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Open AccessArticle

Characterisation of a Novel A-Superfamily Conotoxin

1
Centre for Molecular Therapeutics, Australian Institute of Tropical Health and Medicine, James Cook University, Smithfield, QLD 4878, Australia
2
Centre for Pain Research, Institute for Molecular Bioscience, The University of Queensland, St Lucia, QLD 4072, Australia
3
School of Pharmacy, The University of Queensland, Woolloongabba, QLD 4102, Australia
4
Walther Straub Institute of Pharmacology and Toxicology, Faculty of Medicine, LMU Munich, Nußbaumstraße 26, 80336 Munich, Germany
5
Institut des Biomolécules Max Mousseron, UMR 5247, Université de Montpellier, CNRS, 34095 Montpellier, France
*
Author to whom correspondence should be addressed.
Biomedicines 2020, 8(5), 128; https://doi.org/10.3390/biomedicines8050128
Received: 3 May 2020 / Revised: 15 May 2020 / Accepted: 18 May 2020 / Published: 20 May 2020
(This article belongs to the Special Issue Animal Venoms–Curse or Cure?)
Conopeptides belonging to the A-superfamily from the venomous molluscs, Conus, are typically α-conotoxins. The α-conotoxins are of interest as therapeutic leads and pharmacological tools due to their selectivity and potency at nicotinic acetylcholine receptor (nAChR) subtypes. Structurally, the α-conotoxins have a consensus fold containing two conserved disulfide bonds that define the two-loop framework and brace a helical region. Here we report on a novel α-conotoxin Pl168, identified from the transcriptome of Conus planorbis, which has an unusual 4/8 loop framework. Unexpectedly, NMR determination of its three-dimensional structure reveals a new structural type of A-superfamily conotoxins with a different disulfide-stabilized fold, despite containing the conserved cysteine framework and disulfide connectivity of classical α-conotoxins. The peptide did not demonstrate activity on a range of nAChRs, or Ca2+ and Na+ channels suggesting that it might represent a new pharmacological class of conotoxins. View Full-Text
Keywords: conopeptide; NMR spectroscopy; disulfide framework conopeptide; NMR spectroscopy; disulfide framework
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MDPI and ACS Style

Wilson, D.T.; Bansal, P.S.; Carter, D.A.; Vetter, I.; Nicke, A.; Dutertre, S.; Daly, N.L. Characterisation of a Novel A-Superfamily Conotoxin. Biomedicines 2020, 8, 128.

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