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.

cAMP Hunter cell lines overexpress naturally coupled, wild type GPCRs and are designed to detect increases in intracellular cAMP levels (Gs-coupled receptors) or inhibition of intracellular cAMP production (Gi-coupled receptors) in response to agonist stimulation of the receptor. These cell lines are designed to be used in conjunction with the HitHunter® cAMP Assay Detection Kit. cAMP Hunter cell lines expressing receptors that will couple to Gq proteins can also be used to detect induction of 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:

Antagonist

Testing Information

Control Inhibitor:

LY255283

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