Genomic and in silico analyses of CRBN gene and thalidomide embryopathy in humans

Reprod Toxicol. 2016 Dec:66:99-106. doi: 10.1016/j.reprotox.2016.10.003. Epub 2016 Oct 14.

Abstract

Thalidomide causes Thalidomide Embryopathy (TE), but is largely used to treat several conditions. Investigations with Cereblon, a thalidomide target protein encoded by CRBN gene, have helped to understand thalidomide therapeutic and teratogenic properties. We sequenced CRBN-thalidomide binding region in 38 TE individuals and 136 Brazilians without congenital anomalies, and performed in silico analyses. Eight variants were identified, seven intronic and one in 3'UTR. TE individuals had rare variants in higher frequency than the non-affected group (p=0.04). The genotype rs1620675 CC was related to neurological anomalies in TE individuals (p=0.004). Bioinformatics analysis suggested this genotype leads to potential alterations in splicing sites and binding to transcription factors. Comparison of the Cereblon-thalidomide binding domains in mammals demonstrated that CRBN is highly conserved across species. All the variants require evaluation in functional assays in order to understand their role in Cereblon-thalidomide binding and complex interactions that lead to TE.

Keywords: CRBN; Cereblon; Teratogenesis; Thalidomide; Thalidomide embryopathy.

MeSH terms

  • Abnormalities, Drug-Induced / etiology
  • Abnormalities, Drug-Induced / genetics*
  • Abnormalities, Multiple / chemically induced
  • Abnormalities, Multiple / genetics*
  • Adaptor Proteins, Signal Transducing
  • Binding Sites
  • Brazil
  • Computer Simulation
  • Fetal Diseases / chemically induced
  • Fetal Diseases / genetics*
  • Genomics
  • Humans
  • Peptide Hydrolases / genetics*
  • Teratogens / toxicity*
  • Thalidomide / toxicity*
  • Ubiquitin-Protein Ligases

Substances

  • Adaptor Proteins, Signal Transducing
  • CRBN protein, human
  • Teratogens
  • Thalidomide
  • Ubiquitin-Protein Ligases
  • Peptide Hydrolases