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(Received for publication, December 18, 1995, and in revised form, March 21, 1996)
From Based on the assumption that the prolactin
receptor (PRLR) is activated by PRL-induced sequential dimerization,
potential human PRL (hPRL) antagonists were designed that sterically
interfere with binding site 2. We previously reported the unexpected
agonistic properties of these hPRL analogs in the rat Nb2 bioassay
(Goffin, V., Struman, I., Mainfroid, V., Kinet, S., and Martial, J. A. (1994) J. Biol. Chem. 269, 32598-32606). In order to
investigate whether such paradoxical agonistic behavior might result
from characteristic features of the Nb2 assay (e.g. species
specificity), we transfected in the same cell system the cDNA
encoding the PRLR from rat or human species along with reporter genes
containing PRL-responsive DNA sequences. We characterized the
agonistic, self-antagonistic and/or antagonistic effects of wild type
rat PRL, wild type hPRL, and three hPRL analogs, mutated either at
binding site 1 or at binding site 2. Our results clearly show that the
agonistic/antagonistic properties of PRLs are species-specific. We thus
propose different models of receptor activation, depending on the
relative affinities of each hormonal binding site, which is directed by
species specificity. Finally, this is the first report of hPRL binding
site 2 analogs showing antagonistic properties on human and, to a
lesser extent, rat receptors.
Volume 271, Number 28,
Issue of July 12, 1996
pp. 16573-16579
©1996 by The American Society for Biochemistry and Molecular Biology, Inc.
,
,
,
INSERM unit 344, Endocrinologie
Moléculaire, 156 rue de Vaugirard, 75730, Paris Cedex 15, France
and the ¶ Laboratory of Molecular Biology and Genetic Engineering,
Allée du 6 Août, University of Liège,
4000 Sart-Tilman, Belgium
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