An ion-channel modulator from the saliva of the brown ear tick has a highly modified Kunitz/BPTI structure

J Mol Biol. 2009 Jun 19;389(4):734-47. doi: 10.1016/j.jmb.2009.04.045. Epub 2009 Apr 24.

Abstract

Ra-KLP, a 75 amino acid protein secreted by the salivary gland of the brown ear tick Rhipicephalus appendiculatus has a sequence resembling those of Kunitz/BPTI proteins. We report the detection, purification and characterization of the function of Ra-KLP. In addition, determination of the three-dimensional crystal structure of Ra-KLP at 1.6 A resolution using sulphur single-wavelength anomalous dispersion reveals that much of the loop structure of classical Kunitz domains, including the protruding protease-binding loop, has been replaced by beta-strands. Even more unusually, the N-terminal portion of the polypeptide chain is pinned to the "Kunitz head" by two disulphide bridges not found in classical Kunitz/BPTI proteins. The disulphide bond pattern has been further altered by the loss of the bridge that normally stabilizes the protease-binding loop. Consistent with the conversion of this loop into a beta-strand, Ra-KLP shows no significant anti-protease activity; however, it activates maxiK channels in an in vitro system, suggesting a potential mechanism for regulating host blood supply during feeding.

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Aprotinin / chemistry*
  • Aprotinin / classification
  • Aprotinin / genetics
  • Aprotinin / metabolism
  • Cell Line
  • Crystallography, X-Ray
  • Dimerization
  • Evolution, Molecular
  • Humans
  • Ion Channels / metabolism*
  • Models, Molecular
  • Molecular Sequence Data
  • Patch-Clamp Techniques
  • Phylogeny
  • Protein Structure, Secondary
  • Protein Structure, Tertiary*
  • Rhipicephalus / chemistry*
  • Saliva / chemistry*
  • Sequence Alignment
  • Sequence Homology, Amino Acid

Substances

  • Ion Channels
  • Aprotinin

Associated data

  • GENBANK/FJ042889
  • PDB/2W8X
  • PDB/R2W8XSF