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Submitted on January 26, 2007
Accepted on April 30, 2007
Laboratory for Molecular Pharmacology, Department of Neuroscience and Pharmacology and Department of Biomedical Sciences, University of Copenhagen, Blegdamsvej 3, DK-2200 Copenhagen N, Denmark; Department of Neuroscience, Karolinska Institutet, 171 77 Stockholm, Sweden; 7TM Pharma A/S; Fremtidsvej 3, DK-2790, Hoersholm, Denmark
* To whom correspondence should be addressed. E-mail: schwartz{at}molpharm.dk.
GPR39 is a constitutively active, orphan member of the ghrelin receptor family, which is activated by zinc ions. GPR39 is here described to be expressed in a full length, biologically active 7TM form, GPR39-1a, as well as in a truncated splice variant 5TM form, GPR39-1b. The 3' exon of the GPR39 gene overlaps with an antisense gene called LYPD1. Quantitative RT-PCR (QPCR) analysis demonstrated that GPR39-1a is expressed selectively throughout the GI-tract including the liver and pancreas as well as in the kidney and adipose tissue; whereas the truncated GPR39-1b form has a more broad expression pattern including the CNS but with highest expression in the stomach and small intestine. In contrast, the LYPD1 antisense gene is highly expressed throughout the CNS as characterized with both QPCR and in situ hybridization analysis. A functional analysis of the GPR39 promoter region identified sites for the HNF-1
, HNF-4, and SP1 transcription factors as being important for the expression of GPR39. In vivo experiments in rats demonstrated that GPR39 is upregulated in adipose tissue upon fasting and in response to streptozotocin treatment, while its expression is kept constant in the liver from the same animals. GPR39-1a was expressed in white but not brown adipose tissue and was down-regulated during adipocyte differentiation of fibroblasts. It is concluded that the transcriptional control mechanism, the tissue expression pattern, and in vivo response to physiological stimuli all indicate that the GPR39 receptor very likely is of importance for the function of a number of metabolic organs including the liver, GI-tract, pancreas and adipose tissue.
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