Gene Symbol: CYSLTR1
Description: cysteinyl leukotriene receptor 1
Alias: CYSLT1, CYSLT1R, CYSLTR, HMTMF81, cysteinyl leukotriene receptor 1, G-protein coupled receptor HG55, LTD4 receptor, cysteinyl leukotriene D4 receptor
Species: human
Products:     CYSLTR1

Top Publications

  1. Duroudier N, Sayers I, Castagna C, Fenech A, Halapi E, Swan C, et al. Functional polymorphism and differential regulation of CYSLTR1 transcription in human airway smooth muscle and monocytes. Cell Biochem Biophys. 2007;47:119-30 pubmed
    ..of this study was to characterize the mechanisms underlying transcriptional regulation of the human cysteinyl leukotriene receptor 1 (hCYSLTR1) gene...
  2. Woszczek G, Chen L, Nagineni S, Kern S, Barb J, Munson P, et al. Leukotriene D(4) induces gene expression in human monocytes through cysteinyl leukotriene type I receptor. J Allergy Clin Immunol. 2008;121:215-221.e1 pubmed
    ..CysLT type 1 receptor (CysLTR(1)) transcript 1 is predominantly expressed in human monocytes, and CysLTs signal through CysLTR(1) in these cells...
  3. Sarau H, Ames R, Chambers J, Ellis C, Elshourbagy N, Foley J, et al. Identification, molecular cloning, expression, and characterization of a cysteinyl leukotriene receptor. Mol Pharmacol. 1999;56:657-63 pubmed
    ..on the molecular cloning, expression, localization, and pharmacological characterization of a CysLT receptor (CysLTR), which was identified by ligand fishing of orphan seven-transmembrane-spanning, G protein-coupled receptors...
  4. Zhu J, Qiu Y, Figueroa D, Bandi V, Galczenski H, Hamada K, et al. Localization and upregulation of cysteinyl leukotriene-1 receptor in asthmatic bronchial mucosa. Am J Respir Cell Mol Biol. 2005;33:531-40 pubmed
  5. Woszczek G, Pawliczak R, Qi H, Nagineni S, Alsaaty S, Logun C, et al. Functional characterization of human cysteinyl leukotriene 1 receptor gene structure. J Immunol. 2005;175:5152-9 pubmed
    ..Thus, cysLTs signaling through cysLT(1)R might contribute to inflammatory reactions by cooperating with IL-4 in enhanced CCL2 production in human monocytic cells. ..
  6. Kim S, Oh J, Kim Y, Palmer L, Suh C, Nahm D, et al. Cysteinyl leukotriene receptor 1 promoter polymorphism is associated with aspirin-intolerant asthma in males. Clin Exp Allergy. 2006;36:433-9 pubmed
    ..characterized by bronchoconstriction, mucus secretion and airway hyper-responsiveness via cysteinyl leukotriene receptor 1 (CysLTR1)-mediated mechanism...
  7. Parhamifar L, Sime W, Yudina Y, Vilhardt F, Morgelin M, Sjölander A. Ligand-induced tyrosine phosphorylation of cysteinyl leukotriene receptor 1 triggers internalization and signaling in intestinal epithelial cells. PLoS ONE. 2010;5:e14439 pubmed publisher
  8. Lynch K, O Neill G, Liu Q, Im D, Sawyer N, Metters K, et al. Characterization of the human cysteinyl leukotriene CysLT1 receptor. Nature. 1999;399:789-93 pubmed
    ..Pharmacological studies have determined that cysteinyl leukotrienes activate at least two receptors, designated CysLT1 and CysLT2...
  9. Mellor E, Maekawa A, Austen K, Boyce J. Cysteinyl leukotriene receptor 1 is also a pyrimidinergic receptor and is expressed by human mast cells. Proc Natl Acad Sci U S A. 2001;98:7964-9 pubmed
    ..We now report that human cord-blood-derived MCs (hMCs) express the CysLT1 receptor, which responds not only to inflammation-derived cys-LTs, but also to a pyrimidinergic ligand, UDP...

More Information

Publications136 found, 100 shown here

  1. Nielsen C, Campbell J, Ohd J, Morgelin M, Riesbeck K, Landberg G, et al. A novel localization of the G-protein-coupled CysLT1 receptor in the nucleus of colorectal adenocarcinoma cells. Cancer Res. 2005;65:732-42 pubmed
    ..The present findings indicate that LTD(4) cannot only be synthesized but also signal proliferation through nuclear CysLT(1) receptors, stressing the importance of leukotrienes in inflammation-induced colon carcinogenesis. ..
  2. Mita H, Hasegawa M, Saito H, Akiyama K. Levels of cysteinyl leukotriene receptor mRNA in human peripheral leucocytes: significantly higher expression of cysteinyl leukotriene receptor 2 mRNA in eosinophils. Clin Exp Allergy. 2001;31:1714-23 pubmed
    ..cDNA sequences of cysteinyl leukotriene receptor 1 (CysLTR1) and cysteinyl leukotriene receptor 2 (CysLTR2) have recently been elucidated...
  3. Ohd J, Nielsen C, Campbell J, Landberg G, Löfberg H, Sjölander A. Expression of the leukotriene D4 receptor CysLT1, COX-2, and other cell survival factors in colorectal adenocarcinomas. Gastroenterology. 2003;124:57-70 pubmed
    ..Based on our present and earlier findings, we propose that LT/CysLT(1)R signaling facilitates survival of colon cancer cells, which may affect disease outcome. Like COX-2, LTs are accessible targets for pharmacologic treatment. ..
  4. Deshpande D, Pascual R, Wang S, Eckman D, Riemer E, Funk C, et al. PKC-dependent regulation of the receptor locus dominates functional consequences of cysteinyl leukotriene type 1 receptor activation. FASEB J. 2007;21:2335-42 pubmed
    ..receptor (GPCR) mediating the leukotriene responses in asthma, cysteinyl leukotriene type 1 receptor (CysLT1R), have not been delineated...
