JAK1/3 inhibition preserves epidermal morphology in full-thickness 3D skin models of atopic dermatitis and psoriasis

J Eur Acad Dermatol Venereol. 2019 Feb;33(2):367-375. doi: 10.1111/jdv.15301. Epub 2019 Jan 1.

Abstract

Background: Janus kinase (JAK) inhibition may be a promising new treatment modality for inflammatory (skin) diseases. However, little is known about direct effects of kinase inhibitors on keratinocyte differentiation and function as well as skin barrier formation.

Objective: Our aim was to address the direct impact of kinase inhibition of the JAK1/3 pathways by tofacitinib on keratinocyte immune function and barrier formation in atopic dermatitis (AD) and psoriasis.

Methods: 3D skin equivalents of both diseases were developed and concurrently pretreated with tofacitinib. To induce AD, 3D skin equivalents were stimulated with recombinant human IL-4 and IL-13. Psoriasis-like conditions were induced by incubation with IL-17A, IL-22 and tumour necrosis factor α (TNFα). The activation of signal transducer and activator of transcription (STAT)1, STAT3 and STAT6 was assessed by Western blot analysis. Microarray analysis and quantitative real-time PCR were used for gene expression analysis.

Results: Tofacitinib pretreatment preserved epidermal morphology and reduced STAT3 and STAT6 phosphorylation of AD-like and STAT3 phosphorylation of psoriasis-like culture conditions in 3D skin models compared to sham-controls. Filaggrin expression was fully maintained in the AD-like models, but only partially in psoriasis-like conditions after pretreatment with tofacitinib. In addition, tofacitinib upregulated DSC1, FLG and KRT1. Using gene expression analysis, downregulation of POSTN and IL24 was observed in AD-like conditions, whereas downregulation of IL20 and IL1B was observed in psoriasis-like conditions.

Conclusion: JAK1/3 inhibition counteracted cytokine-induced AD- and psoriasis-like epidermal morphology and enhanced keratinocyte differentiation in 3D skin models. This effect was more pronounced in the AD-like models compared to the psoriasis-like 3D skin models.

Publication types

  • Comparative Study

MeSH terms

  • Cell Proliferation / drug effects
  • Computer Simulation
  • Dermatitis, Atopic / drug therapy
  • Dermatitis, Atopic / pathology*
  • Filaggrin Proteins
  • Humans
  • Imaging, Three-Dimensional*
  • Intermediate Filament Proteins / pharmacology*
  • Janus Kinase 1 / drug effects*
  • Keratinocytes / cytology
  • Keratinocytes / drug effects
  • Piperidines / pharmacology*
  • Psoriasis / drug therapy
  • Psoriasis / pathology*
  • Pyrimidines / pharmacology*
  • Pyrroles / pharmacology*
  • STAT6 Transcription Factor / drug effects
  • Sensitivity and Specificity

Substances

  • FLG protein, human
  • Filaggrin Proteins
  • Intermediate Filament Proteins
  • Piperidines
  • Pyrimidines
  • Pyrroles
  • STAT6 Transcription Factor
  • STAT6 protein, human
  • tofacitinib
  • JAK1 protein, human
  • Janus Kinase 1