The leukotriene receptors (nomenclature as agreed by the NC-IUPHAR subcommittee on Leukotriene Receptors [6-7]) are activated by the endogenous ligands leukotrienes (LT), synthesized from lipoxygenase metabolism of arachidonic acid. The human BLT₁ receptor is the high affinity LTB₄ receptor whereas the BLT₂ receptor in addition to being a low-affinity LTB₄ receptor also binds several other lipoxygenase-products, such as 12S-HETE, 12S-HPETE, 15S-HETE, and the thromboxane synthase product 12-hydroxyheptadecatrienoic acid. The BLT receptors mediate chemotaxis and immunomodulation in several leukocyte populations and are in addition expressed on non-myeloid cells, such as vascular smooth muscle and endothelial cells. In addition to BLT receptors, LTB₄ has been reported to bind to the peroxisome proliferator activated receptor (PPAR) α [41] and the vanilloid TRPV1 ligand-gated nonselective cation channel [46]. The crystal structure of the BLT₁ receptor was initially determined in complex with selective antagonists [32,47] and has recently been extended to the cryo-electron microscopy structure of LTB₄-bound human BLT₁ receptor at 2.91 Å resolution [73]. The receptors for the cysteinyl-leukotrienes (i.e. LTC₄, LTD₄ and LTE₄) are termed CysLT₁ and CysLT₂ and exhibit distinct expression patterns in human tissues, mediating for example smooth muscle cell contraction, regulation of vascular permeability, and leukocyte activation. Quite recently, the the crystal structures of both receptors have been solved, the CysLT₁ in complex with zafirlukast and pranlukast [42] and the CysLT₂ in complex with three dual CysLT₁/CysLT₂ antagonists [28]. There is also evidence in the literature for additional CysLT receptor subtypes, derived from functional in vitro studies, radioligand binding and in mice lacking both CysLT₁ and CysLT₂ receptors [7]. Cysteinyl-leukotrienes have also been suggested to signal through the P2Y₁₂ receptor [21,49,54], GPR17 [14] and GPR99 [37].

The FPR2/ALX receptor (nomenclature as agreed by the NC-IUPHAR subcommittee on Leukotriene and Lipoxin Receptors [7]) is activated by the endogenous lipid-derived, anti-inflammatory ligands lipoxin A₄ (LXA₄) and 15-epi-LXA₄ (aspirin triggered lipoxin A4, ATL). The FPR2/ALX receptor also interacts with endogenous peptide and protein ligands, such as MHC binding peptide [13] as well as annexin I (ANXA1, P04083) (ANXA1) and its N-terminal peptides [16,56]. In addition, a soluble hydrolytic product of protease action on the urokinase-type plasminogen activator receptor has been reported to activate the FPR2/ALX receptor [61]. Furthermore, FPR2/ALX has been suggested to act as a receptor mediating the proinflammatory actions of the acute-phase reactant, serum amyloid A [67,69]. FPR2/ALX has also been reported to be activated by resolvin D1 [48]. The agonist activity of the lipid mediators described has been questioned [29,57], which may derive from batch-to-batch differences, partial agonism or biased agonism. Results from Cooray et al. (2013) [16] have addressed this issue and the role of homodimers and heterodimers in intracellular signaling. ATL-induced conformational changes of recombinant human ALX was demonstrated using FRET analysis [24]; ATL gives a bell-shaped concentration-response relationship, inducing maximal conformational changes of ALX at 0.1-1 nM. In addition, the crystal structure of ALX was reported at 2.8 Å resolution [12]. A receptor selective for LXB₄ has been suggested from functional studies [1,45,62]. Note that the data for FPR2/ALX are also reproduced on the Formylpeptide receptor pages.

Oxoeicosanoid receptors (OXE, nomenclature agreed by the NC-IUPHAR subcommittee on Leukotriene receptors [5]) are activated by endogenous chemotactic eicosanoid ligands oxidised at the C-5 position, with 5-oxo-ETE the most potent agonist identified for this receptor. Initial characterization of the heterologously expressed OXE receptor suggested that polyunsaturated fatty acids, such as docosahexaenoic acid and EPA, acted as receptor antagonists [33].