  5. Gronert K, Martinsson Niskanen T, Ravasi S, Chiang N, Serhan C. Selectivity of recombinant human leukotriene D(4), leukotriene B(4), and lipoxin A(4) receptors with aspirin-triggered 15-epi-LXA(4) and regulation of vascular and inflammatory responses. Am J Pathol. 2001;158:3-9 pubmed
  6. Zhang J, Migita O, Koga M, Shibasaki M, Arinami T, Noguchi E. Determination of structure and transcriptional regulation of CYSLTR1 and an association study with asthma and rhinitis. Pediatr Allergy Immunol. 2006;17:242-9 pubmed
    Pharmacologic studies have revealed that cysteinyl leukotrienes (CYSLTs) act through two receptors, cysteinyl leukotriene receptor 1 (CYSLTR1) and CYSLTR2. CYSLTR1 antagonists are widely used to treat asthma and rhinitis...
  7. Hao L, Sayers I, Cakebread J, Barton S, Beghe B, Holgate S, et al. The cysteinyl-leukotriene type 1 receptor polymorphism 927T/C is associated with atopy severity but not with asthma. Clin Exp Allergy. 2006;36:735-41 pubmed
    ..We screened the CYSLTR1 gene on chromosome Xq13-21 for coding region polymorphisms, and investigated their associations with allergy and ..
  8. Thompson C, Cloutier A, Bosse Y, Thivierge M, Gouill C, Larivee P, et al. CysLT1 receptor engagement induces activator protein-1- and NF-kappaB-dependent IL-8 expression. Am J Respir Cell Mol Biol. 2006;35:697-704 pubmed
    ..the potential for leukotriene (LT) D(4) to induce synthesis of the chemokine IL-8 through activation of the CysLT1 receptor...
  9. Klotsman M, York T, Pillai S, Vargas Irwin C, Sharma S, van den Oord E, et al. Pharmacogenetics of the 5-lipoxygenase biosynthetic pathway and variable clinical response to montelukast. Pharmacogenet Genomics. 2007;17:189-96 pubmed
    ..Associations between polymorphisms in 10 candidate genes (ALOX5, ALOX5AP, LTC4S, CYSLTR1, CYSLTR2, PLA2G4A, CYP2C9, CYP3A4, ADRB2, and NR3C1) and response to montelukast were modeled using change in ..
  10. Jiang Y, Borrelli L, Kanaoka Y, Bacskai B, Boyce J. CysLT2 receptors interact with CysLT1 receptors and down-modulate cysteinyl leukotriene dependent mitogenic responses of mast cells. Blood. 2007;110:3263-70 pubmed
    ..Negative regulation of CysLT(1)-induced mitogenic signaling responses of MCs by CysLT(2) demonstrates physiologically relevant functions for GPCR heterodimers on primary cells central to inflammation. ..
  11. Magnusson C, Ehrnstrom R, Olsen J, Sjölander A. An increased expression of cysteinyl leukotriene 2 receptor in colorectal adenocarcinomas correlates with high differentiation. Cancer Res. 2007;67:9190-8 pubmed
    ..These data suggest that the balance between these two receptors is important for tumor progression and disease outcome. ..
  12. Sjostrom M, Jakobsson P, Heimburger M, Palmblad J, Haeggstrom J. Human umbilical vein endothelial cells generate leukotriene C4 via microsomal glutathione S-transferase type 2 and express the CysLT(1) receptor. Eur J Biochem. 2001;268:2578-86 pubmed
    ..Moreover, HUVEC were found to express the CysLT1 receptor in line with a paracrine and autocrine role for cysteinyl-leukotrienes in endothelial cell function.
  13. Naik S, Billington C, Pascual R, Deshpande D, Stefano F, Kohout T, et al. Regulation of cysteinyl leukotriene type 1 receptor internalization and signaling. J Biol Chem. 2005;280:8722-32 pubmed
    Cysteinyl leukotrienes activate the cysteinyl leukotriene type 1 receptor (CysLT1R) to regulate numerous cell functions important in inflammatory processes and diseases such as asthma...
  14. Surmiak M, Kaczor M, Sanak M. Proinflammatory genes expression in granulocytes activated by native proteinase-binding fragments of anti-proteinase 3 IgG. J Physiol Pharmacol. 2015;66:609-15 pubmed
    ..We observed a consistent upregulation of 17 genes (CYSLTR1, HPGD, IL1R1, IL1RL1, MAPK1, MAPK8, NR3C1, PLA2G7, PTGDR, CD302, DNAJB1, F2R, F2RL1, IER3, RAC1, RPL41, PTGER3), ..
  15. Sekioka T, Kadode M, Osakada N, Fujita M, Matsumura N, Yamaura Y, et al. A new CysLT1 and CysLT2 receptors-mediated anaphylaxis guinea pig model. Prostaglandins Leukot Essent Fatty Acids. 2017;119:18-24 pubmed publisher
  16. Agier J, Rozalska S, Wódz K, Brzezińska Błaszczyk E. Leukotriene receptor expression in mast cells is affected by their agonists. Cell Immunol. 2017;317:37-47 pubmed publisher
    The effects of LTs are mediated by GPCRs: cysLTs interact with CYSLTR1, CYSLTR2, or GPR17, and LTB4 acts via BLT1R or BLT2R. Data relating to the presence of these receptors in mature tissue mast cells are not entirely known...
  17. LUKIC A, Wahlund C, Gomez C, Brodin D, Samuelsson B, Wheelock C, et al. Exosomes and cells from lung cancer pleural exudates transform LTC4 to LTD4, promoting cell migration and survival via CysLT1. Cancer Lett. 2019;444:1-8 pubmed publisher
    ..Furthermore, exosomes promoted migration of cancer cells, which was counteracted by the CysLT1 antagonist montelukast...
