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cysteinyl leukotriene receptor 1 (CysLTR1, cysteinyl leukotriene D4 receptor, LTD4 receptor, HG55, HMTMF81)
Function:
- receptor for cysteinyl leukotrienes mediating bronchoconstriction of individuals with & without asthma
- stimulation by LTD4 results in contraction & proliferation of smooth muscle, edema, eosinophil migration & damage to the mucus layer in the lung
- this response is mediated via a G-protein that activates a phosphatidylinositol-Ca+2 second messenger system
- the rank order of affinities for the leukotrienes is LTD4 >> LTE4 = LTC4 >> LTB4
Structure: belongs to the G-protein coupled receptor 1 family
Compartment: cell membrane
Expression:
- widely expressed, with highest levels in spleen & peripheral blood leukocytes
- lower expression in several tissues, such as lung (mostly in smooth muscle bundles & alveolar macrophages), placenta, small intestine, pancreas, colon & heart
Pharmacology:
- selective antagonists, such as montelukast (singulair), zafirlukast (accolate) & pranlukast (Onon), are used in the treatment of the asthma
Related
leukotriene C
General
glycoprotein
leukotriene receptor
G-protein coupled receptor; serpentine receptor
Properties
SIZE: MW = 39 kD
entity length = 337 aa
COMPARTMENT: cellular membrane
MOTIF: exoplasmic domain {1-28}
MOTIF: N-glycosylation site {N6}
transmembrane domain {29-49}
cytoplasmic loop {50-57}
transmembrane domain {58-78}
exoplasmic loop {79-106}
MOTIF: cysteine residue {C96}
MODIFICATION: cysteine residue {C173}
transmembrane domain {107-127}
cytoplasmic loop {128-141}
transmembrane domain {142-162}
exoplasmic loop {163-193}
MOTIF: N-glycosylation site {N169}
cysteine residue {C173}
MODIFICATION: cysteine residue {C96}
N-glycosylation site {N180}
transmembrane domain {194-214}
cytoplasmic loop {215-230}
transmembrane domain {231-251}
exoplasmic loop {252-276}
MOTIF: N-glycosylation site {N262}
transmembrane domain {277-297}
cytoplasmic domain {298-337}
Database Correlations
OMIM 300201
UniProt Q9Y271
Pfam PF00001
Kegg hsa:1080
References
UniProt :accession Q9Y271