Biological Information
Background Information:
Leukotriene (LT) receptors most sensitive to the endogenous ligand BLT4 are named BLT receptors, whereas those preferentially activated by the CysLTs are named LTC4, D4 and E4. LT receptors belong to the superfamily of G protein-coupled seven transmembrane proteins. G-protein-coupled receptors constitute one of the major signal transduction systems in eukaryotic cells. Coding sequences for these receptors, in those regions believed to contribute to the agonist-antagonist binding site, are strongly conserved across mammalian species. LTB4 receptors are found in leukocytes, spleen and thymus and also reported to be present in peritoneal macrophages and eosinophils. LTB4 receptor agonism promotes neutrophil chemotaxis and secretion contributing to inflammation, but may also affect immunomodulation, etc. BLT receptor antagonism may be useful in the treatment of pulmonary inflammation (COPD, asthma) and ulcerative colitis.
PathHunter β-Arrestin GPCR cell lines are engineered to co-express the ProLink™ (PK) tagged GPCR and the Enzyme Acceptor (EA) tagged β-Arrestin. Activation of the GPCR-PK induces β-Arrestin-EA recruitment, forcing complementation of the two enzyme fragments. The resulting functional enzyme hydrolyzes substrate to generate a chemiluminescent signal. PathHunter cell lines expressing Gq-coupled receptors can also be used to detect calcium mobilization.
Family:
GPCR
Sub Family:
Leukotriene
Class:
Class A
Coupling:
Gi/Go & Gq
Protein Name:
BLT1 (LTB4)
Uniprot Number:
Q15722
Protein Aliases:
LTB4-R1|Chemoattractant receptor-like 1|G-protein coupled receptor 16|P2Y purinoceptor 7|P2Y7
Gene Name:
LTB4R
Gene ID:
1241
Gene Aliases:
BLT|BLT1|BLTR|CMKRL1|GPR16|P2RY7
Accession Number:
AY322535
Organism:
Human
Cell Type:
CHO-K1
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Agonist
β-Arrestin Isoform:
β-Arrestin-2
Testing Information
Control Activator:
Leukotriene B4
Test Concentration / Dose:
Eurofins will provide IC/EC50 calculation if 10 concentrations are selected
Test Sample Requirements:
40uL of a 1000X stock for the first assay and 2uL for each additional assay (assay = 1 target, 1 readout, 1 mode)
Minimum Order Quantity:
20
Turnaround Time
Standard:
15 Business Days
Clinical Relevance
Adverse / Beneficial Action:
LTB4 receptor agonism promotes neutrophil chemotaxis and secretion contributing to inflammation, but may also affect immunomodulation, etc. BLT receptor antagonism may be useful in the treatment of pulmonary inflammation (COPD, asthma) and ulcerative colitis.
Additional Information
Brand:
LeadHunter
Testing Location:
USA - Fremont, CA