  18. Duah E, Teegala L, Kondeti V, Adapala R, Keshamouni V, Kanaoka Y, et al. Cysteinyl leukotriene 2 receptor promotes endothelial permeability, tumor angiogenesis, and metastasis. Proc Natl Acad Sci U S A. 2019;116:199-204 pubmed publisher
    ..mice (Cysltr2 -/-) compared with WT and CysLT1R-null mice (Cysltr1 -/-)...
  19. Lei C, Wu S, Wen C, Li Y, Liu N, Huang J, et al. Zafirlukast attenuates advanced glycation end-products (AGEs)-induced degradation of articular extracellular matrix (ECM). Int Immunopharmacol. 2019;68:68-73 pubmed publisher
    ..NOX-4, generation of ROS, and activation of NF-κB via the IκBα/JNK/AP-1 pathway through targeted inhibition of CysLTR1. These findings suggest that zafirlukast possesses a protective effect against AGEs- induced damage and ..
  20. Yaddaden L, Véronneau S, Thompson M, Rola Pleszczynski M, Stankova J. Cellular signalling of cysteinyl leukotriene type 1 receptor variants CysLT₁-G300S and CysLT₁-I206S. Prostaglandins Leukot Essent Fatty Acids. 2016;105:1-8 pubmed publisher
    ..are pro-inflammatory lipid mediators, involved in allergic asthma, that bind the G-protein-coupled receptors CysLT1, CysLT2 and GPR99...
  21. Shirasaki H, Kanaizumi E, Seki N, Himi T. Leukotriene E4 induces MUC5AC release from human airway epithelial NCI-H292 cells. Allergol Int. 2015;64:169-74 pubmed publisher
    ..However, LTE4 has received little attention because it binds poorly to the CysLT1 and CysLT2 receptors; therefore, little is known about the effects of LTE4 on mucous secretion...
  22. Sekioka T, Kadode M, Fujii M, Kawabata K, Abe T, Horiba M, et al. Expression of CysLT2 receptors in asthma lung, and their possible role in bronchoconstriction. Allergol Int. 2015;64:351-8 pubmed publisher
    ..In this study, we evaluated CysLT2 receptors expression, and effects of CysLT2-and CysLT1/2-receptor antagonists on antigen-induced bronchoconstriction using isolated lung tissues from both asthma and non-..
  23. El Sisi A, Sokar S, Salem T, Abu Risha S. Role of cysteinyl leukotriene receptor-1 antagonists in treatment of experimentally induced mammary tumor: does montelukast modulate antitumor and immunosuppressant effects of doxorubicin?. Toxicol Ind Health. 2015;31:1024-36 pubmed publisher
    It has been reported that a leukotriene (LT)-D4 receptor (i.e. cysteinyl LT1 receptor; CysLT1R) has an important role in carcinogenesis...
  24. Lazarinis N, Bood J, Gomez C, Kolmert J, Lantz A, Gyllfors P, et al. Leukotriene E4 induces airflow obstruction and mast cell activation through the cysteinyl leukotriene type 1 receptor. J Allergy Clin Immunol. 2018;: pubmed publisher
    ..LTE4 induces airflow obstruction and mast cell activation through the CysLT1 receptor. ..
  25. Singh R, Tandon R, Dastidar S, Ray A. A review on leukotrienes and their receptors with reference to asthma. J Asthma. 2013;50:922-31 pubmed publisher
    ..CysLTs including LTC4, LTD4 and LTE4 are ligands for CysLT1 and CysLT2 receptors, and LTB4 is the agonist for BLT1 and BLT2 receptors...
  26. Żelechowska P, Agier J, Rozalska S, Wiktorska M, Brzezińska Błaszczyk E. Leptin stimulates tissue rat mast cell pro-inflammatory activity and migratory response. Inflamm Res. 2018;67:789-799 pubmed publisher
    ..Leptin-induced upregulation of CYSLTR1 and CYSLTR2 surface expression was observed...
  27. Choi J, Park H, Oh H, Lee J, Suh Y, Park C, et al. Leukotriene-related gene polymorphisms in ASA-intolerant asthma: an association with a haplotype of 5-lipoxygenase. Hum Genet. 2004;114:337-44 pubmed
    ..nucleotide polymorphisms (SNPs) of the key enzymes involved in arachidonate metabolism, and the cysteinyl leukotriene receptor 1 (CYSLTR1) in a large Korean population with AIA: 93 AIA and 181 ASA-tolerant asthma (ATA) patients, ..
  28. Darmani N, Chebolu S, Zhong W, Kim W, Narlesky M, Adams J, et al. The anti-asthmatic drug pranlukast suppresses the delayed-phase vomiting and reverses intracellular indices of emesis evoked by cisplatin in the least shrew (Cryptotis parva). Eur J Pharmacol. 2017;809:20-31 pubmed publisher
    ..We introduce a new class of antiemetic, the antiasthmatic leukotriene CysLT1 receptor antagonist pranlukast for the suppression of cisplatin-evoked vomiting...
  29. Sørensen B, Thorsteinsdottir U, Lambert I. Acquired cisplatin resistance in human ovarian A2780 cancer cells correlates with shift in taurine homeostasis and ability to volume regulate. Am J Physiol Cell Physiol. 2014;307:C1071-80 pubmed publisher
    ..bromenol lactone, the 5-lipoxygenase (5-LO) inhibitor ETH 615-139, and the cysteine leukotriene receptor 1 (CysLT1) antagonist zafirlukast and impaired by the anion channel blocker DIDS (4,4'-diisothiocyanatostilbene-2,2'-..
    ..We examined if genes encoding CYSLTR1, CYSLTR2, PTGER2 or PTGER4 could explain differential responses to salmeterol versus montelukast using the ..
