Leukotriene B4 receptors (LTB4Rs) belong to rhodopsin-like G-protein-coupled receptor superfamily, which can bind leukotriene B4, a pro-inflammatory mediator produced predominantly by neutrophils and macrophages. In acute inflammatory responses, leukotriene B4 can recruit and activate the neutrophils, monocytes and eosinophils and prolongs their survival. It also stimulates the production of various proinflammatory cytokines and mediators indicating an ability to augment and prolong tissue inflammation. Two leukotriene B4 receptors have been identified: LTB4R1 with high-affinity, LTB4R2 with low-affinity, and they have 45% amino acid identity. In addition to the classical expression in peripheral leukocytes and peritoneal macrophages, LTB4R1 was shown in differentiated T cells (T helper cells: Th1, Th2, Th17, and effector CD8 T cells), dendritic cells and osteoclasts. The physiological roles of LTB4R1 include: mediating acute inflammatory, calcium mobilization and contraction, protection against invasion, increasing proliferation of myoblasts and neural stem cells, induction of itch responses. LTB4R2 is widely expressed in most human tissues, with highest levels in the liver, spleen, ovary and leukocytes. Binding with leukotriene B4, LTB4R2 can increase the level of inositol trisphosphate and calcium, along with the inhibition of forskolin-stimulated adenylyl cyclase activity and chemotaxis. Several reports suggest that LTB4R2-dependent generation of reactive oxygen species is involved in epithelial-mesenchymal transition and cancer progression.
Here show two subtypes of LTB4Rs (LTB4R1 and LTB4R2). The promoter of LTB4R1 is localized within the open reading frame (ORF) of LTB4R2, a so-called promoter in ORF. As an antagonist, LY255283 inhibits both LTB4R1 and LTB4R2-dependent calcium mobilization. Based on LTB4Rs, a lot of synthetic agonists are under clinical development to treat a series of immunological diseases and cancer.
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