* Key recommended reading is highlighted with an asterisk

* Brink C, Dahlén SE, Drazen J, Evans JF, Hay DW, Nicosia S, Serhan CN, Shimizu T, Yokomizo T. (2003) International Union of Pharmacology XXXVII. Nomenclature for leukotriene and lipoxin receptors. Pharmacol Rev, 55 (1): 195-227. [PMID:12615958]

* Brink C, Dahlén SE, Drazen J, Evans JF, Hay DW, Rovati GE, Serhan CN, Shimizu T, Yokomizo T. (2004) International Union of Pharmacology XLIV. Nomenclature for the oxoeicosanoid receptor. Pharmacol Rev, 56 (1): 149-57. [PMID:15001665]

* Bäck M, Dahlén SE, Drazen JM, Evans JF, Serhan CN, Shimizu T, Yokomizo T, Rovati GE. (2011) International Union of Basic and Clinical Pharmacology. LXXXIV: leukotriene receptor nomenclature, distribution, and pathophysiological functions. Pharmacol Rev, 63 (3): 539-84. [PMID:21771892]

* Bäck M, Powell WS, Dahlén SE, Drazen JM, Evans JF, Serhan CN, Shimizu T, Yokomizo T, Rovati GE. (2014) Update on leukotriene, lipoxin and oxoeicosanoid receptors: IUPHAR Review 7. Br J Pharmacol, 171 (15): 3551-74. [PMID:24588652]

Kanaoka Y, Boyce JA. (2004) Cysteinyl leukotrienes and their receptors: cellular distribution and function in immune and inflammatory responses. J Immunol, 173 (3): 1503-10. [PMID:15265876]

* Laidlaw TM, Boyce JA. (2012) Cysteinyl leukotriene receptors, old and new; implications for asthma. Clin Exp Allergy, 42 (9): 1313-20. [PMID:22925317]

Nelson JW, Leigh NJ, Mellas RE, McCall AD, Aguirre A, Baker OJ. (2014) ALX/FPR2 receptor for RvD1 is expressed and functional in salivary glands. Am J Physiol, Cell Physiol, 306 (2): C178-85. [PMID:24259417]

Sasaki F, Yokomizo T. (2019) The leukotriene receptors as therapeutic targets of inflammatory diseases. Int Immunol, 31 (9): 607-615. [PMID:31135881]

Serhan CN. (2014) Pro-resolving lipid mediators are leads for resolution physiology. Nature, 510 (7503): 92-101. [PMID:24899309]

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Subcommittee members: Magnus Bäck (Chairperson) Translational Cardiology Karolinska Institutet, Department of Medicine Karolinska University Hospital M85 141 86 Stockholm Sweden Sven-Erik Dahlén Unit for Experimental Asthma and Allergy Research The National Institute of Environmental Medicine Karolinska Institutet S-171 77 Stockholm Sweden Jeffrey Drazen Respiratory Division Brigham and Woman's Hospital 75 Francis Street Boston, MA 02115 USA Jilly F. Evans PharmAkea 12780 El Camino Real San Diego, CA 92130 USA G. Enrico Rovati Laboratory of Molecular Pharmacology Department of Pharmaceutical Sciences University of Milan Via Balzaretti 9 Milan 201 33 Italy Takao Shimizu National Center for Global Health and Medicine Shinjyuku Tokyo 166-8655 Japan Charles N. Serhan Center for Experimental Theraputics and Reperfusion Injury Brigham and Women's Hospital Hale Building for Transformative Medicine 60 Fenwood Road, Suite 3-016 Boston, MA 02115 USA Takehiko Yokomizo Department of Biochemistry Juntendo University School of Medicine Hongo 2-1-1 Bunkyo-ku Tokyo 113-8421 Japan

Other contributors: Charles Brink Hopital Marie Lannelongue 133 Ave. de la Rèsistance Le Plessis Robinson F-92350 France Nan Chiang Center for Experimental Theraputics and Reperfusion Injury Brigham and Women's Hospital Hale Building for Transformative Medicine 60 Fenwood Road, Suite 3-016 Boston, MA 02115 USA Gordon Dent Science and Technology in Medicine School of Medicine Keele University Staffordshire, ST5 5BG UK Douglas W. P. Hay Department of Pulmonary Biology SmithKline Beecham Pharmaceuticals 709 Swedeland Road King of Prussia PA 19406-0939 USA Motonao Nakamura Department of Biochemistry and Molecular Biology The University of Tokyo 7-3-1, Hongo Bunkyo-ku Tokyo, Japan William Powell Meakins-Christie Laboratories McGill University 3626 St Urbain Street Montreal, QC H2X 2P2 Canada Joshua Rokach Claude Pepper Institute and Department of Chemistry Florida Institute of Technology 150 West University Boulevard Melbourne Florida 32901 USA Mohib Uddin AstraZeneca R&D BioPharmaceuticals Gothenburg, SE-431 83 Sweden