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Melanocortin 1 Receptor (MC1R): Potentials as Therapeutic Targets

Yoon Woo Mun, Woo Hyun Kim, Dongyun Shin2023Preprints.orgPreprint
10.20944/preprints202305.1558.v1Free full text
DermatologicalImmune/Innate

Abstract

Melanocortins play crucial roles in regulating the stress response, inflammation, and skin pigmentation. In this review, we focus on the melanocortin 1 receptor (MC1R), a G protein-coupled receptor primarily known for regulating skin pigmentation and exhibiting anti-inflammatory effects. First, we provide an overview of the structure, signaling pathways, and related diseases of MC1R. Next, we discuss the potential therapeutic use of synthetic peptides and small molecule modulators of MC1R, highlighting the development of various drugs that enhance stability through amino acid sequence modifications and small molecule drugs to overcome limitations associated with peptide characteristics. Notably, MC1R-targeted drugs have applications beyond skin pigmentation-related diseases, which predominantly affect MC1R in melanocytes. These drugs can also be useful in treating inflammatory diseases with MC1R expression present in various cells. Our review underscores the potential of MC1R-targeted drugs to treat a wide range of diseases and encourages further research in this area.

Cited By (1)

  • Antimicrobial Neuropeptides and Their Receptors: Immunoregulator and Therapeutic Targets for Immune DisordersMolecules · 2025

References (6)

  • Targeting melanocortin receptors as a novel strategy to control inflammationPharmacological Reviews · 2004
  • α-Melanocyte Stimulating Hormone Prevents Lipopolysaccharide-Induced Vasculitis by Down-Regulating Endothelial Cell Adhesion Molecule ExpressionEndocrinology · 2003
  • Melanocortin peptides inhibit production of proinflammatory cytokines and nitric oxide by activated microgliaJournal of Leukocyte Biology · 1998
  • Activation of MC1R with BMS-470539 attenuates neuroinflammation via cAMP/PKA/Nurr1 pathway after neonatal hypoxic-ischemic brain injury in ratsJournal of Neuroinflammation · 2021
  • Structural mechanism of calcium-mediated hormone recognition and Gβ interaction by the human melanocortin-1 receptorCell Research · 2021

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