Page last updated: 2024-08-07 16:10:52
Thromboxane A2 receptor
A thromboxane A2 receptor that is encoded in the genome of human. [PRO:WCB, UniProtKB:P21731]
Synonyms
TXA2-R;
Prostanoid TP receptor
Research
Bioassay Publications (36)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 1 (2.78) | 18.7374 |
| 1990's | 11 (30.56) | 18.2507 |
| 2000's | 16 (44.44) | 29.6817 |
| 2010's | 7 (19.44) | 24.3611 |
| 2020's | 1 (2.78) | 2.80 |
Compounds (33)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Drugs with Other Measurements
| Drug | Taxonomy | Measurement | Average (mM) | Bioassay(s) | Publication(s) |
|---|
| avapro | Homo sapiens (human) | MEC | 0.5000 | 1 | 1 |
| losartan | Homo sapiens (human) | MEC | 0.5000 | 1 | 1 |
| valsartan | Homo sapiens (human) | MEC | 50.0000 | 1 | 1 |
| telmisartan | Homo sapiens (human) | MEC | 5.0000 | 1 | 1 |
Synthesis and structure-activity relationships of novel benzimidazole and imidazo[4,5-b]pyridine acid derivatives as thromboxane A2 receptor antagonists.Journal of medicinal chemistry, , Apr-30, Volume: 36, Issue:9, 1993
Non-prostanoid thromboxane A2 receptor antagonists with a dibenzoxepin ring system. 1.Journal of medicinal chemistry, , Sep-04, Volume: 35, Issue:18, 1992
Synthesis and thromboxane A2 antagonistic activity activity of indane derivatives.Bioorganic & medicinal chemistry letters, , Feb-08, Volume: 9, Issue:3, 1999
Agents combining thromboxane receptor antagonism with thromboxane synthase inhibition: [[[2-(1H-imidazol-1-yl)ethylidene]amino]oxy]alkanoic acids.Journal of medicinal chemistry, , Oct-14, Volume: 37, Issue:21, 1994
Non-prostanoid thromboxane A2 receptor antagonists with a dibenzoxepin ring system. 2.Journal of medicinal chemistry, , Sep-04, Volume: 35, Issue:18, 1992
Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 21, Issue:1, 2011
Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 19, Issue:16, 2009
Isosteric ramatroban analogs: selective and potent CRTH-2 antagonists.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 15, Issue:6, 2005
Minor structural modifications convert the dual TP/CRTH2 antagonist ramatroban into a highly selective and potent CRTH2 antagonist.Journal of medicinal chemistry, , Feb-24, Volume: 48, Issue:4, 2005
Synthesis and biological evaluation of prostaglandin-F alkylphosphinic acid derivatives as bone anabolic agents for the treatment of osteoporosis.Journal of medicinal chemistry, , Nov-22, Volume: 44, Issue:24, 2001
Synthesis and in vitro evaluation of human FP-receptor selective prostaglandin analogues.Bioorganic & medicinal chemistry letters, , Jul-17, Volume: 10, Issue:14, 2000
Design and synthesis of 13,14-dihydro prostaglandin F(1alpha) analogues as potent and selective ligands for the human FP receptor.Journal of medicinal chemistry, , Mar-09, Volume: 43, Issue:5, 2000
Development of dual-acting agents for thromboxane receptor antagonism and thromboxane synthase inhibition. 2. Design, synthesis, and evaluation of a novel series of phenyl oxazole derivatives.Bioorganic & medicinal chemistry letters, , Aug-04, Volume: 8, Issue:15, 1998
Development of dual-acting agents for thromboxane receptor antagonism and thromboxane synthase inhibition. 3. Synthesis and biological activities of oxazolecarboxamide-substituted omega-phenyl-omega-(3-pyridyl)alkenoic acid derivatives and related compounJournal of medicinal chemistry, , Dec-31, Volume: 41, Issue:27, 1998
Synthesis and in vitro evaluation of human FP-receptor selective prostaglandin analogues.Bioorganic & medicinal chemistry letters, , Jul-17, Volume: 10, Issue:14, 2000
Design and synthesis of 13,14-dihydro prostaglandin F(1alpha) analogues as potent and selective ligands for the human FP receptor.Journal of medicinal chemistry, , Mar-09, Volume: 43, Issue:5, 2000
Guanidine derivatives as combined thromboxane A2 receptor antagonists and synthase inhibitors.Journal of medicinal chemistry, , Apr-08, Volume: 42, Issue:7, 1999
Development of dual-acting agents for thromboxane receptor antagonism and thromboxane synthase inhibition. 3. Synthesis and biological activities of oxazolecarboxamide-substituted omega-phenyl-omega-(3-pyridyl)alkenoic acid derivatives and related compounJournal of medicinal chemistry, , Dec-31, Volume: 41, Issue:27, 1998
On the bioisosteric potential of diazines: diazine analogues of the combined thromboxane A2 receptor antagonist and synthetase inhibitor Ridogrel.Journal of medicinal chemistry, , Sep-27, Volume: 39, Issue:20, 1996