  31. Boudaud M, Turcotte S, Stankova J, Rola Pleszczynski M. IL-33 Upregulates Cysteinyl Leukotriene Receptor Type 1 Expression in Human Peripheral Blood CD4+ T Lymphocytes. J Immunol. 2018;201:2787-2798 pubmed publisher
    ..In this work, we aimed at studying the regulation of expression of the cysLT receptors CysLT1 and CysLT2 by IL-33 in human PBLs...
  32. York T, Vargas Irwin C, Anderson W, van den Oord E. Asthma pharmacogenetic study using finite mixture models to handle drug-response heterogeneity. Pharmacogenomics. 2009;10:753-67 pubmed publisher
    ..3 and 13.2%, for four markers in the arachidonate 5-lipoxigenase (ALOX5) and cysteinyl leukotriene receptor 1 (CYSLTR1) genes...
  33. Shirasaki H, Kanaizumi E, Watanabe K, Matsui T, Sato J, Narita S, et al. Expression and localization of the cysteinyl leukotriene 1 receptor in human nasal mucosa. Clin Exp Allergy. 2002;32:1007-12 pubmed
    ..Pharmacological studies using CysLTs indicate that two classes of receptors, named CysLT1 and CysLT2 receptor, exist...
  34. Mechiche H, Naline E, Candenas L, Pinto F, Birembault P, Advenier C, et al. Effects of cysteinyl leukotrienes in small human bronchus and antagonist activity of montelukast and its metabolites. Clin Exp Allergy. 2003;33:887-94 pubmed
    ..Montelukast (MK), a specific CysLT1 receptor antagonist, is metabolized in two main hydroxylated metabolites (termed M5 and M6, respectively)...
  35. Cingi C, Muluk N, Ipci K, Åžahin E. Antileukotrienes in upper airway inflammatory diseases. Curr Allergy Asthma Rep. 2015;15:64 pubmed publisher
    ..By competitive binding to the cysteinyl LT1 (CysLT1) receptor, LT receptor antagonist drugs, such as montelukast, zafirlukast, and pranlukast, block the effects of ..
  36. Kar M, Altıntoprak N, Muluk N, Ulusoy S, Bafaqeeh S, Cingi C. Antileukotrienes in adenotonsillar hypertrophy: a review of the literature. Eur Arch Otorhinolaryngol. 2016;273:4111-4117 pubmed publisher
    ..There are several types (e.g., LTA4, LTB4, LTC4, LTD4, and LTE4). By competitive binding to the cysLT1 receptor, LT-receptor antagonist drugs such as montelukast, zafirlukast, and pranlukast block the effects of ..
  37. Zhu L, Maruvada R, Sapirstein A, Peters Golden M, Kim K. Cysteinyl leukotrienes as novel host factors facilitating Cryptococcus neoformans penetration into the brain. Cell Microbiol. 2017;19: pubmed publisher
    ..cPLA2 α) and 5-lipoxygenase (5-LO) and acting via cysteinyl leukotriene type 1 receptor (CysLT1), for penetration of the blood-brain barrier...
  38. Adel S, Kakularam K, Horn T, Reddanna P, Kuhn H, Heydeck D. Leukotriene signaling in the extinct human subspecies Homo denisovan and Homo neanderthalensis. Structural and functional comparison with Homo sapiens. Arch Biochem Biophys. 2015;565:17-24 pubmed publisher
    ..eicosanoid relevant genes (ALOX5, ALOX15, ALOX12, ALOX15B, ALOX12B, ALOXE3, COX1, COX2, LTA4H, LTC4S, ALOX5AP, CYSLTR1, CYSLTR2, BLTR1, BLTR2) from the corresponding databases...
  39. Matsumoto H, Kanemitsu Y, Nagasaki T, Tohda Y, Horiguchi T, Kita H, et al. Staphylococcus aureus enterotoxin sensitization involvement and its association with the CysLTR1 variant in different asthma phenotypes. Ann Allergy Asthma Immunol. 2017;118:197-203 pubmed publisher
    ..SE sensitization in nonatopic and/or late-onset asthma and its association with a polymorphism of the cysteinyl leukotriene receptor 1 gene (CysLTR1), which was examined because CysLT signaling is closely associated with late-onset ..
  40. Osman J, Savari S, Chandrashekar N, Bellamkonda K, Douglas D, Sjölander A. Cysteinyl leukotriene receptor 1 facilitates tumorigenesis in a mouse model of colitis-associated colon cancer. Oncotarget. 2017;8:34773-34786 pubmed publisher
    b>Cysteinyl leukotriene receptor 1 (CysLT1R) has been shown to be up-regulated in the adenocarcinomas of colorectal cancer patients, which is associated with a poor prognosis...
  41. Chistyakov D, Grabeklis S, Goriainov S, Chistyakov V, Sergeeva M, Reiser G. Astrocytes synthesize primary and cyclopentenone prostaglandins that are negative regulators of their proliferation. Biochem Biophys Res Commun. 2018;500:204-210 pubmed publisher
    ..not effective; while GW9662 (PPAR? antagonist) or MK-741 (inhibitor of multidrug resistance protein-1, MRP1, and CysLT1 receptors) amplified the inhibitory effect of PGA2 and 15d-PGJ2...
  42. Kim S, Ye Y, Hur G, Lee S, Sampson A, Lee H, et al. CysLTR1 promoter polymorphism and requirement for leukotriene receptor antagonist in aspirin-intolerant asthma patients. Pharmacogenomics. 2007;8:1143-50 pubmed
    ..associations between the clinical requirement for LTRA and genetic polymorphisms of the ALOX5, LTC4S, COX-2, CysLTR1 and TBXA2R genes in the arachidonic acid cascade in the long-term management of 89 AIA patients from a Korean ..
