The first crystal structure of phosphofructokinase from a eukaryote: Trypanosoma brucei

J Mol Biol. 2007 Mar 2;366(4):1185-98. doi: 10.1016/j.jmb.2006.10.019. Epub 2006 Oct 11.

Abstract

The crystal structure of the ATP-dependent phosphofructokinase (PFK) from Trypanosoma brucei provides the first detailed description of a eukaryotic PFK, and enables comparisons to be made with the crystal structures of bacterial ATP-dependent and PPi-dependent PFKs. The structure reveals that two insertions (the 17-20 and 329-348 loops) that are characteristic of trypanosomatid PFKs, but absent from bacterial and mammalian ATP-dependent PFKs, are located within and adjacent to the active site, and are in positions to play important roles in the enzyme's mechanism. The 90 residue N-terminal extension forms a novel domain that includes an "embracing arm" across the subunit boundary to the symmetry-related subunit in the tetrameric enzyme. Comparisons with the PPi-dependent PFK from Borrelia burgdorferi show that several features thought to be characteristic of PPi-dependent PFKs are present in the trypanosome ATP-dependent PFK. These two enzymes are generally more similar to each other than to the bacterial or mammalian ATP-dependent PFKs. However, there are critical differences at the active site of PPi-dependent PFKs that are sufficient to prevent the binding of ATP. This crystal structure of a eukaryotic PFK has enabled us to propose a detailed model of human muscle PFK that shows active site and other differences that offer opportunities for structure-based drug discovery for the treatment of sleeping sickness and other diseases caused by the trypanosomatid family of protozoan parasites.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adenosine Triphosphate / pharmacology
  • Amino Acid Sequence
  • Animals
  • Binding Sites
  • Crystallization
  • Diphosphates / pharmacology
  • Humans
  • Molecular Sequence Data
  • Phosphofructokinases / chemistry*
  • Phosphofructokinases / genetics
  • Protein Structure, Quaternary
  • Protein Structure, Tertiary
  • Sequence Homology, Amino Acid
  • Structure-Activity Relationship
  • Trypanosoma brucei brucei / enzymology*
  • X-Ray Diffraction

Substances

  • Diphosphates
  • Adenosine Triphosphate
  • Phosphofructokinases

Associated data

  • PDB/2HIG