Proteins > Cysteinyl leukotriene receptor 1
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Cysteinyl leukotriene receptor 1
A cysteinyl leukotriene receptor 1 that is encoded in the genome of human. [PRO:WCB, UniProtKB:Q9Y271]
Synonyms
CysLTR1;
Cysteinyl leukotriene D4 receptor;
LTD4 receptor;
G-protein coupled receptor HG55;
HMTMF81
Research
Bioassay Publications (16)
| Timeframe | Studies on this Protein(%) | All Drugs % |
|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 7 (43.75) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 8 (50.00) | 24.3611 |
| 2020's | 1 (6.25) | 2.80 |
Compounds (28)
Drugs with Inhibition Measurements
Drugs with Activation Measurements
Structural Basis for Developing Multitarget Compounds Acting on Cysteinyl Leukotriene Receptor 1 and G-Protein-Coupled Bile Acid Receptor 1.Journal of medicinal chemistry, , 11-25, Volume: 64, Issue:22, 2021
Opportunities and Challenges for Fatty Acid Mimetics in Drug Discovery.Journal of medicinal chemistry, , 07-13, Volume: 60, Issue:13, 2017
Discovery of Gemilukast (ONO-6950), a Dual CysLT1 and CysLT2 Antagonist As a Therapeutic Agent for Asthma.Journal of medicinal chemistry, , Aug-13, Volume: 58, Issue:15, 2015
Pharmacophore identification, synthesis, and biological evaluation of carboxylated chalcone derivatives as CysLT1 antagonists.Bioorganic & medicinal chemistry, , Aug-01, Volume: 18, Issue:15, 2010
Development of a three-dimensional CysLT1 (LTD4) antagonist model with an incorporated amino acid residue from the receptor.Journal of medicinal chemistry, , Apr-23, Volume: 41, Issue:9, 1998
Structural Basis for Developing Multitarget Compounds Acting on Cysteinyl Leukotriene Receptor 1 and G-Protein-Coupled Bile Acid Receptor 1.Journal of medicinal chemistry, , 11-25, Volume: 64, Issue:22, 2021
Modulators of leukotriene biosynthesis and receptor activation.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996
Structural Basis for Developing Multitarget Compounds Acting on Cysteinyl Leukotriene Receptor 1 and G-Protein-Coupled Bile Acid Receptor 1.Journal of medicinal chemistry, , 11-25, Volume: 64, Issue:22, 2021
Boosting Anti-Inflammatory Potency of Zafirlukast by Designed Polypharmacology.Journal of medicinal chemistry, , 07-12, Volume: 61, Issue:13, 2018
Opportunities and Challenges for Fatty Acid Mimetics in Drug Discovery.Journal of medicinal chemistry, , 07-13, Volume: 60, Issue:13, 2017
Discovery of 3-Substituted 1H-Indole-2-carboxylic Acid Derivatives as a Novel Class of CysLT1 Selective Antagonists.ACS medicinal chemistry letters, , Mar-10, Volume: 7, Issue:3, 2016
Discovery of Gemilukast (ONO-6950), a Dual CysLT1 and CysLT2 Antagonist As a Therapeutic Agent for Asthma.Journal of medicinal chemistry, , Aug-13, Volume: 58, Issue:15, 2015
Modulators of leukotriene biosynthesis and receptor activation.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996
[no title available],
Structural Basis for Developing Multitarget Compounds Acting on Cysteinyl Leukotriene Receptor 1 and G-Protein-Coupled Bile Acid Receptor 1.Journal of medicinal chemistry, , 11-25, Volume: 64, Issue:22, 2021
Cinnamides as selective small-molecule inhibitors of a cellular model of breast cancer stem cells.Bioorganic & medicinal chemistry letters, , Mar-15, Volume: 23, Issue:6, 2013
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: deBioorganic & medicinal chemistry, , Nov-01, Volume: 18, Issue:21, 2010
The role of receptor binding in drug discovery.Journal of natural products, , Volume: 56, Issue:4, 1993
Discovery of Gemilukast (ONO-6950), a Dual CysLT1 and CysLT2 Antagonist As a Therapeutic Agent for Asthma.Journal of medicinal chemistry, , Aug-13, Volume: 58, Issue:15, 2015
Pharmacophore identification, synthesis, and biological evaluation of carboxylated chalcone derivatives as CysLT1 antagonists.Bioorganic & medicinal chemistry, , Aug-01, Volume: 18, Issue:15, 2010
A series of non-quinoline cysLT1 receptor antagonists: SAR study on pyridyl analogs of Singulair.Bioorganic & medicinal chemistry letters, , Mar-03, Volume: 8, Issue:5, 1998
Modulators of leukotriene biosynthesis and receptor activation.Journal of medicinal chemistry, , Jul-05, Volume: 39, Issue:14, 1996
[no title available],
Class III antiarrhythmic activity in vivo by selective blockade of the slowly activating cardiac delayed rectifier potassium current IKs by (R)-2-(2,4-trifluoromethyl)-N-[2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)- 2, 3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]Journal of medicinal chemistry, , Nov-21, Volume: 40, Issue:24, 1997
Class III antiarrhythmic activity in vivo by selective blockade of the slowly activating cardiac delayed rectifier potassium current IKs by (R)-2-(2,4-trifluoromethyl)-N-[2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)- 2, 3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]Journal of medicinal chemistry, , Nov-21, Volume: 40, Issue:24, 1997
Class III antiarrhythmic activity in vivo by selective blockade of the slowly activating cardiac delayed rectifier potassium current IKs by (R)-2-(2,4-trifluoromethyl)-N-[2-oxo-5-phenyl-1-(2,2,2-trifluoroethyl)- 2, 3-dihydro-1H-benzo[e][1,4]diazepin-3-yl]Journal of medicinal chemistry, , Nov-21, Volume: 40, Issue:24, 1997
Opportunities and Challenges for Fatty Acid Mimetics in Drug Discovery.Journal of medicinal chemistry, , 07-13, Volume: 60, Issue:13, 2017
