Biochemical Characterization of MurF from Streptococcus pneumoniae and the Identification of a New MurF Inhibitor Through Ligand-based Virtual Screening

Authors

  • Samo Turk Faculty of Pharmacy, University of Ljubljana, Aškerčeva 7, 1000 Ljubljana, Slovenia.
  • Martina Hrast Faculty of Pharmacy, University of Ljubljana, Aškerčeva 7, 1000 Ljubljana, Slovenia.
  • Izidor Sosič Faculty of Pharmacy, University of Ljubljana, Aškerčeva 7, 1000 Ljubljana, Slovenia.
  • Hélčne Barreteau University Paris-Sud, Enveloppes Bactériennes et Antibiotiques, IBBMC, UMR 8619 CNRS, 91405 Orsay, France.
  • Dominique Mengin-Lecreulx University Paris-Sud, Enveloppes Bactériennes et Antibiotiques, IBBMC, UMR 8619 CNRS, 91405 Orsay, France.
  • Didier Blanot University Paris-Sud, Enveloppes Bactériennes et Antibiotiques, IBBMC, UMR 8619 CNRS, 91405 Orsay, France.
  • Stanislav Gobec Faculty of Pharmacy, University of Ljubljana, Aškerčeva 7, 1000 Ljubljana, Slovenia.

Keywords:

MurF, peptidoglycan, Streptococcus pneumoniae, ligand-based virtual screening

Abstract

MurF is an essential bacterial enzyme that is involved in the last intracellular stage of peptidoglycan biosynthesis, and therefore it has the potential to be exploited as a target for the development of new antibacterials. Here, we report on the expression, purification and biochemical characterization of MurF from an important pathogen, Streptococcus pneumoniae. Additionally, ligand-based virtual screening was successfully used and a new hit compound with micromolar inhibitory activities against MurF enzymes from S. pneumoniae and Escherichia coli was identified.

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Published

28.10.2013

Issue

Vol. 60 No. 2 (2013)

Section

Biochemistry and molecular biology

License

Except where otherwise noted, articles in this journal are published under the Creative Commons Attribution 4.0 International License