  43. Araújo A, Tang X, Haeggstrom J. Targeting cysteinyl-leukotrienes in abdominal aortic aneurysm. Prostaglandins Other Lipid Mediat. 2018;139:24-28 pubmed publisher
    ..Drugs antagonizing the CysLT1 receptor, termed lukasts and typified by montelukast, are established therapeutics for clinical management of ..
  44. Storch U, Blodow S, Gudermann T, Mederos y Schnitzler M. Cysteinyl leukotriene 1 receptors as novel mechanosensors mediating myogenic tone together with angiotensin II type 1 receptors-brief report. Arterioscler Thromb Vasc Biol. 2015;35:121-6 pubmed publisher
    ..Moreover, our findings suggest that myogenic tone is determined by AT1 and CysLT1 receptors acting together as mechanosensors via Gq/11-protein activation.
  45. Saad M, Abdelsalam R, Kenawy S, Attia A. Montelukast, a cysteinyl leukotriene receptor-1 antagonist protects against hippocampal injury induced by transient global cerebral ischemia and reperfusion in rats. Neurochem Res. 2015;40:139-50 pubmed publisher
    ..Therefore it seemed interesting to study the possible neuroprotective effect of Montelukast, a CysLTR1 antagonist in global cerebral ischemia/reperfusion (IR) injury in rats...
  46. Mansour R, Ahmed M, El Sahar A, El Sayed N. Montelukast attenuates rotenone-induced microglial activation/p38 MAPK expression in rats: Possible role of its antioxidant, anti-inflammatory and antiapoptotic effects. Toxicol Appl Pharmacol. 2018;358:76-85 pubmed publisher
    Montelukast (MK),a cysteinyl leukotriene (CysLT1) receptor antagonist, latterly exhibited a remarkable neuroprotective activity in various neurodegenerative disorders...
  47. Lima J, Zhang S, Grant A, Shao L, Tantisira K, Allayee H, et al. Influence of leukotriene pathway polymorphisms on response to montelukast in asthma. Am J Respir Crit Care Med. 2006;173:379-85 pubmed
    ..Twenty-eight SNPs in the ALOX5, LTA4H, LTC4S, MRP1, and cysLT1R genes, and an ALOX5 repeat polymorphism were successfully typed...
  48. Fleck J, Marafiga J, Jesse A, Ribeiro L, Rambo L, Mello C. Montelukast potentiates the anticonvulsant effect of phenobarbital in mice: an isobolographic analysis. Pharmacol Res. 2015;94:34-41 pubmed publisher
    ..leukotrienes have been implicated in seizures, no study has systematically investigated whether the blockade of CysLT1 receptors synergistically increases the anticonvulsant action of classic antiepileptics...
  49. Capra V, Carnini C, Accomazzo M, Di Gennaro A, Fiumicelli M, Borroni E, et al. Autocrine activity of cysteinyl leukotrienes in human vascular endothelial cells: Signaling through the CysLTâ‚‚ receptor. Prostaglandins Other Lipid Mediat. 2015;120:115-25 pubmed publisher
    ..We also demonstrate here that the CysLT1R antagonist zafirlukast, pranlukast, pobilukast and iralukast also possess CysLT2R antagonistic activity, which ..
  50. Scott J, Peters Golden M. Antileukotriene agents for the treatment of lung disease. Am J Respir Crit Care Med. 2013;188:538-44 pubmed publisher
    ..are so central to asthma pathophysiology are mediated to a significant extent by ligation of the cysLT receptor 1 (CysLT1)...
  51. Doherty T, Khorram N, Lund S, Mehta A, Croft M, Broide D. Lung type 2 innate lymphoid cells express cysteinyl leukotriene receptor 1, which regulates TH2 cytokine production. J Allergy Clin Immunol. 2013;132:205-13 pubmed publisher
    Cysteinyl leukotrienes (CysLTs) contribute to asthma pathogenesis, in part through cysteinyl leukotriene receptor 1 (CysLT1R). Recently discovered lineage-negative type 2 innate lymphoid cells (ILC2s) potently produce IL-5 and IL-13...
  52. Magi S, Takemoto Y, Kobayashi H, Kasamatsu M, Akita T, Tanaka A, et al. 5-Lipoxygenase and cysteinyl leukotriene receptor 1 regulate epidermal growth factor-induced cell migration through Tiam1 upregulation and Rac1 activation. Cancer Sci. 2014;105:290-6 pubmed publisher
    ..these effects caused by LTC4 were found to be blocked in the presence of the antagonist of cysteinyl leukotriene receptor 1 (CysLT1)...
  53. Shi Q, Wang H, Liu Z, Fang S, Song X, Lu Y, et al. HAMI 3379, a CysLT2R antagonist, dose- and time-dependently attenuates brain injury and inhibits microglial inflammation after focal cerebral ischemia in rats. Neuroscience. 2015;291:53-69 pubmed publisher
    Cysteinyl leukotrienes (CysLTs) induce inflammatory responses by activating their receptors, CysLT1R and CysLT2R...
  54. Simon K, Merten N, Schröder R, Hennen S, Preis P, Schmitt N, et al. The Orphan Receptor GPR17 Is Unresponsive to Uracil Nucleotides and Cysteinyl Leukotrienes. Mol Pharmacol. 2017;91:518-532 pubmed publisher
    ..both ligand classes, nor with exogenous transfection of partner receptors (nucleotide P2Y12, cysteinyl-leukotriene CysLT1) to reconstitute the elusive pharmacology...
  55. Guo R, Jiang J, Jing Z, Chen Y, Shi Z, Deng B. Cysteinyl leukotriene receptor 1 regulates glucose-stimulated insulin secretion (GSIS). Cell Signal. 2018;46:129-134 pubmed publisher
    ..b>Cysteinyl leukotriene receptor 1 (cysLT1R) is an important G protein-coupled receptor mediating the biological functions of cysteinyl ..