6,6-Disubstituted Hex-5-enoic acid derivatives as combined thromboxane A2 receptor antagonists and synthetase inhibitors.Journal of medicinal chemistry, , Jan-07, Volume: 37, Issue:1, 1994
Agents combining thromboxane receptor antagonism with thromboxane synthase inhibition: [[[2-(1H-imidazol-1-yl)ethylidene]amino]oxy]alkanoic acids.Journal of medicinal chemistry, , Oct-14, Volume: 37, Issue:21, 1994
Designed multiple ligands. An emerging drug discovery paradigm.Journal of medicinal chemistry, , Oct-20, Volume: 48, Issue:21, 2005
Guanidine derivatives as combined thromboxane A2 receptor antagonists and synthase inhibitors.Journal of medicinal chemistry, , Apr-08, Volume: 42, Issue:7, 1999
6,6-Disubstituted Hex-5-enoic acid derivatives as combined thromboxane A2 receptor antagonists and synthetase inhibitors.Journal of medicinal chemistry, , Jan-07, Volume: 37, Issue:1, 1994
Update on the development of antagonists of chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2). From lead optimization to clinical proof-of-concept in asthma and allergic rhinitis.Journal of medicinal chemistry, , Apr-12, Volume: 55, Issue:7, 2012
Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 21, Issue:1, 2011
Discovery of diphenylcarbamate derivatives as highly potent and selective IP receptor agonists: orally active prostacyclin mimetics. Part 3.Bioorganic & medicinal chemistry letters, , Jun-15, Volume: 15, Issue:12, 2005
Discovery of diphenyloxazole and Ndelta-Z-ornithine derivatives as highly potent and selective human prostaglandin EP(4) receptor antagonists.Journal of medicinal chemistry, , May-05, Volume: 48, Issue:9, 2005
Metabolism investigation leading to novel drug design: orally active prostacyclin mimetics. Part 4.Bioorganic & medicinal chemistry letters, , Jul-01, Volume: 15, Issue:13, 2005
Azaindoles as potent CRTH2 receptor antagonists.Bioorganic & medicinal chemistry letters, , Jan-15, Volume: 21, Issue:2, 2011
Discovery of MK-7246, a selective CRTH2 antagonist for the treatment of respiratory diseases.Bioorganic & medicinal chemistry letters, , Jan-01, Volume: 21, Issue:1, 2011
Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis.Bioorganic & medicinal chemistry letters, , Aug-15, Volume: 19, Issue:16, 2009
[no title available],
Enables
This protein enables 3 target(s):
| Target | Category | Definition |
|---|
| thromboxane A2 receptor activity | molecular function | Combining with thromboxane A2 (TXA(2)) and transmitting the signal across the membrane to activate an associated G-protein. [GOC:signaling, ISBN:0198506732] |
| guanyl-nucleotide exchange factor activity | molecular function | Stimulates the exchange of GDP to GTP on a signaling GTPase, changing its conformation to its active form. Guanine nucleotide exchange factors (GEFs) act by stimulating the release of guanosine diphosphate (GDP) to allow binding of guanosine triphosphate (GTP), which is more abundant in the cell under normal cellular physiological conditions. [GOC:kd, GOC:mah, PMID:23303910, PMID:27218782] |
| protein binding | molecular function | Binding to a protein. [GOC:go_curators] |
Located In
This protein is located in 3 target(s):
| Target | Category | Definition |
|---|
| acrosomal vesicle | cellular component | A structure in the head of a spermatozoon that contains acid hydrolases, and is concerned with the breakdown of the outer membrane of the ovum during fertilization. It lies just beneath the plasma membrane and is derived from the lysosome. [ISBN:0124325653, ISBN:0198506732] |
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
| nuclear speck | cellular component | A discrete extra-nucleolar subnuclear domain, 20-50 in number, in which splicing factors are seen to be localized by immunofluorescence microscopy. [http://www.cellnucleus.com/] |
Active In
This protein is active in 1 target(s):
| Target | Category | Definition |
|---|
| plasma membrane | cellular component | The membrane surrounding a cell that separates the cell from its external environment. It consists of a phospholipid bilayer and associated proteins. [ISBN:0716731363] |
Involved In
This protein is involved in 17 target(s):
| Target | Category | Definition |
|---|
| smooth muscle contraction | biological process | A process in which force is generated within smooth muscle tissue, resulting in a change in muscle geometry. Force generation involves a chemo-mechanical energy conversion step that is carried out by the actin/myosin complex activity, which generates force through ATP hydrolysis. Smooth muscle differs from striated muscle in the much higher actin/myosin ratio, the absence of conspicuous sarcomeres and the ability to contract to a much smaller fraction of its resting length. [GOC:ef, GOC:jl, GOC:mtg_muscle, ISBN:0198506732] |
