International Union of Pharmacology XXXVII. Nomenclature for Leukotriene and Lipoxin Receptors

Brink, Charles; Dahlén, Sven‐Erik; Drazen, Jeffrey M.; Evans, Jilly F.; Hay, Douglas W. P.; Nicosia, S.; Serhan, Charles N.; Shimizu, Takao; Yokomizo, Takehiko

doi:10.1124/pr.55.1.8

Cited by 254 publications

(262 citation statements)

References 328 publications

(395 reference statements)

Supporting

Mentioning

257

Contrasting

Unclassified

Order By: Relevance

“…1) [5]. While the BLT receptors are denoted BLT 1 and BLT 2 , for the high and low affinity receptor subtypes, respectively, receptors activated by the cysteinyl-LTs are characterized by their sensitivity to available antagonists and are referred to as CysLT 1 and CysLT 2 [7,8] The latter nomenclature probably only in part describes the cysteinyl-LT signaling, since limitation of the currently available CysLT receptor antagonists [8], as well as cross-reactivities between CysLT and purinoreceptors [9] indicate more complex receptor ligation properties for cysteinyl-LTs.…”

Section: Leukotriene Receptorsmentioning

confidence: 99%

Leukotriene Signaling in Atherosclerosis and Ischemia

Bäck

2008

Cardiovasc Drugs Ther

121

View full text Add to dashboard Cite

Section: Leukotriene Receptorsmentioning

confidence: 99%

Leukotriene Signaling in Atherosclerosis and Ischemia

Bäck

2008

Cardiovasc Drugs Ther

121

View full text Add to dashboard Cite

Section: Introductionmentioning

confidence: 99%

“…Until now, two receptor subtypes have been cloned, namely CysLT 1 and CysLT 2 [8]. In particular, when the CysLT 1 receptor is expressed in recombinant systems it shows a preferential coupling to G q/11 , whereas when constitutively expressed it has been reported to activate both pertussis toxin (PTX)-sensitive and -insensitive G-proteins [8,9]. This was demonstrated in dimethyl sulfoxide-differentiated U937 (dU937) cells, an immortalized cell line known to constitutively express a high density of CysLT 1 receptors upon differentiation to monocytes/macrophages [10,11], CysLT 1 receptors respond to LTD 4 with a strong increase in cytosolic Ca 2+ concentration ([Ca 2+ ] i ) partially sensitive to PTX, and with the activation of the Ras-MAPK cascade totally dependent upon G i/o [12].…”

Section: Introductionmentioning

confidence: 99%

CysLT1 leukotriene receptor antagonists inhibit the effects of nucleotides acting at P2Y receptors

Mamedova

Capra

Accomazzo

et al. 2005

Biochemical Pharmacology

View full text Add to dashboard Cite

Montelukast and pranlukast are orally active leukotriene receptor antagonists selective for the CysLT 1 receptor. Conversely, the hP2Y 1,2,4,6,11,12,13,14 receptors represent a large family of GPCRs responding to either adenine or uracil nucleotides, or to sugar-nucleotides. Montelukast and pranlukast were found to inhibit nucleotide-induced calcium mobilization in a human monocyte-macrophage like cell line, DMSO-differentiated U937 (dU937). Montelukast and pranlukast inhibited the effects of UTP with IC 50 values of 7.7 and 4.3 μM, respectively, and inhibited the effects of UDP with IC 50 values of 4.5 and 1.6 μM, respectively, in an insurmountable manner. Furthermore, ligand binding studies using [ 3 H]LTD 4 excluded the possibility of orthosteric nucleotide binding to the CysLT 1 receptor. dU937 cells were shown to express P2Y 2 , P2Y 4 , P2Y 6 , P2Y 11 , P2Y 13 and P2Y 14 receptors. Therefore, these antagonists were studied functionally in a heterologous expression system for the human P2Y receptors. In 1321N1 astrocytoma cells stably expressing human P2Y 1,2,4,6 receptors, CysLT 1 antagonists inhibited both the P2Y agonist-induced activation of phospholipase C and intracellular Ca 2+ mobilization. IC 50 values at P2Y 1 and P2Y 6 receptors were <1 μM. In control astrocytoma cells expressing an endogenous M3 muscarinic receptor, 10 μM montelukast had no effect on the carbachol-induced rise in intracellular Ca 2+ . These data demonstrated that CysLT 1 receptor antagonists interact functionally with signaling pathways of P2Y receptors, and this should foster the study of possible implications for the clinical use of these compounds in asthma or in other inflammatory conditions.

show abstract

“…Among them, LTB 4 acts via BLT1 and BLT2. These receptors belong to a GPCR superfamily and share high similarity with other chemoattractant receptors [22]. Unlike BLT1, the molecular mechanism for BLT2 regulation remains unexplored.…”

Section: Discussionmentioning

confidence: 99%

BLT2 phosphorylation at Thr³⁵⁵by Akt is necessary for BLT2-mediated chemotaxis

Wei

Kim

2011

FEBS Letters

View full text Add to dashboard Cite

Edited by Masayuki MiyasakaKeywords: Leukotriene B 4 receptor 2 (BLT2) Chemotaxis Akt Reactive oxygen species a b s t r a c t BLT2, a low-affinity leukotriene B 4 (LTB 4 ) receptor, is a member of the G protein-coupled receptor family and is involved in multiple cellular responses, including chemotaxis. Despite its biological significance, the mechanisms of BLT2 regulation, especially by protein kinases, are poorly characterised. In this study, we found that Akt phosphorylates BLT2 at its C-terminal Thr 355 residue and that this event is critical for BLT2-mediated chemotactic responses. In addition, we found that Rac1 stimulation and subsequent reactive oxygen species (ROS) production lie downstream of BLT2 phosphorylation, thus mediating chemotaxis. Structured summary of protein interactions:BLT2 physically interacts with Akt by pull down (View interaction) BLT2 physically interacts with Akt by pull down (View interaction)

show abstract

International Union of Pharmacology XXXVII. Nomenclature for Leukotriene and Lipoxin Receptors

Cited by 254 publications

References 328 publications

Leukotriene Signaling in Atherosclerosis and Ischemia

Leukotriene Signaling in Atherosclerosis and Ischemia

CysLT1 leukotriene receptor antagonists inhibit the effects of nucleotides acting at P2Y receptors

BLT2 phosphorylation at Thr³⁵⁵by Akt is necessary for BLT2-mediated chemotaxis

Contact Info

Product

Resources

About

International Union of Pharmacology XXXVII. Nomenclature for Leukotriene and Lipoxin Receptors

Cited by 254 publications

References 328 publications

Leukotriene Signaling in Atherosclerosis and Ischemia

Leukotriene Signaling in Atherosclerosis and Ischemia

CysLT1 leukotriene receptor antagonists inhibit the effects of nucleotides acting at P2Y receptors

BLT2 phosphorylation at Thr355by Akt is necessary for BLT2-mediated chemotaxis

Contact Info

Product

Resources

About

BLT2 phosphorylation at Thr³⁵⁵by Akt is necessary for BLT2-mediated chemotaxis