  56. Dong H, Liu F, Ma F, Xu L, Pang L, Li X, et al. Montelukast inhibits inflammatory response in rheumatoid arthritis fibroblast-like synoviocytes. Int Immunopharmacol. 2018;61:215-221 pubmed publisher
    ..Whether montelukast can protect against the inflammatory milieu of RA remains unclear. Here, it is shown that cysLT1R is present in FLSs and unregulated in RA-FLSs...
  57. Hu C, Yang J, He Q, Luo Y, Chen Z, Yang L, et al. CysLTR1 Blockage Ameliorates Liver Injury Caused by Aluminum-Overload via PI3K/AKT/mTOR-Mediated Autophagy Activation in Vivo and in Vitro. Mol Pharm. 2018;15:1996-2006 pubmed publisher
    ..We demonstrated that Al-overload significantly increased the protein expression levels of CysLTR1, PI3K, AKT, mTOR, and p62, while significantly decreasing the LC3BII protein levels in rat liver; thus, ..
  58. Tufvesson E, Nihlberg K, Westergren Thorsson G, Bjermer L. Leukotriene receptors are differently expressed in fibroblast from peripheral versus central airways in asthmatics and healthy controls. Prostaglandins Leukot Essent Fatty Acids. 2011;85:67-73 pubmed publisher
    ..Leukotriene receptors are differently expressed in fibroblasts from peripheral compared to central airways, which may explain a suggested cysteinyl-leukotriene driven remodeling mainly in the peripheral airways. ..
  59. Savari S, Chandrashekar N, Osman J, Douglas D, Bellamkonda K, Jönsson G, et al. Cysteinyl leukotriene 1 receptor influences intestinal polyp incidence in a gender-specific manner in the ApcMin/+ mouse model. Carcinogenesis. 2016;37:491-9 pubmed publisher
    ..Increased expression of both the cysteinyl leukotriene receptor 1 (CysLTR1) and the enzyme responsible for the production of leukotrienes, 5-lipoxygenase, is ..
  60. Najar M, Fayyad Kazan M, Raicevic G, Fayyad Kazan H, Meuleman N, Bron D, et al. Advanced Glycation End-Products-, C-Type Lectin- and Cysteinyl/ Leukotriene-Receptors in Distinct Mesenchymal Stromal Cell Populations: Differential Transcriptional Profiles in Response to Inflammation. Cell J. 2018;20:250-258 pubmed publisher
    ..and MINCLE), leukotriene B4 (LTB4) receptors (BLT1 and BLT2) and cysteinyl leukotrienes (CysLTs) receptors (CYSLTR1 and CYSLTR2) in distinct populations of MSCs grown under basic or inflammatory conditions...
  61. Csandl M, Conseil G, Cole S. Cysteinyl Leukotriene Receptor 1/2 Antagonists Nonselectively Modulate Organic Anion Transport by Multidrug Resistance Proteins (MRP1-4). Drug Metab Dispos. 2016;44:857-66 pubmed publisher
    ..The cysteinyl leukotriene receptor 1 (CysLT1R) antagonist MK-571 inhibits all four MRP homologs, but little is known about the modulatory ..
  62. Han H, Xue Franzén Y, Miao X, Nagy E, Li N, Xu D, et al. Early growth response gene (EGR)-1 regulates leukotriene D4-induced cytokine transcription in Hodgkin lymphoma cells. Prostaglandins Other Lipid Mediat. 2015;121:122-30 pubmed publisher
    ..The effect of LTD4 on the expression of transcription factors and cytokines were also blocked by the specific CysLT1 receptor antagonist zafirlukast...
  63. Song W, Zhang Y, Wang J, Ma T, Hao L, Wang K. Antagonism of cysteinyl leukotriene receptor 1 (cysLTR1) by montelukast suppresses cell senescence of chondrocytes. Cytokine. 2018;103:83-89 pubmed publisher
    ..In the current study, we found that cysLTR1 but not cysLTR2 is expressed in human primary chondrocytes...
  64. Di Gennaro A, Araújo A, Busch A, Jin H, Wågsäter D, Vorkapic E, et al. Cysteinyl leukotriene receptor 1 antagonism prevents experimental abdominal aortic aneurysm. Proc Natl Acad Sci U S A. 2018;115:1907-1912 pubmed publisher
    ..Here we show that antagonism of the CysLT1 receptor by montelukast, an established antiasthma drug, protects against a strong aorta dilatation (>50% ..
  65. Ballerini P, Di Iorio P, Ciccarelli R, Caciagli F, Poli A, Beraudi A, et al. P2Y1 and cysteinyl leukotriene receptors mediate purine and cysteinyl leukotriene co-release in primary cultures of rat microglia. Int J Immunopathol Pharmacol. 2005;18:255-68 pubmed
    ..RT-PCR analysis showed that microglia expressed both CysLT1 / CysLT2 receptors, P2Y1ATP receptors and several members of the ATP binding cassette (ABC) transporters including ..
  66. Paulucci B, Pereira J, Picciarelli P, Levy D, Di Francesco R. Expression of cysteinyl leukotriene receptor 1 and 2 (CysLTR1 and CysLTR2) in the lymphocytes of hyperplastic tonsils: comparison between allergic and nonallergic snoring children. Int Forum Allergy Rhinol. 2016;6:1151-1158 pubmed publisher
    b>Cysteinyl leukotriene receptor 1 and 2 (CysLTR1 and CysLTR2) are involved in allergic processes and play a role in adenotonsillar hyperplasia (AH). Clinically, only CysLTR1 may be blocked by montelukast...
  67. Zamani M, Prabhakaran M, Varshosaz J, Mhaisalkar P, Ramakrishna S. Electrosprayed Montelukast/poly (lactic-co-glycolic acid) particle based coating: A new therapeutic approach towards the prevention of in-stent restenosis. Acta Biomater. 2016;42:316-328 pubmed publisher
    ..Montelukast (MK) is a selective cysLT1 receptor antagonist, with anti-inflammatory and anti-proliferative properties, which has been used for treatment ..
