PMID: 9547367May 9, 1998Paper

Identification and characterization of two cysteinyl-leukotriene high affinity binding sites with receptor characteristics in human lung parenchyma

Molecular Pharmacology
V CapraG E Rovati

Abstract

We report the characterization of two distinct binding sites with receptor characteristics for leukotriene (LT)D4 and LTC4 in membranes from human lung parenchyma. The use of S-decyl-glutathione allowed us to characterize a previously unidentified high affinity binding site for LTC4. Computerized analysis of binding data revealed that each leukotriene interacts with two distinct classes of binding sites (Kd = 0.015 and 105 nM for LTC4 and 0.023 and 230 nM for LTD4) and that despite cross-reactivity, the two high affinity sites are different entities. LTD4 binding sites displayed features of G protein-coupled receptors, whereas LTC4 binding sites did not show any significant modulation by guanosine-5'-(beta, gamma-imido)triphosphate or stimulation of GTPase activity. The antagonists ICI 198,615 and SKF 104353 were unselective for the high and low affinity states of LTD4 receptor, whereas only SKF 104353 was able to recognize the two [3H]LTC4 binding sites although with different affinities. These data indicate that in human lung parenchyma, LTD4 and LTC4 recognize two different binding sites; these binding sites are different entities; and for LTD4, the two binding sites represent the interconvertible affinity states of a G prot...Continue Reading

References

Sep 1, 1979·Proceedings of the National Academy of Sciences of the United States of America·R C MurphyB Samuelsson
Dec 8, 1976·Biochimica Et Biophysica Acta·D Cassel, Z Selinger
Jan 1, 1992·Reviews of Physiology, Biochemistry and Pharmacology·D Keppler
Jan 1, 1991·Annals of the New York Academy of Sciences·P J PiperD A Spencer
Jul 3, 1990·European Journal of Pharmacology·P J GardinerN J Cuthbert
Mar 1, 1989·Trends in Pharmacological Sciences·S T CrookeC F Bennett
Dec 4, 1980·Nature·S E DahlénB Samuelsson
Sep 1, 1980·Analytical Biochemistry·P J Munson, D Rodbard
Jan 1, 1994·Drugs·N Chanarin, S L Johnston
Mar 1, 1994·European Journal of Biochemistry·I LeierD Keppler
Dec 1, 1993·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·G E Rovati
Aug 1, 1993·Trends in Pharmacological Sciences·R J LefkowitzT Costa

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Citations

May 13, 2005·International Journal of Immunopathology and Pharmacology·P BalleriniU Traversa
Feb 15, 2000·American Journal of Respiratory and Critical Care Medicine·S T Holgate, A P Sampson
Feb 15, 2000·American Journal of Respiratory and Critical Care Medicine·S NicosiaG E Rovati
Mar 22, 2012·Medicinal Research Reviews·Valérie CapraG Enrico Rovati
Mar 5, 2014·British Journal of Pharmacology·Magnus BäckG Enrico Rovati
Jul 15, 2011·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·Chiara CarniniAngelo Sala
Nov 7, 2001·Clinical and Experimental Allergy : Journal of the British Society for Allergy and Clinical Immunology·H MitaK Akiyama
Jul 29, 2000·Biochemical and Biophysical Research Communications·J TakasakiK Furuichi
Oct 6, 2001·Biochemical and Biophysical Research Communications·M KamoharaK Furuichi
Feb 13, 2001·Pulmonary Pharmacology & Therapeutics·S NicosiaG E Rovati
Oct 24, 1998·Trends in Pharmacological Sciences·G E Rovati
Oct 2, 2003·Prostaglandins & Other Lipid Mediators·Valérie CapraG Enrico Rovati

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