Complex approach for analysis of snake venom α-neurotoxins binding to HAP, the high-affinity peptide

Sci Rep. 2020 Mar 2;10(1):3861. doi: 10.1038/s41598-020-60768-y.

Abstract

Snake venom α-neurotoxins, invaluable pharmacological tools, bind with high affinity to distinct subtypes of nicotinic acetylcholine receptor. The combinatorial high-affinity peptide (HAP), homologous to the C-loop of α1 and α7 nAChR subunits, binds biotinylated α-bungarotoxin (αBgt) with nanomolar affinity and might be a protection against snake-bites. Since there are no data on HAP interaction with other toxins, we checked its binding of α-cobratoxin (αCtx), similar to αBgt in action on nAChRs. Using radioiodinated αBgt, we confirmed a high affinity of HAP for αBgt, the complex formation is supported by mass spectrometry and gel chromatography, but only weak binding was registered with αCtx. A combination of protein intrinsic fluorescence measurements with the principal component analysis of the spectra allowed us to measure the HAP-αBgt binding constant directly (29 nM). These methods also confirmed weak HAP interaction with αCtx (>10000 nM). We attempted to enhance it by modification of HAP structure relying on the known structures of α-neurotoxins with various targets and applying molecular dynamics. A series of HAP analogues have been synthesized, HAP[L9E] analogue being considerably more potent than HAP in αCtx binding (7000 nM). The proposed combination of experimental and computational approaches appears promising for analysis of various peptide-protein interactions.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Bungarotoxins / chemistry*
  • Cobra Neurotoxin Proteins / chemistry*
  • Molecular Dynamics Simulation*
  • Neurotoxins / chemistry*
  • Peptides / chemistry*
  • Protein Binding
  • Protein Structure, Secondary
  • alpha7 Nicotinic Acetylcholine Receptor / chemistry*

Substances

  • Bungarotoxins
  • Cobra Neurotoxin Proteins
  • Neurotoxins
  • Peptides
  • alpha7 Nicotinic Acetylcholine Receptor
  • alpha-cobratoxin