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Journal of Receptors and Signal Transduction Volume 27, 2007 - Issue 4
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Research Article

The Hepatocarcinoma Cell Line HepG2 Does Not Express a GHS-R1a-Type Ghrelin Receptor

LEEN THIELEMANS Department of Internal Medicine, Johnson & Johnson Pharmaceutical Research & Development, a division of Janssen Pharmaceutica NV, Beerse, Belgium
,
PIETER J. PEETERS Department of Internal Medicine, Johnson & Johnson Pharmaceutical Research & Development, a division of Janssen Pharmaceutica NV, Beerse, Belgium
,
HEIDI JONCKHEERE IriDM Corporation, Leuven, Belgium
,
WALTER LUYTEN IriDM Corporation, Leuven, Belgium
,
RONALD DE HOOGT Department of Internal Medicine, Johnson & Johnson Pharmaceutical Research & Development, a division of Janssen Pharmaceutica NV, Beerse, Belgium
,
BERNARD COULIE Department of Internal Medicine, Johnson & Johnson Pharmaceutical Research & Development, a division of Janssen Pharmaceutica NV, Beerse, Belgium
&
JEROEN AERSSENS Department of Internal Medicine, Johnson & Johnson Pharmaceutical Research & Development, a division of Janssen Pharmaceutica NV, Beerse, Belgium
 show all
Pages 309-322 | Published online: 10 Oct 2008
 
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Abstract

The interaction of ghrelin, a 28-residue acylated peptide, with the growth hormone secretagogue receptor 1a (GHS-R1a) has been studied mostly in cells expressing a recombinant GHS-R1a. As awareness is growing on the importance to study G protein-coupled receptors in a natural environment, we studied the effect of ghrelin in the human hepatocellular HepG2 cell line because it has been described in literature to respond to ghrelin. Despite extensive efforts, we were not able to confirm mRNA expression of GHS-R1a by reverse transcription PCR, radioligand binding, or ghrelin-induced GHS-R1a receptor activation; therefore, we conclude that HepG2 cells do not express GHS-R1a. On the other hand, we confirmed a modest effect of ghrelin on the up-regulation of IRS-1 phosphorylation, which might suggest the existence of an alternative ghrelin receptor in HepG2 cells.

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