo sapiens (human) | IC50 | 6.4000 | 1 | 1 |
| genistein | Homo sapiens (human) | IC50 | 7.8000 | 1 | 1 |
| daidzein | Homo sapiens (human) | IC50 | 16.0000 | 1 | 1 |
| cyclosporine | Homo sapiens (human) | Ki | 0.0026 | 1 | 1 |
| gamma-mangostin | Homo sapiens (human) | IC50 | 10.0000 | 1 | 1 |
| scy-635 | Homo sapiens (human) | Ki | 0.0018 | 1 | 1 |
| tafamidis | Homo sapiens (human) | IC50 | 3.3713 | 7 | 8 |
| nuclear fast red | Homo sapiens (human) | IC50 | 11.0000 | 1 | 1 |
| ucph 101 | Homo sapiens (human) | IC50 | 308.1140 | 1 | 2 |
| idarucizumab | Homo sapiens (human) | IC50 | 0.1600 | 1 | 1 |
Drugs with Activation Measurements
Drugs with Other Measurements
Transthyretin Amyloidogenesis Inhibitors: From Discovery to Current Developments.Journal of medicinal chemistry, , 12-10, Volume: 63, Issue:23, 2020
Enthalpic Forces Correlate with the Selectivity of Transthyretin-Stabilizing Ligands in Human Plasma.Journal of medicinal chemistry, , Aug-27, Volume: 58, Issue:16, 2015
Synthesis, structure, and activity of diclofenac analogues as transthyretin amyloid fibril formation inhibitors.Journal of medicinal chemistry, , Jan-17, Volume: 45, Issue:2, 2002
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.Journal of medicinal chemistry, , 10-14, Volume: 64, Issue:19, 2021
Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis.Bioorganic & medicinal chemistry, , 08-15, Volume: 44, 2021
Transthyretin Amyloidogenesis Inhibitors: From Discovery to Current Developments.Journal of medicinal chemistry, , 12-10, Volume: 63, Issue:23, 2020
[no title available]Journal of medicinal chemistry, , 03-26, Volume: 63, Issue:6, 2020
Crown Ethers as Transthyretin Amyloidogenesis Inhibitors.Journal of medicinal chemistry, , 02-28, Volume: 62, Issue:4, 2019
Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis.Journal of medicinal chemistry, , 09-13, Volume: 61, Issue:17, 2018
Enthalpic Forces Correlate with the Selectivity of Transthyretin-Stabilizing Ligands in Human Plasma.Journal of medicinal chemistry, , Aug-27, Volume: 58, Issue:16, 2015
Crystal structures of human transthyretin complexed with glabridin.Journal of medicinal chemistry, , Feb-13, Volume: 57, Issue:3, 2014
Inhibitory activities of propolis and its promising component, caffeic acid phenethyl ester, against amyloidogenesis of human transthyretin.Journal of medicinal chemistry, , Nov-13, Volume: 57, Issue:21, 2014
Diflunisal analogues stabilize the native state of transthyretin. Potent inhibition of amyloidogenesis.Journal of medicinal chemistry, , Jan-15, Volume: 47, Issue:2, 2004
Transthyretin Amyloidogenesis Inhibitors: From Discovery to Current Developments.Journal of medicinal chemistry, , 12-10, Volume: 63, Issue:23, 2020
Synthesis and evaluation of transthyretin amyloidosis inhibitors containing carborane pharmacophores.Proceedings of the National Academy of Sciences of the United States of America, , Mar-20, Volume: 104, Issue:12, 2007
A novel bis-furan scaffold for transthyretin stabilization and amyloid inhibition.European journal of medicinal chemistry, , Oct-04, Volume: 121, 2016
Isatin derivatives, a novel class of transthyretin fibrillogenesis inhibitors.Bioorganic & medicinal chemistry letters, , Sep-01, Volume: 19, Issue:17, 2009
Structurally specific binding of halogenated biphenyls to thyroxine transport protein.Journal of medicinal chemistry, , Volume: 29, Issue:5, 1986
Transthyretin Amyloidogenesis Inhibitors: From Discovery to Current Developments.Journal of medicinal chemistry, , 12-10, Volume: 63, Issue:23, 2020
Insights on the Interaction between Transthyretin and Aβ in Solution. A Saturation Transfer Difference (STD) NMR Analysis of the Role of Iododiflunisal.Journal of medicinal chemistry, , 07-13, Volume: 60, Issue:13, 2017
[no title available]Journal of medicinal chemistry, , 11-10, Volume: 65, Issue:21, 2022
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.Journal of medicinal chemistry, , 10-14, Volume: 64, Issue:19, 2021
Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis.Journal of medicinal chemistry, , 09-13, Volume: 61, Issue:17, 2018
Enthalpic Forces Correlate with the Selectivity of Transthyretin-Stabilizing Ligands in Human Plasma.Journal of medicinal chemistry, , Aug-27, Volume: 58, Issue:16, 2015
Crystal structures of human transthyretin complexed with glabridin.Journal of medicinal chemistry, , Feb-13, Volume: 57, Issue:3, 2014
Synthesis and biological evaluation of quinolone derivatives as transthyretin amyloidogenesis inhibitors and fluorescence sensors.Bioorganic & medicinal chemistry, , 01-01, Volume: 53, 2022
[no title available]Journal of medicinal chemistry, , 11-10, Volume: 65, Issue:21, 2022
Identification of Transthyretin Tetramer Kinetic Stabilizers That Are Capable of Inhibiting the Retinol-Dependent Retinol Binding Protein 4-Transthyretin Interaction: Potential Novel Therapeutics for Macular Degeneration, Transthyretin Amyloidosis, and ThJournal of medicinal chemistry, , 07-08, Volume: 64, Issue:13, 2021
Repositioning of the Anthelmintic Drugs Bithionol and Triclabendazole as Transthyretin Amyloidogenesis Inhibitors.Journal of medicinal chemistry, , 10-14, Volume: 64, Issue:19, 2021
Inhibitory activities of anthraquinone and xanthone derivatives against transthyretin amyloidogenesis.Bioorganic & medicinal chemistry, , 08-15, Volume: 44, 2021
[no title available]Journal of medicinal chemistry, , 03-26, Volume: 63, Issue:6, 2020
