Chemogenomic profiling predicts antifungal synergies

Mol Syst Biol. 2009:5:338. doi: 10.1038/msb.2009.95. Epub 2009 Dec 22.

Abstract

Chemotherapies, HIV infections, and treatments to block organ transplant rejection are creating a population of immunocompromised individuals at serious risk of systemic fungal infections. Since single-agent therapies are susceptible to failure due to either inherent or acquired resistance, alternative therapeutic approaches such as multi-agent therapies are needed. We have developed a bioinformatics-driven approach that efficiently predicts compound synergy for such combinatorial therapies. The approach uses chemogenomic profiles in order to identify compound profiles that have a statistically significant degree of similarity to a fluconazole profile. The compounds identified were then experimentally verified to be synergistic with fluconazole and with each other, in both Saccharomyces cerevisiae and the fungal pathogen Candida albicans. Our method is therefore capable of accurately predicting compound synergy to aid the development of combinatorial antifungal therapies.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antifungal Agents / chemistry
  • Antifungal Agents / pharmacology*
  • Antifungal Agents / therapeutic use
  • Candida albicans / drug effects*
  • Candida albicans / genetics
  • Candida albicans / growth & development
  • Computational Biology*
  • Computer-Aided Design*
  • Dose-Response Relationship, Drug
  • Drug Design*
  • Drug Resistance, Fungal / genetics
  • Drug Synergism
  • Drug Therapy, Combination
  • Fluconazole / chemistry
  • Fluconazole / pharmacology*
  • Fluconazole / therapeutic use
  • Gene Expression Regulation, Fungal
  • Humans
  • Models, Molecular
  • Molecular Structure
  • Reproducibility of Results
  • Saccharomyces cerevisiae / drug effects*
  • Saccharomyces cerevisiae / genetics
  • Saccharomyces cerevisiae / growth & development
  • Structure-Activity Relationship

Substances

  • Antifungal Agents
  • Fluconazole