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Full-Text Articles in Physiology
Melanocortin 1 Receptor: Structure, Function, And Regulation, Erin M. Wolf Horrell, Mary C. Boulanger, John A. D'Orazio
Melanocortin 1 Receptor: Structure, Function, And Regulation, Erin M. Wolf Horrell, Mary C. Boulanger, John A. D'Orazio
Physiology Faculty Publications
The melanocortin 1 receptor (MC1R) is a melanocytic Gs protein coupled receptor that regulates skin pigmentation, UV responses, and melanoma risk. It is a highly polymorphic gene, and loss of function correlates with a fair, UV-sensitive, and melanoma-prone phenotype due to defective epidermal melanization and sub-optimal DNA repair. MC1R signaling, achieved through adenylyl cyclase activation and generation of the second messenger cAMP, is hormonally controlled by the positive agonist melanocortin, the negative agonist agouti signaling protein, and the neutral antagonist β-defensin 3. Activation of cAMP signaling up-regulates melanin production and deposition in the epidermis which functions to limit UV …