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CysLT2 receptor

Family: Leukotriene receptors

Contents:
Gene and Protein Information
Previous and Unofficial Names
Database Links
Agonists
Functional Assays
Physiological Functions
Phenotypes, Alleles and Disease Models
General Comments
References
Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 346 13q14.12-q21.1 CYSLTR2 cysteinyl leukotriene receptor 2
Mouse 7 309 14 D2 Cysltr2 cysteinyl leukotriene receptor 2
Rat 7 309 15p11 Cysltr2 cysteinyl leukotriene receptor 2
Previous and Unofficial Names
LTC4
HPN321
LTC4
CysLT(2)
CYSLT2R
Cyslt2
RSBPT32
cysteinyl leukotriene CysLT2 receptor
cysteinyl leukotriene receptor 2
2300001H05Rik
Database Links
ChEMBL Target 10015 (Hs)
DrugBank Target 111 (Hs)
Ensembl ENSG00000152207 (Hs), ENSMUSG00000033470 (Mm), ENSRNOG00000015042 (Rn)
Entrez Gene 57105 (Hs), 70086 (Mm), 170926 (Rn)
GeneCards CYSLTR2 (Hs)
GenitoUrinary Development Molecular Anatomy Project Cysltr2 (Mm)
HomoloGene 10688 (Hs)
Human Protein Reference Database 09293 (Hs)
InterPro Q9NS75 (Hs), Q920A1 (Mm), Q924T9 (Rn)
KEGG Gene hsa:57105 (Hs), mmu:70086 (Mm), rno:170926 (Rn)
OMIM 605666 (Hs)
PharmGKB Gene PA38518 (Hs)
Protein Ontology (PRO) PRO:000001219 (Hs)
RefSeq Nucleotide NM_020377 (Hs), NM_133720 (Mm), NM_133413 (Rn)
RefSeq Protein NP_065110 (Hs), NP_598481 (Mm), NP_596904 (Rn)
TreeFam ENSG00000152207 (Hs), ENSMUSG00000033470 (Mm), ENSRNOG00000015042 (Rn)
UniGene Hs. 253706 (Hs)
UniProt Q9NS75 (Hs), Q920A1 (Mm), Q924T9 (Rn)
Wikipedia CysLT2 receptor
Leukotriene receptors
Search for 3D structures on the PDB
Search by keyword: Leukotriene receptors CysLT2 receptor Search by accession number: Q924T9, Q9NS75, Q920A1
Natural/Endogenous Ligand(s)
LTC4
LTD4
LTE4
Comments: LTC4 and LTD4 are more potent agonists than LTE4
Rank order of potency
LTC4 ≥ LTD4 >> LTE4  [2]
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
BAYu9773 Rn Full agonist 6.8 – 7.2 pA2 3

Explore drug-target interactions for this set of compounds using iPHACE

Functional Assay Comments
Shown to induce contraction of human pulmonary vein [4].
Physiological Functions
Contraction of smooth muscles, especially in vascular tissues.
Species:  None
Tissue: 
References: 
Phenotypes, Alleles and Disease Models Mouse data from MGI

Click here to show/hide data

Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Cysltr2tm1Ykn Cysltr2tm1Ykn/Cysltr2tm1Ykn
C57BL/6-Cysltr2		 MGI:1917336  MP:0009811 abnormal prostaglandin level PMID: 15328359 
Cysltr2tm1Sish Cysltr2tm1Sish/Cysltr2tm1Sish
involves: C57BL/6		 MGI:1917336  MP:0000343 altered response to myocardial infarction PMID: 18276782 
Cysltr2tm1Ykn Cysltr2tm1Ykn/Cysltr2tm1Ykn
C57BL/6-Cysltr2		 MGI:1917336  MP:0005597 decreased susceptibility to type I hypersensitivity reaction PMID: 15328359 
Cysltr2tm1Ykn Cysltr2tm1Ykn/Cysltr2tm1Ykn
C57BL/6-Cysltr2		 MGI:1917336  MP:0006050 pulmonary fibrosis PMID: 15328359 
General Comments
A recently cloned human 7TM, G protein-coupled receptor (346aa) appears to meet several criteria for the postulated CysLT2 receptor. Its gene is on 13q14 and the tissue distribution for expression is different from the CysLT1 receptor; it is located in lung macrophages, airway smooth muscle, cardiac Purkinjie cells, adrenal medulla cells, peripheral blood leukocytes and brain. The receptor has 38% aa identity to the CysLT1 receptor[1].

REFERENCES

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1. Heise, C. E., O'Dowd, B. F., Figueroa, D. J., Sawyer, N., Nguyen, T., Im, D. S., Stocco, R., Bellefeuille, J. N., Abramovitz, M., Cheng, R., Williams, D. L. Jr., Zeng, Z., Liu, Q., Ma, L., Clements, M. K., Coulombe, N., Liu, Y., Austin, C. P., George, S. R., O'Neill, G. P., Metters, K. M., Lynch, K. R. and Evans, J. F. (2000) Characterization of the new human cysteinyl leukotriene 2 receptor. J. Biol. Chem., 275: 30531-30536. [PMID:10851239]

2. Nothacker, H. P., Wang, Z., Zhu, Y., Reinscheid, R. K., Lin, S. H. and Civelli, O. (2000) Molecular cloning and characterization of a second human cysteinyl leukotriene receptor: discovery of a subtype selective agonist. Mol. Pharmacol., 58: 1601-1608. [PMID:11093801]

3. Tudhope, S. R., Cuthbert, N. J., Abram, T. S., Jennings, M. A., Maxey, R. J., Thompson, A. M., Norman, P. and Gardiner, P. J. (1994) BAYu9773, a novel antagonist of cysteinyl-leukotrienes with activity against two receptor subtypes. Eur. J. Pharmacol., 264: 317-323. [PMID:7698171]

4. Walch, L., Norel, X., Bäck, M., Gascard, J. P., Dahlén, S. E. and Brink, C. (2002) Pharmacological evidence for a novel cysteinyl-leukotriene receptor subtype in human pulmonary artery smooth muscle. Br. J. Pharmacol., 137: 1339-1345. [PMID:12466244]

To cite this database page, please use the following:

Charles Brink, Sven-Erik Dahlén, Jeffrey Drazen, Jilly F. Evans, Douglas W. P. Hay, G. Enrico Rovati, Charles N. Serhan, Takehiko Yokomizo.
Leukotriene receptors: CysLT2 receptor. Last modified on 14/03/2013. Accessed on 20/05/2013. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=270.


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