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)

McRobie, Helen R. and King, Linda M. and Fanutti, Cristina and Symmons, Martyn F. and Coussons, Peter J. (2014) 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). FEBS Letters. ISSN 0014-5793

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Abstract

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.

Item Type: Journal Article
Additional Information: Citation: 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) 2014, 588 (14):2335 FEBS Letters.
Faculty: Faculty of Science & Technology
Depositing User: Mr I Walker
Date Deposited: 11 Mar 2015 11:31
Last Modified: 07 Jul 2016 12:52
URI: http://arro.anglia.ac.uk/id/eprint/346499

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