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Exploring the pharmacology of the leukotriene B-4 receptor BLT1, without the confounding effects of BLT2

Sabirsh, Alan LU ; Bristulf, Jesper LU and Owman, Christer LU (2004) In European Journal of Pharmacology 499(1-2). p.53-65
Abstract
Most previous studies of leukotriene B-4 (LTB4) pharmacology using primary leukocyte cultures and myeloid cell lines do not differentiate between leukotriene BLT1 and BLT1 receptor activation because both receptors are often expressed by these cells. Here we show that in HeLa cells expressing BLT1 but not BLT2 receptors, BLT1 receptor activation resulted in IP3 mediated calcium release from intracellular stores initially, followed by calcium influx through cell membrane channels. BLT1 calcium signalling was sensitive to the activity of protein kinase C (PKC). protein kinase A (PKA) and protein-tyrosine kinases (PTKs), as well as changes in membrane cholesterol levels and treatments that are known to disrupt normal membrane physiology... (More)
Most previous studies of leukotriene B-4 (LTB4) pharmacology using primary leukocyte cultures and myeloid cell lines do not differentiate between leukotriene BLT1 and BLT1 receptor activation because both receptors are often expressed by these cells. Here we show that in HeLa cells expressing BLT1 but not BLT2 receptors, BLT1 receptor activation resulted in IP3 mediated calcium release from intracellular stores initially, followed by calcium influx through cell membrane channels. BLT1 calcium signalling was sensitive to the activity of protein kinase C (PKC). protein kinase A (PKA) and protein-tyrosine kinases (PTKs), as well as changes in membrane cholesterol levels and treatments that are known to disrupt normal membrane physiology and/or lipid rafts. Inhibition of MAP kinases, Rho-associated kinases, or phosphomositol-3-kinases (PI3K) had no effect on BLT1 receptor induced calcium signalling, and the receptor was insensitive to the redox state of the extracellular compartment. (C) 2004 Elsevier B.V. All rights reserved. (Less)
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author
organization
publishing date
type
Contribution to journal
publication status
published
subject
keywords
fura-2, BLT1, leukotriene B-4, g-protein coupled receptor, pharmacology, calcium
in
European Journal of Pharmacology
volume
499
issue
1-2
pages
53 - 65
publisher
Elsevier
external identifiers
  • wos:000224090000006
  • pmid:15363951
  • scopus:19344376165
ISSN
1879-0712
DOI
10.1016/j.ejphar.2004.07.060
language
English
LU publication?
yes
id
7d4ecaf6-b4db-41e5-a88d-a967026883c4 (old id 266529)
date added to LUP
2007-10-31 11:04:18
date last changed
2017-01-01 04:53:34
@article{7d4ecaf6-b4db-41e5-a88d-a967026883c4,
  abstract     = {Most previous studies of leukotriene B-4 (LTB4) pharmacology using primary leukocyte cultures and myeloid cell lines do not differentiate between leukotriene BLT1 and BLT1 receptor activation because both receptors are often expressed by these cells. Here we show that in HeLa cells expressing BLT1 but not BLT2 receptors, BLT1 receptor activation resulted in IP3 mediated calcium release from intracellular stores initially, followed by calcium influx through cell membrane channels. BLT1 calcium signalling was sensitive to the activity of protein kinase C (PKC). protein kinase A (PKA) and protein-tyrosine kinases (PTKs), as well as changes in membrane cholesterol levels and treatments that are known to disrupt normal membrane physiology and/or lipid rafts. Inhibition of MAP kinases, Rho-associated kinases, or phosphomositol-3-kinases (PI3K) had no effect on BLT1 receptor induced calcium signalling, and the receptor was insensitive to the redox state of the extracellular compartment. (C) 2004 Elsevier B.V. All rights reserved.},
  author       = {Sabirsh, Alan and Bristulf, Jesper and Owman, Christer},
  issn         = {1879-0712},
  keyword      = {fura-2,BLT1,leukotriene B-4,g-protein coupled receptor,pharmacology,calcium},
  language     = {eng},
  number       = {1-2},
  pages        = {53--65},
  publisher    = {Elsevier},
  series       = {European Journal of Pharmacology},
  title        = {Exploring the pharmacology of the leukotriene B-4 receptor BLT1, without the confounding effects of BLT2},
  url          = {http://dx.doi.org/10.1016/j.ejphar.2004.07.060},
  volume       = {499},
  year         = {2004},
}