Inhibitory effect of peptides derived from the N-terminus of lipocortin 1 on arachidonic acid release and proliferation in the A549 cell line: identification of E-Q-E-Y-V as a crucial component

British Journal of Pharmacology
J D CroxtallR J Flower

Abstract

1. The ability of the glucocorticoid-induced protein lipocortin 1 (LC1) to inhibit arachidonic acid release and cell proliferation in A549 cells may be mimicked by a sequence taken from the N-terminal, LC1(13-25) (FIENEEQEYVQTV). We have now synthesized and tested for biological activity a library of 25 smaller peptides derived from this sequence. 2. Peptides were tested in two assays: A549 cells were prelabelled with tritiated arachidonic acid and thapsigargin (50 nM) and EGF (10 nM) used to stimulate the release of this fatty acid. Cell proliferation was determined by counting cell numbers following 3 day incubation with these peptides, or controls. 3. Many of the peptides were highly insoluble but could be more readily dissolved in aqueous solution in the presence of commercial liposomes or phosphatidyl serine (5 microM). Since neither of these agents alone had any effect on arachidonic acid release or cell proliferation, all peptides were tested in the presence of 5 microM phosphatidyl serine. Under these conditions LC1(13-25) was active in both assay systems with an IC40 of 40.7 and 57.0 microM respectively. 4. Deletion of amino acids from the C-terminus of the peptide progressively diminished (2-3 fold) the molar potency ...Continue Reading

References

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Citations

Jul 1, 1994·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·J C BuckinghamR J Flower
Jan 30, 2002·British Journal of Pharmacology·Jamie D CroxtallRod J Flower
Jun 15, 2012·Molecular Membrane Biology·Joanna Bandorowicz-PikulaSlawomir Pikula
Jun 18, 2005·Memórias do Instituto Oswaldo Cruz·Ahmad M KamalMauro Perretti
Oct 23, 2009·British Journal of Pharmacology·Mauro Perretti, Jesmond Dalli
Sep 18, 2007·Fundamental & Clinical Pharmacology·Christian DürstelerMargarita M Puig
Dec 23, 1999·The Journal of Biological Chemistry·L C AlldridgeC E Bryant
Feb 11, 2015·British Journal of Pharmacology·P G TrentinP M R Silva
Jan 4, 2006·Molecular and Cellular Endocrinology·In-Ho Song, Frank Buttgereit

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