Physiol. Genomics AJP: Gastrointestinal and Liver Physiology
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Physiol. Genomics 5: 11-19, 2001;
1094-8341/01 $5.00
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Received 7 October 1999; accepted in final form 21 November 2000.
Physiological Genomics 5:11-19 (2001)
1094-8341/01 $5.00 © 2001 American Physiological Society

Melanocortin receptor-mediated mobilization of intracellular free calcium in HEK293 cells

KATHLEEN G. MOUNTJOY1, PHILIP L. KONG1, JOHN A. TAYLOR2, DERRIL H. WILLARD3 and WILLIAM O. WILKISON3

1 Research Centre for Developmental Medicine and Biology, Department of Paediatrics
2 School of Biological Sciences, University of Auckland, Auckland 1, New Zealand
3 Glaxo Wellcome Research Institute, Research Triangle Park, North Carolina 27709

Mouse melanocortin receptors, MC1-R, MC3-R, MC4-R, and MC5-R, when expressed in HEK293 cells and stimulated with either {alpha}-melanocyte-stimulating hormone ({alpha}-MSH) or desacetyl-{alpha}-MSH, mediate increases in intracellular free calcium concentration ([Ca2+]i) with EC50 values between 0.3 and 4.3 nM. The increase in [Ca2+]i is cholera toxin sensitive and pertussis toxin insensitive. The mechanism involves calcium mobilization from intracellular stores without a transient rise in inositol trisphosphate. Mouse agouti protein (55 nM) is a competitive antagonist of {alpha}-MSH (6-fold) and desacetyl-{alpha}-MSH (8-fold), coupling the mMC1-R to increased [Ca2+]i. Agouti protein (55 nM) significantly increased the EC50 for {alpha}-MSH (3-fold), and 550 nM agouti protein significantly increased the EC50 for desacetyl-{alpha}-MSH (4-fold), coupling the mMC4-R to a rise in [Ca2+]i. However, agouti protein antagonism of the MC4-R may not be competitive since there was a trend for the maximum response to also increase. There was no significant antagonism of the MC3-R and MC5-R by agouti protein (55 nM). Understanding the physiological relevance of the transduction of a calcium signal by melanocortin peptides may be important for future development of therapeutic targeting of the melanocortin receptors.

agouti; desacetyl-{alpha}-melanocyte-stimulating hormone; {alpha}-melanocyte-stimulating hormone




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