Calcineurin regulatory subunit is essential for virulence and mediates interactions with FKBP12-FK506 in Cryptococcus neoformans

Mol Microbiol. 2001 Feb;39(4):835-49. doi: 10.1046/j.1365-2958.2001.02295.x.

Abstract

Calcineurin is a Ca2+-calmodulin-regulated protein phosphatase that is the target of the immunosuppressive drugs cyclosporin A and FK506. Calcineurin is a heterodimer composed of a catalytic A and a regulatory B subunit. In previous studies, the calcineurin A homologue was identified and shown to be required for growth at 37 degrees C and hence for virulence of the pathogenic fungus Cryptococcus neoformans. Here, we identify the gene encoding the calcineurin B regulatory subunit and demonstrate that calcineurin B is also required for growth at elevated temperature and virulence. We show that the FKR1-1 mutation, which confers dominant FK506 resistance, results from a 6 bp duplication generating a two-amino-acid insertion in the latch region of calcineurin B. This mutation was found to reduce FKBP12-FK506 binding to calcineurin both in vivo and in vitro. Molecular modelling based on the FKBP12-FK506-calcineurin crystal structure illustrates how this mutation perturbs drug interactions with the phosphatase target. In summary, our studies reveal a central role for calcineurin B in virulence and antifungal drug action in the human fungal pathogen C. neoformans.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Base Sequence
  • Calcineurin / chemistry
  • Calcineurin / genetics
  • Calcineurin / metabolism*
  • Cryptococcosis / microbiology
  • Cryptococcus neoformans / genetics
  • Cryptococcus neoformans / growth & development
  • Cryptococcus neoformans / metabolism*
  • Cryptococcus neoformans / pathogenicity
  • DNA, Fungal
  • Disease Models, Animal
  • Fungal Proteins / chemistry
  • Fungal Proteins / genetics
  • Fungal Proteins / metabolism*
  • Genes, Fungal
  • Heating
  • Humans
  • Mice
  • Mice, Inbred DBA
  • Molecular Sequence Data
  • Mutagenesis
  • Protein Structure, Secondary
  • Recombination, Genetic
  • Sequence Homology, Amino Acid
  • Tacrolimus / chemistry
  • Tacrolimus / metabolism*
  • Tacrolimus Binding Protein 1A / chemistry
  • Tacrolimus Binding Protein 1A / metabolism*
  • Virulence

Substances

  • DNA, Fungal
  • Fungal Proteins
  • Calcineurin
  • Tacrolimus Binding Protein 1A
  • Tacrolimus

Associated data

  • GENBANK/AF282385
  • GENBANK/AF282386
  • GENBANK/AF282387
  • GENBANK/AF282388