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CYSLTR1 Gene Record

  • Summary
  • Interactions
  • Claims
  • CYSLTR1 10800 Druggable Genome

    Alternate Names:

    10800
    CYSTEINYL LEUKOTRIENE RECEPTOR 1
    CYSLTR1
    CYSLT1
    CYSLT1R
    CYSLTR
    HMTMF81
    300201
    17451
    ENSG00000173198
    OTTHUMG00000021889
    LTD4 receptor
    Cysteinyl leukotriene D4 receptor
    G-protein coupled receptor HG55
    Q9Y271
    HG55
    CLTR1_HUMAN
    269
    NP_006630
    NM_006639
    CysLT<sub>1</sub> receptor
    BE0000705
    CYSTEINYL LEUKOTRIENE RECEPTOR 1 (CYSLTR1) (CYSTEINYL LEUKOTRIENE D4 RECEPTOR) (LTD4 RECEPTOR) (HG55) (HMTMF81). [SOURCE:UNIPROT/SWISSPROT;ACC:Q9Y271]
    PA38453
    Leukotriene CysLT1 receptor
    T71192

    Gene Info:

    Target Class Receptors
    Target Subclass GPCR
    Target Subclass Rhodopsin
    Human Readable Name G PROTEIN COUPLED RECEPTOR
    Transmembrane Helix Count 7
    Target Main Class Receptors
    Interpro Acc IPR000276
    Uniprot Evidence 2: Evidence at transcript level
    Uniprot Status Swiss-Prot
    Interpro Type Family
    Human Readable Name DRUGGABLE GENOME
    Interpro Short Name 7TM_GPCR_Rhodpsn
    Interpro Name GPCR, rhodopsin-like, 7TM
    GuideToPharmacology Gene Category Name Leukotriene receptors
    GuideToPharmacology Gene Category ID 35
    Gene Biotype PROTEIN_CODING
    (9 More Sources)

    Gene Categories: Category Details

    G PROTEIN COUPLED RECEPTOR
    DRUGGABLE GENOME

    Publications:

    O'Byrne, 1997, Leukotrienes in the pathogenesis of asthma., Chest
    Cazzola et al., 2000, Lung function improvement in smokers suffering from COPD with zafirlukast, a CysLT(1)-receptor antagonist., Pulm Pharmacol Ther
    Heise et al., 2000, Characterization of the human cysteinyl leukotriene 2 receptor., J. Biol. Chem.
    Wang et al., 2000, A novel hepatointestinal leukotriene B4 receptor. Cloning and functional characterization., J. Biol. Chem.
    Chen et al., 2002, TTD: Therapeutic Target Database., Nucleic Acids Res.
    Murata et al., 2002, [Zafirlukast (Accolate): a review of its pharmacological and clinical profile]., Nippon Yakurigaku Zasshi
    Zhang et al., 2004, Montelukast modulates lung CysLT(1) receptor expression and eosinophilic inflammation in asthmatic mice., Acta Pharmacol. Sin.
    Langlois et al., 2006, Montelukast regulates eosinophil protease activity through a leukotriene-independent mechanism., J. Allergy Clin. Immunol.
    Nayak, 2004, A review of montelukast in the treatment of asthma and allergic rhinitis., Expert Opin Pharmacother
    Hamacher et al., 2007, Montelukast exerts no acute direct effect on NO synthases., Pulm Pharmacol Ther
    Alfieri et al., 2007, Heterogeneous effect of leucotriene CysLT1 receptor antagonists on antigen-induced motor and inflammatory responses in guinea-pig airways., Auton Autacoid Pharmacol
    Adelroth et al., 1997, Prolonged protection against exercise-induced bronchoconstriction by the leukotriene D4-receptor antagonist cinalukast., J. Allergy Clin. Immunol.
    Foller et al., 2009, Participation of leukotriene C(4) in the regulation of suicidal erythrocyte death., J. Physiol. Pharmacol.
    Ogasawara et al., 2002, Characterization of mouse cysteinyl leukotriene receptors mCysLT1 and mCysLT2: differential pharmacological properties and tissue distribution., J. Biol. Chem.
    Yoo et al., 2001, Clinical effects of pranlukast, an oral leukotriene receptor antagonist, in mild-to-moderate asthma: a 4 week randomized multicentre controlled trial., Respirology
    Ishinaga et al., 2005, Pranlukast inhibits NF-kappaB activation and MUC2 gene expression in cultured human epithelial cells., Pharmacology
    Ding et al., 2006, Cysteinyl leukotriene receptor 1 is involved in N-methyl-D-aspartate-mediated neuronal injury in mice., Acta Pharmacol. Sin.
    Shirasaki et al., 2006, Distribution of specific binding sites for cysteinyl leukotriene 1 receptor antagonist in human nasal mucosa., Acta Otolaryngol.
    Yazid et al., 2010, Antiallergic cromones inhibit neutrophil recruitment onto vascular endothelium via annexin-A1 mobilization., Arterioscler. Thromb. Vasc. Biol.
    Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
    Radeau et al., 1993, Effect of nedocromil sodium on sulfidopeptide leukotrienes-stimulated human alveolar macrophages in asthma., Pulm Pharmacol
    Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
    Monteseirín et al., 2005, L-selectin expression on neutrophils from allergic patients., Clin. Exp. Allergy
    Sarau et al., 1999, Identification, molecular cloning, expression, and characterization of a cysteinyl leukotriene receptor., Mol. Pharmacol.
    Lynch et al., 1999, Characterization of the human cysteinyl leukotriene CysLT1 receptor., Nature
    Bouchelouche K et al., 2003, The cysteinyl-leukotriene D4 induces cytosolic Ca2+ elevation and contraction of the human detrusor muscle., J Urol
  • CINALUKAST   CYSLTR1

