ArticleThe Journal of investigative dermatology2012
Defining MC1R regulation in human melanocytes by its agonist α-melanocortin and antagonists agouti signaling protein and β-defensin 3.
Article in The Journal of investigative dermatology, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 52 papers.
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Who cites it
52 citing papers in PubMed, 95 citations in OpenAlex.
- Review
- The Genetics and Evolution of Human Pigmentation.Biology · 2025Review
- An overview of benefits and risks of chronic melanocortin-1 receptor activation.Journal of the European Academy of Dermatology and Venereology : JEADV · 2025Review
- Journey through the spectacular landscape of melanocortin 1 receptor.Pigment cell & melanoma research · 2024Review
- Distinct cAMP Signaling Microdomains Differentially Regulate Melanosomal pH and Pigmentation.The Journal of investigative dermatology · 2023Article
- Melanocortin 1 Receptor (MC1R): Pharmacological and Therapeutic Aspects.International journal of molecular sciences · 2023Review
- MC1R and melanin-based molecular probes for theranostic of melanoma and beyond.Acta pharmacologica Sinica · 2022Review
- The potential impact of melanosomal pH and metabolism on melanoma.Frontiers in oncology · 2022Review
- Implications of Oxidative Stress in the Pathogenesis and Treatment of Hyperpigmentation Disorders.Oxidative medicine and cellular longevity · 2022Review
- Review
- Pharmacologic manipulation of skin pigmentation.Pigment cell & melanoma research · 2021Review
- Participation of keratinocyte- and fibroblast-derived factors in melanocyte homeostasis, the response to UV, and pigmentary disorders.Pigment cell & melanoma research · 2021Review
- Melanocortin 1 receptor is dispensable for acute stress induced hair graying in mice.Experimental dermatology · 2021Article
- Activation of MC1R with BMS-470539 attenuates neuroinflammation via cAMP/PKA/Nurr1 pathway after neonatal hypoxic-ischemic brain injury in rats.Journal of neuroinflammation · 2021Article
- Article
- Cyclic adenosine monophosphate (cAMP) signaling in melanocyte pigmentation and melanomagenesis.Pigment cell & melanoma research · 2021Review
- Up- or Downregulation of Melanin Synthesis Using Amino Acids, Peptides, and Their Analogs.Biomedicines · 2020Review
- Elucidation of Melanogenesis Cascade for Identifying Pathophysiology and Therapeutic Approach of Pigmentary Disorders and Melanoma.International journal of molecular sciences · 2020Review
- NB-UVB Induces Melanocytic Differentiation of Human Hair Follicle Neural Crest Stem Cells.Annals of dermatology · 2020Article
- Peptide Hormone Regulation of DNA Damage Responses.Endocrine reviews · 2020Review
Corrections and comments
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Authors and funding
11 authors at 3 institutions in 1 country.
Funding
Abstract
The melanocortin 1 receptor (MC1R), a G(s) protein-coupled receptor, has an important role in human pigmentation. We investigated the regulation of expression and activity of the MC1R in primary human melanocyte cultures. Human β-defensin 3 (HBD3) acted as an antagonist for MC1R, inhibiting the α-melanocortin (α-melanocyte-stimulating hormone (α-MSH))-induced increase in the activities of adenylate cyclase and tyrosinase, the rate-limiting enzyme for melanogenesis. α-Melanocortin and forskolin, which activate adenylate cyclase, and 12-O-tetradecanoylphorbol-13-acetate, which activates protein kinase C, increased, whereas exposure to UV radiation reduced, MC1R gene and membrane protein expression. Brief treatment with α-MSH resulted in MC1R desensitization, whereas continuous treatment up to 3 hours caused a steady rise in cAMP, suggesting receptor recycling. Pretreatment with agouti signaling protein or HBD3 prohibited responsiveness to α-MSH, but not forskolin, suggesting receptor desensitization by these antagonists. Melanocytes from different donors expressed different levels of the G protein-coupled receptor kinases (GRKs) 2, 3, 5, and 6, as well as β-arrestin 1. Therefore, in addition to the MC1R genotype, regulation of MC1R expression and activity is expected to affect human pigmentation and the responses to UV.
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Registered trials
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