Cellular models for the study of the pharmacology and signaling of melanin-concentrating hormone receptors

Cellular models for the study of the neuropeptide melanin-concentrating hormone (MCH) have become indispensable tools for pharmacological profiling and signaling analysis of MCH and its synthetic analogues. Although expression of MCH receptors is most abundant in the brain, MCH-R1 is also found in d...

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Bibliographic Details
Published in:Journal of receptors and signal transduction 2010-12, Vol.30 (6), p.385-402
Main Authors: Eberle, Alex N., Mild, Gabriele, Zumsteg, Urs
Format: Article
Language:English
Subjects:
Amino Acid Sequence
Animals
biochemical analysis
Cell Line
cell lines
expression
Humans
Hypothalamic Hormones - genetics
Hypothalamic Hormones - metabolism
MCH receptor
MCH-R
Melanins - genetics
Melanins - metabolism
Melanoma - metabolism
Melanoma - pathology
Models, Biological
Molecular Sequence Data
Molecular Structure
Pituitary Hormones - genetics
Pituitary Hormones - metabolism
Protein Isoforms - metabolism
Receptors, Pituitary Hormone - agonists
Receptors, Pituitary Hormone - antagonists & inhibitors
Receptors, Pituitary Hormone - metabolism
regulation
Signal Transduction - physiology
signaling
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Summary:Cellular models for the study of the neuropeptide melanin-concentrating hormone (MCH) have become indispensable tools for pharmacological profiling and signaling analysis of MCH and its synthetic analogues. Although expression of MCH receptors is most abundant in the brain, MCH-R1 is also found in different peripheral tissues. Therefore, not only cell lines derived from nervous tissue but also from peripheral tissues that naturally express MCH receptors have been used to study receptor signaling and regulation. For screening of novel compounds, however, heterologous expression of MCH-R1 or MCH-R2 genes in HEK293, Chinese hamster ovary, COS-7, or 3T3-L1 cells, or amplified MCH-R1 expression/signaling in IRM23 cells transfected with the Gq protein gene are the preferred tools because of more distinct pharmacological effects induced by MCH, which include inhibition of cAMP formation, stimulation of inositol triphosphate production, increase in intracellular free Ca2+ and/or activation of mitogen-activated protein kinases. Most of the published data originate from this type of model system, whereas data based on studies with cell lines endogenously expressing MCH receptors are more limited. This review presents an update on the different cellular models currently used for the analysis of MCH receptor interaction and signaling.
ISSN:1079-9893
1532-4281
DOI:10.3109/10799893.2010.524223