  68. Dolinska M, Piccini A, Wong W, Gelali E, Johansson A, Klang J, et al. Leukotriene signaling via ALOX5 and cysteinyl leukotriene receptor 1 is dispensable for in vitro growth of CD34+CD38- stem and progenitor cells in chronic myeloid leukemia. Biochem Biophys Res Commun. 2017;490:378-384 pubmed publisher
    ..leukemic BCR-ABL+CD34+CD38- cells expressed cysteinyl leukotriene receptors CYSLT1 and CYSLT2...
  69. Drost A, Seitz G, Boehmler A, Funk M, Norz K, Zipfel A, et al. The G protein-coupled receptor CysLT1 mediates chemokine-like effects and prolongs survival in chronic lymphocytic leukemia. Leuk Lymphoma. 2012;53:665-73 pubmed publisher
    ..The function of the GPCRs cysteinyl leukotriene receptor 1 (CysLT1) and CysLT2 remains elusive...
  70. Kondeti V, Al Azzam N, Duah E, Thodeti C, Boyce J, Paruchuri S. Leukotriene D4 and prostaglandin E2 signals synergize and potentiate vascular inflammation in a mast cell-dependent manner through cysteinyl leukotriene receptor 1 and E-prostanoid receptor 3. J Allergy Clin Immunol. 2016;137:289-298 pubmed publisher
    ..Furthermore, LTD4 plus PGE2, through cysteinyl leukotriene receptor 1 (CysLT1R) and E-prostanoid receptor (EP) 3, enhanced extracellular signal-regulated kinase (Erk) and ..
  71. Singh P, Sharma B. Reversal in Cognition Impairments, Cholinergic Dysfunction, and Cerebral Oxidative Stress Through the Modulation of Ryanodine Receptors (RyRs) and Cysteinyl Leukotriene-1 (CysLT1) Receptors. Curr Neurovasc Res. 2016;13:10-21 pubmed
    ..of this study is to examine the role of ruthenium red; a selective RyR blocker as well as montelukast; a specific CysLT1 antagonist in CCH induced VaD in mice...
  72. Reynolds A, Alvarez Y, Sasore T, Waghorne N, Butler C, Kilty C, et al. Phenotype-based Discovery of 2-[(E)-2-(Quinolin-2-yl)vinyl]phenol as a Novel Regulator of Ocular Angiogenesis. J Biol Chem. 2016;291:7242-55 pubmed publisher
    ..that quininib does not directly target VEGF receptors but antagonizes cysteinyl leukotriene receptors 1 and 2 (CysLT1-2) at micromolar IC50values...
  73. Chen F, Ghosh A, Wu F, Tang S, Hu M, Sun H, et al. Preventive effect of genetic knockdown and pharmacological blockade of CysLT1R on lipopolysaccharide (LPS)-induced memory deficit and neurotoxicity in vivo. Brain Behav Immun. 2017;60:255-269 pubmed publisher
  74. Cheung D, Sigua J, Simpson P, Yan K, Hussain S, Santoro J, et al. Cysteinyl leukotriene receptor 1 expression identifies a subset of neutrophils during the antiviral response that contributes to postviral atopic airway disease. J Allergy Clin Immunol. 2018;142:1206-1217.e5 pubmed publisher
    ..001). In mice CD49d+ PMNs represented a "proatopic" neutrophil subset that expressed cysteinyl leukotriene receptor 1 (CysLTR1) and produced TNF, CCL2, and CCL5...
  75. Liu T, Barrett N, Kanaoka Y, Yoshimoto E, Garofalo D, Cirka H, et al. Type 2 Cysteinyl Leukotriene Receptors Drive IL-33-Dependent Type 2 Immunopathology and Aspirin Sensitivity. J Immunol. 2018;200:915-927 pubmed publisher
    ..Deletion of Cysltr1 blunted LTC4-induced ILC2 expansion and eosinophilia but did not alter IL-33 induction...
  76. Matsuyama M, Hayama T, Funao K, Kawahito Y, Sano H, Takemoto Y, et al. Overexpression of cysteinyl LT1 receptor in prostate cancer and CysLT1R antagonist inhibits prostate cancer cell growth through apoptosis. Oncol Rep. 2007;18:99-104 pubmed
    ..We investigated LTD4 receptor (cysteinyl LT1 receptor: CysLT1R) expression in prostate cancer (PC), as well as the effects of CysLT1R ..
  77. Thompson M, Capra V, Takasaki J, Maresca G, Rovati G, Slutsky A, et al. A functional G300S variant of the cysteinyl leukotriene 1 receptor is associated with atopy in a Tristan da Cunha isolate. Pharmacogenet Genomics. 2007;17:539-49 pubmed
    ..Moreover, the product of cysteinyl-leukotriene 1 receptor gene (CysLT1), located at Xq13.2, is targeted by LT receptor antagonists...
  78. Yonetomi Y, Sekioka T, Kadode M, Kitamine T, Kamiya A, Inoue A, et al. Effects of ONO-6950, a novel dual cysteinyl leukotriene 1 and 2 receptors antagonist, in a guinea pig model of asthma. Eur J Pharmacol. 2015;765:242-8 pubmed publisher
    We assessed in this study the anti-asthmatic effects of ONO-6950, a novel cysteinyl leukotriene 1 (CysLT1) and 2 (CysLT2) receptors dual antagonist, in normal and S-hexyl glutathione (S-hexyl GSH)-treated guinea pigs, and compared these ..
  79. Paulucci B, Pereira J, Picciarelli P, Levy D, Di Francesco R. Expression of CysLTR1 and 2 in Maturating Lymphocytes of Hyperplasic Tonsils Compared to Peripheral Cells in Children. Inflammation. 2016;39:1216-24 pubmed publisher
    Cysteinyl-leukotriene receptors 1 and 2 (CysLTR1 and 2) are related to allergic inflammatory responses. Recent studies demonstrated their role in lymphocyte division and maturation in the bone marrow...
