Expression, Desensitization, and Internalization of the ACTH Receptor (MC2R)

: Research into the functions and mechanisms of action of the melanocortin 2 receptor (MC2R) has been severely hampered by difficulties in expressing this gene in heterologous cells. This probably arises because of the need for a cofactor for cell surface expression. Using either the Y1 cell line th...

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Bibliographic Details
Published in:Annals of the New York Academy of Sciences 2003-06, Vol.994 (1), p.111-117
Main Authors: CLARK, ADRIAN J.L., BAIG, ASMA H., NOON, LUKE, SWORDS, FRANCESCA M., HUNYADY, LASZLO, KING, PETER J.
Format: Article
Language:English
Subjects:
Adrenocorticotropic Hormone - metabolism
adrenocorticotropin
Animals
Cell Line
constitutive activity
Cyclic AMP - metabolism
Cyclic AMP-Dependent Protein Kinases - metabolism
desensitization
Endocytosis - physiology
G protein receptor kinase
G protein-coupled receptors
Humans
melanocortin 2 receptor
molecular chaperones
protein kinase A
receptor internalization
Receptor, Melanocortin, Type 2
Receptors, Corticotropin - genetics
Receptors, Corticotropin - metabolism
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Summary:: Research into the functions and mechanisms of action of the melanocortin 2 receptor (MC2R) has been severely hampered by difficulties in expressing this gene in heterologous cells. This probably arises because of the need for a cofactor for cell surface expression. Using either the Y1 cell line that expresses endogenous MC2R or the Y6 cell line that expresses this putative expression factor, we have explored the mechanisms of desensitization and internalization after agonist stimulation. Protein kinase A dependence of desensitization has been demonstrated, although internalization is apparently independent of this kinase and dependent on a G protein receptor kinase. Possible underlying reasons for this paradox are discussed.
ISSN:0077-8923
1749-6632
DOI:10.1111/j.1749-6632.2003.tb03169.x