Leukotriene receptors

Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).

Overview

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Leukotriene receptors (nomenclature agreed by NC-IUPHAR subcommittee on Leukotriene Receptors, [4]) are activated by the endogenous ligands leukotriene B4 (LTB4), LTC4, LTD4, LTE4, 12R-HETE and 12S-HETE. CysLT1 and CysLT2 are co-expressed by most myeloid cells. However, the function of CysLT2 remains unclear. CysLT2 has been demonstrated to exert a suppressive influence on CysLT1 expression, suggesting an autoregulatory function which is indicated by a reported up-regulation of CysLT-mediated responses in mice lacking CysLT2 receptors [20].

Leukotrienes bind extensively to enzymes in their metabolic pathways (glutathione-S-transferase/LTC4 synthase, γ-glutamyltranspeptidase and several aminopeptidases) and can also bind to peroxisome proliferator-activated receptor α (PPARα, [24]) and the FPR2/ALX lipoxin receptor [8], complicating the interpretation of radioligand binding and functional studies (e.g. LTC4 is rapidly converted in many systems to LTD4). Metabolic inhibitors (e.g. serine–borate complex) reduce this problem but can also have nonspecific effects.

Receptors

BLT1 receptor Show summary » More detailed page

BLT2 receptor Show summary » More detailed page

CysLT1 receptor Show summary » More detailed page

CysLT2 receptor Show summary » More detailed page

OXE receptor Show summary » More detailed page

FPR2/ALX Show summary » More detailed page

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References

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NC-IUPHAR subcommittee and family contributors

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How to cite this family page

Database page citation:

Leukotriene receptors. Accessed on 27/08/2014. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=35.

Concise Guide to PHARMACOLOGY citation:

Alexander SPH, Benson HE, Faccenda E, Pawson AJ, Sharman JL, Spedding M, Peters JA and Harmar AJ, CGTP Collaborators. (2013) The Concise Guide to PHARMACOLOGY 2013/14: G Protein-Coupled Receptors. Br J Pharmacol. 170: 1459–1581.