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Molecular and pharmacological characterization of the melanocortin type 1 receptor in the sea bass

Other TitlesSea bass MC1R
AuthorsSánchez, Elisa ; Rubio, V. C.; Cerdá-Reverter, José Miguel
KeywordsMelanocortin receptor 1 (MC1R)
Agouti-related protein (AGRP)
Constitutive activity
Inverse agonism
Phosphodiesterase inhibitor
Issue DateJan-2010
Academic Press
CitationGeneral and Comparative Endocrinology 165(1): 163-169 (2010)
AbstractMelanocortin 1 receptor (MC1R) plays a key role in the physiology of the vertebrate pigment system. Point mutations producing hyperactive or inactive receptors result in darkening or paling effects, respectively. We report the molecular and pharmacological characterization, as well as the tissue expression pattern, of the sea bass Mc1r. Similar to other MC1Rs, the sea bass gene is highly polymorphic and nine DNA polymorphisms, seven of them involving an amino acid substitution, were detected. SbMc1r is mainly expressed in the testis, fat and liver with moderate levels in the ventral and dorsal skin. The sea bass receptor was activated by all the melanocortins tested, with ACTH showing the lowest efficiency. The acetylation level of the MSH isoforms seems to be critical for the effectively of the agonist. Agouti-related protein (AGRP) drastically inhibited the basal activity of the receptor in vitro, as an inverse agonist does, but only in the presence of phosphodiesterase inhibitors. This observation suggests that sbMc1r is constitutively activated and inversely regulated by AGRP, which is expressed in the skin of different fish species.
Description28 p., figuras y bibliografía
Publisher version (URL)http://dx.doi.org/10.1016/j.ygcen.2009.06.008
Appears in Collections:(IATS) Artículos
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