Figure. Concentration-dependent activation of CYSLTR1 by LTD4

Reporter cells were transfected with either the expression plasmid for human cysteinyl leukotriene receptor 1 (CYSLTR1) or the mock plasmid and treated with various concentrations of LTD4. Data points shown are the mean ± SEM of an experiment (n = 3), and the curve is a fit to Hill equation with an EC50 of 7.9 nM.

cysteinyl leukotriene receptor 1
Available assay modes
Agonist, Inverse agonist, Antagonist, PAM, NAM
à la carte, Immunology/Infection, Hematology, Respiratory, Human non-orphan GPCRs

Leukotriene receptors

The leukotriene receptors 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 [1] and the vanilloid TRPV1 ligand-gated nonselective cation channel [2]. 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. 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 [3]. Cysteinyl-leukotrienes have also been suggested to signal through the P2Y12 receptor [4,5,6], GPR17 [7] and GPR99 [8].


  1. Lin Q, Ruuska SE, Shaw NS, et al. Ligand selectivity of the peroxisome proliferator-activated receptor alpha. Biochemistry 1999;38:185-90.
  2. McHugh D, McMaster RS, Pertwee RG, et al. Novel compounds that interact with both leukotriene B4 receptors and vanilloid TRPV1 receptors. J Pharmacol Exp Ther 2006;316:955-65.
  3. Bäck M, Powell WS, Dahlén SE, et al. Update on leukotriene, lipoxin and oxoeicosanoid receptors: IUPHAR Review 7. Br J Pharmacol 2014;171:3551-74.
  4. Fredman G, Van Dyke TE, Serhan CN. Resolvin E1 regulates adenosine diphosphate activation of human platelets. Arterioscler Thromb Vasc Biol 2010;30:2005-13.
  5. Nonaka Y, Hiramoto T, Fujita N. Identification of endogenous surrogate ligands for human P2Y12 receptors by in silico and in vitro methods. Biochem Biophys Res Commun 2005;337:281-288.
  6. Paruchuri S, Tashimo H, Feng C, et al. Leukotriene E4-induced pulmonary inflammation is mediated by the P2Y12 receptor. J Exp Med 2009;206:2543-55.
  7. Ciana P, Fumagalli M, Trincavelli ML, et al. The orphan receptor GPR17 identified as a new dual uracil nucleotides/cysteinyl-leukotrienes receptor. EMBO J 2006;25:4615-27.
  8. Kanaoka Y, Maekawa A, Austen KF. Identification of GPR99 protein as a potential third cysteinyl leukotriene receptor with a preference for leukotriene E4 ligand. J Biol Chem 2013;288:10967-72.
Excerpt from IUPHAR/BPS Guide to Pharmacology

Related Receptors

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