Molecular analysis, pathogenic mechanisms, and readthrough therapy on a large cohort of Kabuki syndrome patients

Hum Mutat. 2014 Jul;35(7):841-50. doi: 10.1002/humu.22547. Epub 2014 Apr 9.

Abstract

Kabuki syndrome (KS) is a multiple congenital anomalies syndrome characterized by characteristic facial features and varying degrees of mental retardation, caused by mutations in KMT2D/MLL2 and KDM6A/UTX genes. In this study, we performed a mutational screening on 303 Kabuki patients by direct sequencing, MLPA, and quantitative PCR identifying 133 KMT2D, 62 never described before, and four KDM6A mutations, three of them are novel. We found that a number of KMT2D truncating mutations result in mRNA degradation through the nonsense-mediated mRNA decay, contributing to protein haploinsufficiency. Furthermore, we demonstrated that the reduction of KMT2D protein level in patients' lymphoblastoid and skin fibroblast cell lines carrying KMT2D-truncating mutations affects the expression levels of known KMT2D target genes. Finally, we hypothesized that the KS patients may benefit from a readthrough therapy to restore physiological levels of KMT2D and KDM6A proteins. To assess this, we performed a proof-of-principle study on 14 KMT2D and two KDM6A nonsense mutations using specific compounds that mediate translational readthrough and thereby stimulate the re-expression of full-length functional proteins. Our experimental data showed that both KMT2D and KDM6A nonsense mutations displayed high levels of readthrough in response to gentamicin treatment, paving the way to further studies aimed at eventually treating some Kabuki patients with readthrough inducers.

Keywords: KDM6A; KMT2D; Kabuki syndrome; haploinsufficiency; readthrough.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Abnormalities, Multiple / drug therapy
  • Abnormalities, Multiple / genetics*
  • Cell Line
  • Codon, Nonsense / drug effects
  • Cohort Studies
  • DNA Mutational Analysis
  • DNA-Binding Proteins / genetics
  • DNA-Binding Proteins / metabolism
  • Face / abnormalities*
  • Gene Expression
  • Gene Expression Regulation / drug effects
  • Genetic Association Studies
  • Gentamicins / pharmacology
  • Gentamicins / therapeutic use
  • Haploinsufficiency
  • Hematologic Diseases / drug therapy
  • Hematologic Diseases / genetics*
  • Histone Demethylases / genetics
  • Homeodomain Proteins / genetics
  • Humans
  • Mutation
  • Neoplasm Proteins / genetics
  • Neoplasm Proteins / metabolism
  • Nonsense Mediated mRNA Decay
  • Nuclear Proteins / genetics
  • RNA Splice Sites
  • Sequence Analysis, DNA
  • Transcription, Genetic
  • Vestibular Diseases / drug therapy
  • Vestibular Diseases / genetics*

Substances

  • Codon, Nonsense
  • DNA-Binding Proteins
  • Gentamicins
  • HOXC6 protein, human
  • Homeodomain Proteins
  • KMT2D protein, human
  • Neoplasm Proteins
  • Nuclear Proteins
  • RNA Splice Sites
  • Histone Demethylases
  • KDM6A protein, human

Supplementary concepts

  • Kabuki syndrome