Leukotriene B4 receptor 1 and Leukotriene B4 receptor 2 (BLT1 and BLT2)

Leukotriene B4 receptors BLT1 and BLT2 are G protein-coupled receptors (GPCRs) that serve as the primary mediators for leukotriene B4 (LTB4), a potent lipid chemoattractant derived from arachidonic acid [1][3]. BLT1 is a high-affinity receptor predominantly expressed on leukocytes, including neutrophils and T cells, where it plays a critical role in driving acute and chronic inflammatory responses by promoting cell recruitment and activation [1][6]. BLT2, while having a lower affinity for LTB4, is a high-affinity receptor for 12-hydroxyheptadecatrienoic acid (12-HHT) and is expressed more ubiquitously, contributing to epithelial barrier maintenance and wound healing [1][10]. These receptors are significant therapeutic targets in inflammatory diseases such as asthma, rheumatoid arthritis, and psoriasis, as well as in various cancers where they promote tumor cell proliferation and metastasis [1][11][13]. Although numerous BLT1 antagonists, such as Amelubant and LY293111, have been investigated in clinical trials, none have yet achieved regulatory approval, often due to insufficient efficacy or safety concerns related to impaired host defense [11][13][14]. Recent drug discovery efforts are increasingly focused on achieving high selectivity between the two receptors to avoid the potentially counterproductive effects of non-selective modulation [11][13].

Other names

LTB4RLTB4R2BLTR1BLTR2P2Y7LTB4-R1LTB4-R2Leukotriene B4 receptorLTB4 receptor

Antagonism of the BLT1 receptor to inhibit pro-inflammatory leukocyte recruitment and activation, and modulation (agonism or antagonism) of the BLT2 receptor to influence epithelial barrier function and wound healing [1][11][13].