Targeting glycolysis in the malaria parasite Plasmodium falciparum

FEBS J. 2016 Feb;283(4):634-46. doi: 10.1111/febs.13615. Epub 2016 Jan 4.

Abstract

Glycolysis is the main pathway for ATP production in the malaria parasite Plasmodium falciparum and essential for its survival. Following a sensitivity analysis of a detailed kinetic model for glycolysis in the parasite, the glucose transport reaction was identified as the step whose activity needed to be inhibited to the least extent to result in a 50% reduction in glycolytic flux. In a subsequent inhibitor titration with cytochalasin B, we confirmed the model analysis experimentally and measured a flux control coefficient of 0.3 for the glucose transporter. In addition to the glucose transporter, the glucokinase and phosphofructokinase had high flux control coefficients, while for the ATPase a small negative flux control coefficient was predicted. In a broader comparative analysis of glycolytic models, we identified a weakness in the P. falciparum pathway design with respect to stability towards perturbations in the ATP demand.

Database: The mathematical model described here has been submitted to the JWS Online Cellular Systems Modelling Database and can be accessed at http://jjj.bio.vu.nl/database/vanniekerk1. The SEEK-study including the experimental data set is available at DOI 10.15490/seek.1.

Investigation: 56 (http://dx.doi.org/10.15490/seek.1.

Investigation: 56).

Keywords: drug target identification; glycolysis; mathematical model; metabolic control analysis; systems biology.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine Triphosphatases / antagonists & inhibitors
  • Adenosine Triphosphatases / metabolism
  • Adenosine Triphosphate / biosynthesis
  • Cytochalasin B / pharmacology
  • Glucose / antagonists & inhibitors
  • Glucose / metabolism
  • Glucose Transport Proteins, Facilitative / antagonists & inhibitors
  • Glucose Transport Proteins, Facilitative / metabolism
  • Glycolysis / drug effects*
  • Models, Molecular
  • Monte Carlo Method
  • Plasmodium falciparum / drug effects*
  • Plasmodium falciparum / enzymology
  • Plasmodium falciparum / metabolism*

Substances

  • Glucose Transport Proteins, Facilitative
  • Cytochalasin B
  • Adenosine Triphosphate
  • Adenosine Triphosphatases
  • Glucose