Discovery of 3-Substituted 1H-Indole-2-carboxylic Acid Derivatives as a Novel Class of CysLT1 Selective Antagonists.ACS medicinal chemistry letters, , Mar-10, Volume: 7, Issue:3, 2016
Discovery of 3-Substituted 1H-Indole-2-carboxylic Acid Derivatives as a Novel Class of CysLT1 Selective Antagonists.ACS medicinal chemistry letters, , Mar-10, Volume: 7, Issue:3, 2016
Discovery of Highly Potent Dual CysLT1 and CysLT2 Antagonist.ACS medicinal chemistry letters, , Nov-13, Volume: 5, Issue:11, 2014
Enables
This protein enables 3 target(s):
| Target | Category | Definition |
|---|
| leukotriene receptor activity | molecular function | Combining with a leukotriene to initiate a change in cell activity. Leukotrienes are pharmacologically active substances with a set of three conjugated double bonds; some contain a peptide group based on cysteine. [GOC:ai, ISBN:0198506732] |
| cysteinyl leukotriene receptor activity | molecular function | Combining with a cysteinyl leukotriene to initiate a change in cell activity. Cysteinyl leukotrienes are leukotrienes that contain a peptide group based on cysteine. [GOC:ai, ISBN:0198506732] |
| G protein-coupled peptide receptor activity | molecular function | Combining with a peptide and transmitting the signal across the membrane by activating an associated G-protein; promotes the exchange of GDP for GTP on the alpha subunit of a heterotrimeric G-protein complex. [GOC:dph, GOC:tb] |
Located In
This protein is located in 2 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] |
| membrane | cellular component | A lipid bilayer along with all the proteins and protein complexes embedded in it and attached to it. [GOC:dos, GOC:mah, ISBN:0815316194] |
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 14 target(s):
| Target | Category | Definition |
|---|
| inflammatory response to antigenic stimulus | biological process | An inflammatory response to an antigenic stimulus, which can be include any number of T cell or B cell epitopes. [GOC:add, ISBN:0781735149] |
| calcium ion transport | biological process | The directed movement of calcium (Ca) ions into, out of or within a cell, or between cells, by means of some agent such as a transporter or pore. [GOC:ai] |
| chemotaxis | biological process | The directed movement of a motile cell or organism, or the directed growth of a cell guided by a specific chemical concentration gradient. Movement may be towards a higher concentration (positive chemotaxis) or towards a lower concentration (negative chemotaxis). [ISBN:0198506732] |
| defense response | biological process | Reactions, triggered in response to the presence of a foreign body or the occurrence of an injury, which result in restriction of damage to the organism attacked or prevention/recovery from the infection caused by the attack. [GOC:go_curators] |
| cell surface receptor signaling pathway | biological process | The series of molecular signals initiated by an extracellular ligand binding to a receptor located on the cell surface. The pathway ends with regulation of a downstream cellular process, e.g. transcription. [GOC:signaling] |
| positive regulation of cytosolic calcium ion concentration | biological process | Any process that increases the concentration of calcium ions in the cytosol. [GOC:ai] |
| respiratory gaseous exchange by respiratory system | biological process | The process of gaseous exchange between an organism and its environment. In plants, microorganisms, and many small animals, air or water makes direct contact with the organism's cells or tissue fluids, and the processes of diffusion supply the organism with dioxygen (O2) and remove carbon dioxide (CO2). In larger animals the efficiency of gaseous exchange is improved by specialized respiratory organs, such as lungs and gills, which are ventilated by breathing mechanisms. [ISBN:0198506732] |
| positive regulation of angiogenesis | biological process | Any process that activates or increases angiogenesis. [GOC:go_curators] |
| positive regulation of vasoconstriction | biological process | Any process that activates or increases the frequency, rate or extent of vasoconstriction. [GOC:go_curators] |
| establishment of localization in cell | biological process | Any process, occuring in a cell, that localizes a substance or cellular component. This may occur via movement, tethering or selective degradation. [GOC:ai, GOC:dos, GOC:dph, GOC:tb] |
| positive regulation of glial cell proliferation | biological process | Any process that activates or increases the rate or extent of glial cell proliferation. [GOC:dph, GOC:sl, GOC:tb] |
| leukotriene signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by leukotriene binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process. [GOC:dph, PMID:21771892] |
| cellular response to hypoxia | 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 stimulus indicating lowered oxygen tension. Hypoxia, defined as a decline in O2 levels below normoxic levels of 20.8 - 20.95%, results in metabolic adaptation at both the cellular and organismal level. [GOC:mah] |
| neuropeptide signaling pathway | biological process | A G protein-coupled receptor signaling pathway initiated by a neuropeptide binding to its receptor on the surface of a target cell, and ending with the regulation of a downstream cellular process. [GOC:mah, ISBN:0815316194] |