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Agouti signalling protein is an inverse agonist to the wildtype and agonist to the melanic variant of the melanocortin‐1 receptor in the grey squirrel ( Sciurus carolinensis )
Author(s) -
McRobie Helen R.,
King Linda M.,
Fanutti Cristina,
Symmons Martyn F.,
Coussons Peter J.
Publication year - 2014
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/j.febslet.2014.05.032
Subject(s) - melanocortin 1 receptor , sciurus carolinensis , agonist , inverse agonist , melanocortin , receptor , biology , basal (medicine) , mutant , endocrinology , medicine , wild type , genetics , phenotype , gene , zoology , insulin
The melanocortin‐1 receptor (MC1R) is a key regulator of mammalian pigmentation. Melanism in the grey squirrel is associated with an eight amino acid deletion in the mutant melanocortin‐1 receptor with 24 base pair deletion (MC1RΔ24) variant. We demonstrate that the MC1RΔ24 exhibits a higher basal activity than the wildtype MC1R (MC1R‐wt). We demonstrate that agouti signalling protein (ASIP) is an inverse agonist to the MC1R‐wt but is an agonist to the MC1RΔ24. We conclude that the deletion in the MC1RΔ24 leads to a receptor with a high basal activity which is further activated by ASIP. This is the first report of ASIP acting as an agonist to MC1R.