| G protein-coupled receptor signaling pathway | biological process | The series of molecular signals initiated by a ligand binding to its receptor, in which the activated receptor promotes the exchange of GDP for GTP on the alpha-subunit of an associated heterotrimeric G-protein complex. The GTP-bound activated alpha-G-protein then dissociates from the beta- and gamma-subunits to further transmit the signal within the cell. The pathway begins with receptor-ligand interaction, and ends with regulation of a downstream cellular process. The pathway can start from the plasma membrane, Golgi or nuclear membrane. [GOC:bf, GOC:mah, PMID:16902576, PMID:24568158, Wikipedia:G_protein-coupled_receptor] |
| response to nutrient | 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 nutrient stimulus. [GOC:go_curators] |
| response to xenobiotic stimulus | 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 stimulus from a xenobiotic, a compound foreign to the organim exposed to it. It may be synthesized by another organism (like ampicilin) or it can be a synthetic chemical. [GOC:jl, GOC:krc] |
| positive regulation of blood coagulation | biological process | Any process that activates or increases the frequency, rate or extent of blood coagulation. [GOC:mah] |
| response to testosterone | 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 testosterone stimulus. [GOC:sl] |
| thromboxane A2 signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by thromboxane A2 binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process, e.g. transcription. [GOC:nhn, PMID:15893915] |
| response to ethanol | 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 an ethanol stimulus. [GOC:go_curators] |
| positive regulation of angiogenesis | biological process | Any process that activates or increases angiogenesis. [GOC:go_curators] |
| positive regulation of smooth muscle contraction | biological process | Any process that activates or increases the frequency, rate or extent of smooth muscle contraction. [GOC:go_curators] |
| cellular response to lipopolysaccharide | biological process | Any process that results in a change in state or activity of a cell (in terms of movement, secretion, enzyme production, gene expression, etc.) as a result of a lipopolysaccharide stimulus; lipopolysaccharide is a major component of the cell wall of gram-negative bacteria. [GOC:mah] |
| negative regulation of cell migration involved in sprouting angiogenesis | biological process | Any process that decreases the frequency, rate or extent of cell migration involved in sprouting angiogenesis. Cell migration involved in sprouting angiogenesis is the orderly movement of endothelial cells into the extracellular matrix in order to form new blood vessels contributing to the process of sprouting angiogenesis. [GOC:BHF, GOC:dph, GOC:rl, GOC:tb] |
| inflammatory response | biological process | The immediate defensive reaction (by vertebrate tissue) to infection or injury caused by chemical or physical agents. The process is characterized by local vasodilation, extravasation of plasma into intercellular spaces and accumulation of white blood cells and macrophages. [GO_REF:0000022, ISBN:0198506732] |
| positive regulation of blood pressure | biological process | Any process in which the force of blood traveling through the circulatory system is increased. [GOC:go_curators, GOC:mtg_cardio] |
| positive regulation of vasoconstriction | biological process | Any process that activates or increases the frequency, rate or extent of vasoconstriction. [GOC:go_curators] |
| positive regulation of cytosolic calcium ion concentration | biological process | Any process that increases the concentration of calcium ions in the cytosol. [GOC:ai] |
| adenylate cyclase-activating G protein-coupled receptor signaling pathway | biological process | A G protein-coupled receptor signaling pathway in which the signal is transmitted via the activation of adenylyl cyclase activity which results in an increase in the intracellular concentration of cyclic AMP (cAMP). This pathway is negatively regulated by phosphodiesterase, which cleaves cAMP and terminates the signaling. [GOC:dph, GOC:mah, GOC:signaling, GOC:tb, ISBN:0815316194] |