  80. McGovern T, Goldberger M, Chen M, Allard B, Hamamoto Y, Kanaoka Y, et al. CysLT1 Receptor Is Protective against Oxidative Stress in a Model of Irritant-Induced Asthma. J Immunol. 2016;197:266-77 pubmed publisher
    ..leukotrienes (cysLTs) in allergic asthma mediate their effects predominantly through the cysLT1 receptor (cysLT1R). However, the role of cysLTs and cysLT1R in innate immune-triggered asthma is largely unexplored...
  81. Nielsen C, Ohd J, Wikström K, Massoumi R, Paruchuri S, Juhas M, et al. The leukotriene receptor CysLT1 and 5-lipoxygenase are upregulated in colon cancer. Adv Exp Med Biol. 2003;525:201-4 pubmed
  82. Cabral M, Martín Venegas R, Moreno J. Leukotriene D4-induced Caco-2 cell proliferation is mediated by prostaglandin E2 synthesis. Physiol Rep. 2015;3: pubmed publisher
    ..Colon tumors generally have an increased expression of CysLT1R and colon cancer patients with high expression levels of CysLT1R have poor prognosis...
  83. Yu X, Dong R, Wang H, Lin J, An Y, Du Y, et al. Knockdown of hippocampal cysteinyl leukotriene receptor 1 prevents depressive behavior and neuroinflammation induced by chronic mild stress in mice. Psychopharmacology (Berl). 2016;233:1739-49 pubmed publisher associated with depression-like symptoms and neuropsychological disturbances, and cysteinyl leukotriene receptor 1 (CysLT1R) was reported to be involved in neuroinflammation...
  84. Huang J, Wu B, Song J, Wu J. Mechanisms of hyperventilation-induced lung injuries in neonatal rats. Minerva Pediatr. 2016;: pubmed
    ..changes in lung tissues were observed, and the levels of interleukin-6 (IL-6), cysteinyl leukotriene mRNA (CysLT1 mRNA), and nuclear factor-?B mRNA (NF-?Bp65 mRNA) in lung tissues were analyzed...
  85. Vinnakota K, Zhang Y, Selvanesan B, Topi G, Salim T, Sand Dejmek J, et al. M2-like macrophages induce colon cancer cell invasion via matrix metalloproteinases. J Cell Physiol. 2017;232:3468-3480 pubmed publisher
    ..MMP-9 expression and activity were reduced by a TNF? blocking antibody adalimumab and a cysteinyl leukotriene receptor 1 (CysLTR1, the receptor for LTD4 ) antagonist montelukast...
  86. Mehdawi L, Osman J, Topi G, Sjölander A. High tumor mast cell density is associated with longer survival of colon cancer patients. Acta Oncol. 2016;55:1434-1442 pubmed
    ..Previous studies have shown that CRC patients with increased expression of cysteinyl leukotriene receptor 1 (CysLTR1) have a poorer prognosis, and Cysltr1-/- mice display fewer intestinal polyps...
  87. Lund S, Portillo A, Cavagnero K, Baum R, Naji L, Badrani J, et al. Leukotriene C4 Potentiates IL-33-Induced Group 2 Innate Lymphoid Cell Activation and Lung Inflammation. J Immunol. 2017;199:1096-1104 pubmed publisher
    ..Levels of CysLT1R, CysLT2R, and candidate leukotriene E4 receptor P2Y12 mRNAs were increased in ILC2s...
  88. Chibana K, Ishii Y, Asakura T, Fukuda T. Up-regulation of cysteinyl leukotriene 1 receptor by IL-13 enables human lung fibroblasts to respond to leukotriene C4 and produce eotaxin. J Immunol. 2003;170:4290-5 pubmed
    ..To examine the mechanism(s) involved, the expression of CysLT1R in HFL-1 was investigated by quantitative real-time PCR and flow cytometry...
  89. Sanz C, Isidro García M, Davila I, Moreno E, Laffond E, Lorente F. Analysis of 927T> C CYSLTRI and -444A > C LTC4S polymorphisms in patients with asthma. J Investig Allergol Clin Immunol. 2006;16:331-7 pubmed
    ..Cys-LTs exert their biological action by binding two types of G-protein-coupled seven transmembrane receptors, CYSLTR1 and CYSLTR2...
  90. Arriba Mendez S, Sanz C, Isidoro Garcia M, Pascual M, Avila C, Davila I, et al. Analysis of 927T > C CYSLTR1 and -444A > C LTC4S polymorphisms in children with asthma. Allergol Immunopathol (Madr). 2008;36:259-63 pubmed
    ..In this study, polymorphisms 927T > C CYSLTR1 and -444A > C LTC4S were analysed in a Spanish population of 188 individuals (109 asthmatic children and 79 ..
  91. Peng J, Zhou H, Kuang G, Xie L, Tian T, Liu R. The selective cysteinyl leukotriene receptor 1 (CysLT1R) antagonist montelukast regulates extracellular matrix remodeling. Biochem Biophys Res Commun. 2017;484:474-479 pubmed publisher
    ..Montelukast, a potent and specific cysteinyl leukotriene receptor 1 (cysLT1R) antagonist, is a licensed drug clinically used for the treatment of bronchial asthma...
  92. Wei J, Chen S, Huang C, Guo W, Yang S, Feng B, et al. Antagonism of cysteinyl leukot-riene receptor 1 (cysLT1R) by montelukast regulates differentiation of MC3T3-E1 cells under overloaded mechanical environment. Biochem Biophys Res Commun. 2018;495:995-1001 pubmed publisher
    ..Montelukast is a selective cysteinyl leukot-riene receptor 1 (cysLT1R) antagonist, which has been used for the treatment of bronchial asthma in clinics...