    Interaction Score: 8.28

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    9042047 19826192 11752352


    Sources:
    TEND TdgClinicalTrial TTD DrugBank

  • CR-3465   CYSLTR1

    Interaction Score: 7.1

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Cysteinyl leukotriene receptor 1 antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    TTD ChemblInteractions

  • PRANLUKAST   CYSLTR1

    Interaction Score: 6.09

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Details of the Assay for Interaction against [<sup>3</sup>H]LTD<sub>4</sub> in human lung parenchyma
    Specific Action of the Ligand Antagonist
    Endogenous Drug? False

    PMIDs:
    11854273 11264758 15475658 17112405 16864492 11752352


    Sources:
    TEND PharmGKB TdgClinicalTrial TTD DrugBank GuideToPharmacology

  • CHEMBL451509   CYSLTR1

    Interaction Score: 4.73

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10462554 10391245 12853847


    Sources:
    DrugBank

  • LEUKOTRIENE D4   CYSLTR1

    Interaction Score: 4.73

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    10462554 10391245 12853847


    Sources:
    DrugBank

  • NEDOCROMIL   CYSLTR1

    Interaction Score: 4.73

    Interaction Types & Directionality:
    suppressor (inhibitory)

    Interaction Info:
    Trial Name -
    Novel drug target Established target

    PMIDs:
    20558817 17139284 8386571 17016423 16164449


    Sources:
    TEND TdgClinicalTrial DrugBank

  • SULUKAST   CYSLTR1

    Interaction Score: 3.55

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Direct Interaction? False
    Endogenous Drug? False
    Specific Action of the Ligand Antagonist

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • IRALUKAST   CYSLTR1

    Interaction Score: 3.55

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Antagonist
    Details of Interaction against [<sup>3</sup>H]LTD<sub>4</sub> in human lung parenchyma
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    TTD GuideToPharmacology

  • ZAFIRLUKAST   CYSLTR1

    Interaction Score: 2.71

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Details of Interaction against 10nM LTD<sub>4</sub> aequorin-based Ca<sup>2+</sup> assay in CHO cells
    Details of Interaction zafirlukast is only about 100-fold selective for CysLT<sub>1</sub>
    Details of the Assay for Interaction against [<sup>3</sup>H]LTD<sub>4</sub> in human lung parenchyma

    PMIDs:
    9042024 11061985 10851239 11006272 11752352 11979731


    Sources:
    TEND PharmGKB TdgClinicalTrial TTD DrugBank GuideToPharmacology ChemblInteractions

  • MONTELUKAST   CYSLTR1

    Interaction Score: 2.37

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Details of the Assay for Interaction against [<sup>3</sup>H]LTD4 in COS-7 or HEK-293 cells
    Details of Interaction against 33nM LTD<sub>4</sub> Ca<sup>2+</sup> mobilization assay in HEK-293
    Direct Interaction? True

    PMIDs:
    15456537 16815146 15013935 16815057 11752352 17199874


    Sources:
    TEND PharmGKB TdgClinicalTrial TTD DrugBank GuideToPharmacology

  • LY-2300559   CYSLTR1

    Interaction Score: 1.78

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • VERLUKAST   CYSLTR1

    Interaction Score: 1.78

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Details of the Assay for Interaction against [<sup>3</sup>H]LTD<sub>4</sub> in human lung homogenate
    Specific Action of the Ligand Antagonist
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • CHEMBL314115   CYSLTR1

    Interaction Score: 1.78

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    None found


    Sources:
    TTD

  • POBILUKAST   CYSLTR1

    Interaction Score: 1.78

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Specific Action of the Ligand Antagonist
    Details of Interaction against [<sup>3</sup>H]LTD<sub>4</sub> in HEK-293
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • MK-571   CYSLTR1

    Interaction Score: 0.71

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Details of the Assay for Interaction Antagonism of [<sup>3</sup>H]LTD<sub>4</sub> binding in COS-7 cells.
    Specific Action of the Ligand Antagonist
    Endogenous Drug? False

    PMIDs:
    None found


    Sources:
    GuideToPharmacology

  • MONTELUKAST SODIUM   CYSLTR1

    Interaction Score: 0.71

    Interaction Types & Directionality:
    antagonist (inhibitory)

