Defining the Contribution of MC1R Physiological Ligands to ATR Phosphorylation at Ser435, a Predictor of DNA Repair in Melanocytes

J Invest Dermatol. 2015 Dec;135(12):3086-3095. doi: 10.1038/jid.2015.280. Epub 2015 Jul 13.

Abstract

The melanocortin 1 receptor (MC1R), a GS-coupled receptor that signals through cAMP and protein kinase A (PKA), regulates pigmentation, adaptive tanning, and melanoma resistance. MC1R-cAMP signaling promotes PKA-mediated phosphorylation of ataxia telangiectasia and rad3-related (ATR) at Ser435 (ATR-pS435), a modification that enhances nucleotide excision repair (NER) by facilitating recruitment of the XPA protein to sites of UV-induced DNA damage. High-throughput methods were developed to quantify ATR-pS435, measure XPA-photodamage interactions, and assess NER function. We report that melanocyte-stimulating hormone (α-MSH) or ACTH induce ATR-pS435, enhance XPA's association with UV-damaged DNA and optimize melanocytic NER. In contrast, MC1R antagonists agouti signaling protein (ASIP) or human β-defensin 3 (HBD3) interfere with ATR-pS435 generation, impair the XPA-DNA interaction, and reduce DNA repair. Although ASIP and HBD3 each blocked α-MSH-mediated induction of the signaling pathway, only ASIP depleted basal ATR-pS435. Our findings confirm that ASIP diminishes agonist-independent MC1R basal signaling whereas HBD3 is a neutral MC1R antagonist that blocks activation by melanocortins. Furthermore, our data suggest that ATR-pS435 may be a useful biomarker for the DNA repair-deficient MC1R phenotype.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Agouti Signaling Protein / pharmacology
  • Ataxia Telangiectasia Mutated Proteins / metabolism
  • Biomarkers
  • Cells, Cultured
  • Cyclic AMP-Dependent Protein Kinases / physiology
  • DNA / metabolism
  • DNA Repair*
  • Humans
  • Melanocytes / metabolism*
  • Phosphorylation
  • Receptor, Melanocortin, Type 1 / physiology*
  • Serine / metabolism
  • Xeroderma Pigmentosum Group A Protein / metabolism
  • beta-Defensins / pharmacology

Substances

  • Agouti Signaling Protein
  • Biomarkers
  • DEFB103A protein, human
  • Receptor, Melanocortin, Type 1
  • XPA protein, human
  • Xeroderma Pigmentosum Group A Protein
  • beta-Defensins
  • Serine
  • DNA
  • ATR protein, human
  • Ataxia Telangiectasia Mutated Proteins
  • Cyclic AMP-Dependent Protein Kinases