Identification of the nuclear receptor DAF-12 as a therapeutic target in parasitic nematodes

Proc Natl Acad Sci U S A. 2009 Jun 9;106(23):9138-43. doi: 10.1073/pnas.0904064106. Epub 2009 Jun 2.

Abstract

Nematode parasitism is a worldwide health problem resulting in malnutrition and morbidity in over 1 billion people. The molecular mechanisms governing infection are poorly understood. Here, we report that an evolutionarily conserved nuclear hormone receptor signaling pathway governs development of the stage 3 infective larvae (iL3) in several nematode parasites, including Strongyloides stercoralis, Ancylostoma spp., and Necator americanus. As in the free-living Caenorhabditis elegans, steroid hormone-like dafachronic acids induced recovery of the dauer-like iL3 in parasitic nematodes by activating orthologs of the nuclear receptor DAF-12. Moreover, administration of dafachronic acid markedly reduced the pathogenic iL3 population in S. stercoralis, indicating the potential use of DAF-12 ligands to treat disseminated strongyloidiasis. To understand the pharmacology of targeting DAF-12, we solved the 3-dimensional structure of the S. stercoralis DAF-12 ligand-binding domain cocrystallized with dafachronic acids. These results reveal the molecular basis for DAF-12 ligand binding and identify nuclear receptors as unique therapeutic targets in parasitic nematodes.

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

  • Ancylostoma / metabolism*
  • Animals
  • Caenorhabditis elegans / metabolism
  • Caenorhabditis elegans Proteins / chemistry
  • Caenorhabditis elegans Proteins / metabolism
  • Cell Line
  • Cholestenes / metabolism
  • Crystallography, X-Ray
  • Humans
  • Larva
  • Models, Molecular
  • Necator americanus / metabolism*
  • Protein Structure, Tertiary
  • Receptors, Cytoplasmic and Nuclear / antagonists & inhibitors*
  • Receptors, Cytoplasmic and Nuclear / chemistry
  • Receptors, Cytoplasmic and Nuclear / metabolism*
  • Steroids / metabolism
  • Strongylida Infections / drug therapy
  • Strongylida Infections / parasitology*
  • Strongyloides stercoralis / metabolism*

Substances

  • Caenorhabditis elegans Proteins
  • Cholestenes
  • DAF-12 protein, C elegans
  • Receptors, Cytoplasmic and Nuclear
  • Steroids
  • dafachronic acid

Associated data

  • PDB/3GYT
  • PDB/3GYU