    Interaction Info:
    Mechanism of Interaction Cysteinyl leukotriene receptor 1 antagonist
    Direct Interaction yes

    PMIDs:
    None found


    Sources:
    ChemblInteractions

  • Ensembl: ENSG00000173198

    • Version: 101_38

    Alternate Names:
    CYSLTR1 Ensembl Gene Name

    Gene Info:
    Gene Biotype PROTEIN_CODING

    Publications:

  • RussLampel: ENSG00000173198

    • Version: 26-July-2011

    Alternate Names:
    ENSG00000173198 Ensembl Gene Id
    CYSTEINYL LEUKOTRIENE RECEPTOR 1 (CYSLTR1) (CYSTEINYL LEUKOTRIENE D4 RECEPTOR) (LTD4 RECEPTOR) (HG55) (HMTMF81). [SOURCE:UNIPROT/SWISSPROT;ACC:Q9Y271] Description
    CYSLTR1 Display Id

    Gene Info:
    Human Readable Name DRUGGABLE GENOME

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • TEND: Q9Y271

    • Version: 01-August-2011

    Alternate Names:
    10800 Entrez Gene Id
    CLTR1_HUMAN Uniprot Id
    CYSLTR1 Gene Symbol

    Gene Info:
    Transmembrane Helix Count 7
    Target Main Class Receptors
    Target Subclass GPCR

    Publications:

  • TdgClinicalTrial: Q9Y271

    • Version: January-2014

    Alternate Names:
    CYSLTR1 Gene Symbol

    Gene Info:
    Target Class Receptors
    Target Subclass GPCR
    Target Subclass Rhodopsin

    Publications:

  • HopkinsGroom: Q9Y271

    • Version: 11-September-2012

    Alternate Names:
    ENSG00000173198 Ensembl Gene Id
    Q9Y271 Uniprot Accession
    CLTR1_HUMAN Uniprot Id

    Gene Info:
    Interpro Acc IPR000276
    Uniprot Evidence 2: Evidence at transcript level
    Uniprot Status Swiss-Prot

    Gene Categories:
    G PROTEIN COUPLED RECEPTOR, DRUGGABLE GENOME

    Publications:

  • GuideToPharmacology: 10800

    • Version: 29-September-2020

    Alternate Names:
    17451 HUGO Gene ID
    17451 HUGO Gene Symbol
    cysteinyl leukotriene receptor 1 HUGO Gene Name

    Gene Info:
    GuideToPharmacology Gene Category Name Leukotriene receptors
    GuideToPharmacology Gene Category ID 35

    Gene Categories:
    G PROTEIN COUPLED RECEPTOR

    Publications:

  • DrugBank: BE0000705

    • Version: 5.1.7

    Alternate Names:
    CYSLTR1 DrugBank Gene Name
    Q9Y271 UniProt Accession
    10800 Entrez Gene Id

    Gene Info:

    Publications:
    O'Byrne, 1997, Leukotrienes in the pathogenesis of asthma., Chest
    Cazzola et al., 2000, Lung function improvement in smokers suffering from COPD with zafirlukast, a CysLT(1)-receptor antagonist., Pulm Pharmacol Ther
    Heise et al., 2000, Characterization of the human cysteinyl leukotriene 2 receptor., J. Biol. Chem.

  • NCI: CYSLTR1

    • Version: 14-September-2017

    Alternate Names:

    Gene Info:

    Publications:
    Asakura et al., 2004, Leukotriene D4 stimulates collagen production from myofibroblasts transformed by TGF-beta., J. Allergy Clin. Immunol.

  • ChemblInteractions: CYSLT1

    • Version: chembl_23

    Alternate Names:
    CYSLT1 GENE_SYMBOL
    CYSLTR1 GENE_SYMBOL
    Cysteinyl leukotriene receptor 1 UNIPROT

    Gene Info:

    Publications:

  • HingoraniCasas: ENSG00000173198

    • Version: 31-May-2017

    Alternate Names:
    ENSG00000173198 Gene Symbol
    CYSLTR1 Ensembl Id

    Gene Info:

    Gene Categories:
    DRUGGABLE GENOME

    Publications:

  • PharmGKB: CYSLTR1

    • Version: 18-August-2020

    Alternate Names:
    PA38453 PharmGKB ID

    Gene Info:

    Publications:

  • dGene: CYSLTR1

    • Version: 27-Jun-2013

    Alternate Names:
    10800 Gene ID
    CYSLT1 dGene Synonym
    CYSLT1R dGene Synonym

    Gene Info:

    Gene Categories:
    G PROTEIN COUPLED RECEPTOR

    Publications:

  • TTD: Leukotriene CysLT1 receptor

    • Version: 2020.06.01

    Alternate Names:
    CYSLTR1 TTD Gene Abbreviation
    T71192 TTD Target ID

    Gene Info:

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

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DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21