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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)
- Publication Year :
- 2014
- Publisher :
- Wiley, 2014.
-
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.
- Subjects :
- CAMP Responsive Element Binding Protein
Agonist
medicine.medical_specialty
medicine.drug_class
Biophysics
Second Messenger Systems
Biochemistry
chemistry.chemical_compound
Melanocyte stimulating hormone
Melanocortin-1 receptor
Structural Biology
Internal medicine
Cyclic AMP
Genetics
medicine
Animals
Humans
Inverse agonist
Receptor
Melanism
Molecular Biology
Sequence Deletion
Sciurus carolinensis
biology
Wild type
Sciuridae
Grey squirrel
Cell Biology
biology.organism_classification
Molecular biology
alpha-Melanocyte-stimulating hormone
HEK293 Cells
Endocrinology
chemistry
Agouti signalling protein
Agouti Signaling Protein
Receptor, Melanocortin, Type 1
Melanocortin 1 receptor
Subjects
Details
- Language :
- English
- ISSN :
- 18733468
- Database :
- OpenAIRE
- Accession number :
- edsair.doi.dedup.....77673f8d0b98ffaf7409cc3ed1c373a5