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J Biol Chem, Vol. 273, Issue 37, 24181-24189, September 11, 1998

High Constitutive Activity of the Human Formyl Peptide Receptor

Katharina Wenzel-Seifert, Carl M. Hurt, and Roland Seifert

From the Howard Hughes Medical Institute, Stanford University Medical School, Stanford, California 94305-5428

The formyl peptide receptor (FPR) couples to pertussis toxin (PTX)-sensitive Gi-proteins to activate chemotaxis and exocytosis in neutrophils. PTX reduces not only formyl peptide-stimulated but also agonist-independent ("basal") Gi-protein activity, suggesting that the FPR is constitutively active. We aimed at identifying an inverse FPR agonist, i.e. a compound that suppresses constitutive FPR activity. In Sf9 insect cell membranes, the G-protein heterotrimer Gialpha 2beta 1gamma 2 reconstituted N-formyl-L-methionyl-L-leucyl-L-phenylalanine (FMLP)-stimulated guanosine 5'-O-(3-thiotriphosphate) (GTPgamma S) binding and GTPgamma S-sensitive high affinity [3H]FMLP binding. The FPR "antagonist" cyclosporin H (CsH) potently and efficiently reduced basal GTPgamma S binding in Sf9 membranes. Another FPR antagonist, N-t-butoxycarbonyl-L-phenylalanyl-L-leucyl-L-phenylalanyl-L-leucyl-L-phenylalanine did not inhibit basal GTPgamma S binding but blocked the inhibitory effect of CsH on GTPgamma S binding. Na+ reduced basal GTPgamma S binding and eliminated the inhibitory effect of CsH. Similar effects of FMLP, CsH, and Na+ as in Sf9 membranes were observed with FPR expressed in the mammalian cell line HEK293. Our data show that the human FPR possesses high constitutive activity. CsH is an inverse FPR agonist and stabilizes the FPR in an inactive state. Na+ also stabilizes the FPR in an inactive state and, thereby, diminishes inverse agonist efficacy.

Copyright © 1998 by The American Society for Biochemistry and Molecular Biology, Inc.
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