Transthyretin Amyloidogenesis Inhibitors: From Discovery to Current Developments.Journal of medicinal chemistry, , 12-10, Volume: 63, Issue:23, 2020
Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis.Journal of medicinal chemistry, , 09-13, Volume: 61, Issue:17, 2018
Stilbene Boronic Acids Form a Covalent Bond with Human Transthyretin and Inhibit Its Aggregation.Journal of medicinal chemistry, , 09-28, Volume: 60, Issue:18, 2017
Systemic optimization and structural evaluation of quinoline derivatives as transthyretin amyloidogenesis inhibitors.European journal of medicinal chemistry, , Nov-10, Volume: 123, 2016
A novel bis-furan scaffold for transthyretin stabilization and amyloid inhibition.European journal of medicinal chemistry, , Oct-04, Volume: 121, 2016
Enhancing the Safety and Efficacy of PSMA-Based Small-Molecule Drug Conjugates by Linker Stabilization and Conjugation to Transthyretin Binding Ligand.Journal of medicinal chemistry, , 11-24, Volume: 65, Issue:22, 2022
Identification of Transthyretin Tetramer Kinetic Stabilizers That Are Capable of Inhibiting the Retinol-Dependent Retinol Binding Protein 4-Transthyretin Interaction: Potential Novel Therapeutics for Macular Degeneration, Transthyretin Amyloidosis, and ThJournal of medicinal chemistry, , 07-08, Volume: 64, Issue:13, 2021
Enthalpy-Driven Stabilization of Transthyretin by AG10 Mimics a Naturally Occurring Genetic Variant That Protects from Transthyretin Amyloidosis.Journal of medicinal chemistry, , 09-13, Volume: 61, Issue:17, 2018
Enables
This protein enables 4 target(s):
| Target | Category | Definition |
|---|
| hormone activity | molecular function | The action characteristic of a hormone, any substance formed in very small amounts in one specialized organ or group of cells and carried (sometimes in the bloodstream) to another organ or group of cells in the same organism, upon which it has a specific regulatory action. The term was originally applied to agents with a stimulatory physiological action in vertebrate animals (as opposed to a chalone, which has a depressant action). Usage is now extended to regulatory compounds in lower animals and plants, and to synthetic substances having comparable effects; all bind receptors and trigger some biological process. [GOC:dph, GOC:mah, ISBN:0198506732] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
| identical protein binding | molecular function | Binding to an identical protein or proteins. [GOC:jl] |
| thyroid hormone binding | molecular function | Binding to thyroxine (T4) or triiodothyronine (T3), tyrosine-based hormones produced by the thyroid gland. [GOC:rph] |
Located In
This protein is located in 4 target(s):
| Target | Category | Definition |
|---|
| extracellular region | cellular component | The space external to the outermost structure of a cell. For cells without external protective or external encapsulating structures this refers to space outside of the plasma membrane. This term covers the host cell environment outside an intracellular parasite. [GOC:go_curators] |
| extracellular space | cellular component | That part of a multicellular organism outside the cells proper, usually taken to be outside the plasma membranes, and occupied by fluid. [ISBN:0198547684] |
| azurophil granule lumen | cellular component | The volume enclosed by the membrane of an azurophil granule, a primary lysosomal granule found in neutrophil granulocytes that contains a wide range of hydrolytic enzymes and is released into the extracellular fluid. [GOC:bf, PMID:17152095] |
| extracellular exosome | cellular component | A vesicle that is released into the extracellular region by fusion of the limiting endosomal membrane of a multivesicular body with the plasma membrane. Extracellular exosomes, also simply called exosomes, have a diameter of about 40-100 nm. [GOC:BHF, GOC:mah, GOC:vesicles, PMID:15908444, PMID:17641064, PMID:19442504, PMID:19498381, PMID:22418571, PMID:24009894] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| extracellular space | cellular component | That part of a multicellular organism outside the cells proper, usually taken to be outside the plasma membranes, and occupied by fluid. [ISBN:0198547684] |
Involved In
This protein is involved in 2 target(s):
| Target | Category | Definition |
|---|
| signal transduction | biological process | The cellular process in which a signal is conveyed to trigger a change in the activity or state of a cell. Signal transduction begins with reception of a signal (e.g. a ligand binding to a receptor or receptor activation by a stimulus such as light), or for signal transduction in the absence of ligand, signal-withdrawal or the activity of a constitutively active receptor. Signal transduction ends with regulation of a downstream cellular process, e.g. regulation of transcription or regulation of a metabolic process. Signal transduction covers signaling from receptors located on the surface of the cell and signaling via molecules located within the cell. For signaling between cells, signal transduction is restricted to events at and within the receiving cell. [GOC:go_curators, GOC:mtg_signaling_feb11] |
| purine nucleobase metabolic process | biological process | The chemical reactions and pathways involving purine nucleobases, one of the two classes of nitrogen-containing ring compounds found in DNA and RNA, which include adenine and guanine. [GOC:go_curators] |