The 1.85 A structure of an 8R-lipoxygenase suggests a general model for lipoxygenase product specificity

Biochemistry. 2009 Aug 25;48(33):7906-15. doi: 10.1021/bi900084m.

Abstract

Lipoxygenases (LOX) play pivotal roles in the biosynthesis of leukotrienes and other biologically active eicosanoids derived from arachidonic acid. A mechanistic understanding of substrate recognition, when lipoxygenases that recognize the same substrate generate different products, can be used to help guide the design of enzyme-specific inhibitors. We report here the 1.85 A resolution structure of an 8R-lipoxygenase from Plexaura homomalla, an enzyme with a sequence approximately 40% identical to that of human 5-LOX. The structure reveals a U-shaped channel, defined by invariant amino acids, that would allow substrate access to the catalytic iron. We demonstrate that mutations within the channel significantly impact enzyme activity and propose a novel model for substrate binding potentially applicable to other members of this enzyme family.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Anthozoa / enzymology*
  • Binding Sites
  • Crystallography, X-Ray
  • Enzyme Activation
  • Humans
  • Intramolecular Oxidoreductases / chemistry*
  • Intramolecular Oxidoreductases / genetics
  • Lipoxygenase / chemistry*
  • Lipoxygenase / genetics
  • Models, Chemical*
  • Models, Molecular*
  • Molecular Sequence Data
  • Mutagenesis, Site-Directed
  • Stereoisomerism
  • Substrate Specificity

Substances

  • Lipoxygenase
  • Intramolecular Oxidoreductases
  • hydroperoxide isomerase

Associated data

  • PDB/2FNQ
  • PDB/3FG1
  • PDB/3FG3
  • PDB/3FG4