Leukotriene B4 receptor 1 (BLT1) (BLT1)

Leukotriene B4 receptor 1 (BLT1) is a high-affinity G protein-coupled receptor (GPCR) that serves as the primary mediator for the potent pro-inflammatory lipid leukotriene B4 (LTB4) [1, 6]. It is predominantly expressed on the surface of various immune cells, including neutrophils, eosinophils, monocytes, and T lymphocytes, where it orchestrates chemotaxis and cellular activation [2, 11]. Upon binding LTB4, BLT1 triggers intracellular signaling pathways such as calcium mobilization and phospholipase C activation, leading to the recruitment of inflammatory cells to sites of injury or infection [7, 12]. Dysregulation of the LTB4-BLT1 axis is implicated in a wide range of chronic inflammatory and autoimmune conditions, including asthma, rheumatoid arthritis, and atherosclerosis [5, 10]. Consequently, BLT1 has been a significant focus for drug development, with various antagonists like Amelubant and LY293111 being evaluated in clinical trials to dampen excessive inflammatory responses [3, 8]. Despite its clear role in disease, clinical success has been limited, with some trials showing unexpected outcomes such as increased pulmonary exacerbations in cystic fibrosis patients [8]. Ongoing research continues to explore its potential in metabolic diseases and cancer immunotherapy [14, 15].

Other names

LTB4RBLTRP2Y7GPR16LTB4R1CMKRL1Chemoattractant receptor-like 1

Antagonist of the BLT1 receptor, which inhibits the binding of leukotriene B4 and subsequent pro-inflammatory signaling and leukocyte recruitment.