Leukotriene GPCR Assays

Background of Leukotriene Receptors

Leukotrienes refer to a class of arachidonic acid-derived bioactive molecules that are considered to be the drug targets against allergic and inflammatory reactions. The leukotriene receptors are G protein-coupled receptors that bind and are activated by the leukotrienes.

Fig.1. Structure of guinea pig BLT1 bound with a BLT antagonist, BIIL260. (Yokomizo, et al., 2018)

Distribution and Function of Leukotriene Receptors

Human BLT1 is mainly expressed in various subsets of leukocytes, subsets of dendritic cells, and macrophages. The expression of BLT2 can be detected in keratinocytes, epithelial cells of the intestine, lung alveolar type 2 cells, and vascular endothelial cells. CysLT receptors can be expressed in peripheral blood leukocytes, spleen, lung, as well as other tissues at lower levels. The binding of leukotrienes and leukotriene receptors plays an important role in inflammatory signaling pathways.

Subtypes and Mechanisms of Leukotriene Receptors

The leukotriene receptors can be divided into two groups of structurally related GPCRs, including the chemoattractant-like BLT receptors (BLT1 and BLTR2) and the CysLT receptors (CysLT1 and CysLT2). They are all of the G_q/G₁₁ family that activates PLC signaling mechanisms.

Receptor	Gene	Mechanism	Agonists	Antagonists
Leukotriene B4 receptor 1	LTB4R	BLT1 is able to couple with both G_i-like and G_q-like (G16) G proteins. BLT1 stimulation results in degranulation through the production of phosphatidylinositol tris-phosphates (IP3) via activation of phosphatidylinositol-3-kinase (PI3 kinase).	Leukotriene B4	BIIL260 LY255283 ZK158252 CP195543 U75302
Leukotriene B4 receptor 2	LTB4R2	Activation of BLT2 leads to the activation of G_i- and G_q-type G proteins. BLT2 activates the generation of reactive oxygen species in some cancer cells.	Leukotriene B4	LY255283 ZK158252 CP195543
Cysteinyl leukotriene receptor 1	CYSLTR1	Activation of CysLT1 by LTD4 results in the production of several second intracellular messengers via phospholipase Cβ.	MK 571	Montelukast ONO 1078 Zafirlukast MK-571 Pranlukast
Cysteinyl leukotriene receptor 2	CYSLTR2	CysLT2 stimulation elicits IL-8 secretion via G_i/o protein. CysLT2 negatively regulates Th2 development of lung inflammation by inhibiting CysLT1 function on dendritic cells.	MK 571	Zafirlukast Pranlukast BAY-u9773 Gemilukast

Assay List of Leukotriene Receptors

Creative Biolabs can provide a range of assays of leukotriene receptors. You can choose the assay in the list or contact us for more information:

LTB4R LTB4R2 OXER1

Assay No.	Assay Name	Host Cell	Assay Type	Datasheet
[³⁵S]GTPγS Binding Assay
S01YF-1122-KX557	Magic™ Human LTB4R In Vitro [³⁵S]GTPγS binding Assay	CHO-K1	[³⁵S]GTPγS binding Assay

Assay No.	Assay Name	Host Cell	Assay Type	Datasheet
Calcium Flux Assay
S01YF-1122-KX558	Magic™ Human LTB4R2 In Vitro Calcium Flux Assay	CHO-K1-Gqi5	Calcium Flux Assay

Assay No.	Assay Name	Host Cell	Assay Type	Datasheet
Calcium Flux Assay
S01YF-1122-KX563	Magic™ Human OXER1 In Vitro Calcium Flux Assay	CHO-K1-Gα16	Calcium Flux Assay

Published Data

Paper Title	Leukotriene receptors as potential therapeutic targets
Journal	The Journal of clinical investigation
Published	2018
Abstract	Derived from arachidonic acid, leukotrienes are a class of bioactive molecules known as mediators of allergic and inflammatory responses. On the basis of leukotriene receptor molecules, leukotriene biosynthesis inhibitors, and cysteinyl leukotriene receptor antagonists have been developed for the treatment of bronchial asthma and allergic rhinitis. This article details the discovery of leukotriene receptors as potential drug targets.
Result	CysLT1 antagonists and LT biosynthesis inhibitors have been shown to be useful in the symptomatic treatment of bronchial asthma and allergic rhinitis. In recent years, BLT1 antagonists have failed to demonstrate the ability to alleviate arthritis and psoriasis. Furthermore, studies of BLT1-KO mice and BLT1 antagonists expand BLT1-associated inflammatory diseases and demonstrate potential utility. BLT2 agonists are also used in the treatment of several diseases, especially refractory skin and corneal ulcers. Therefore, leukotriene receptors are important drug targets. Fig.2. Signaling via CysLT1, CysLT2, GPR17, GPR99, and P2Y12. (Yokomizo, et al., 2018)

Reference

Yokomizo, T.; et al. Leukotriene receptors as potential therapeutic targets. The Journal of clinical investigation. 2018, 128(7): 2691-2701.

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