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1 Institut de Pharmacologie Moléculaire et Cellulaire (IPMC), CNRS UMR 6097, Sophia-Antipolis, 06560 Valbonne, France
2 Architecture et Fonction des Macromolécules Biologiques (AFMB), CNRS UMR 6098 and Universités d’Aix-Marseille I and II, 13402 Marseille Cedex 20, France
3 Université Pierre et Marie Curie, Paris, France
Reprint requests to: Hervé Darbon, UMR 6098, CNRS, 31 ch. Joseph Aiguier, F-13402, Marseille Cedex 20, France; e-mail: herve{at}afmb.cnrs-mrs.fr; fax: 33 (0)4-91-16-45-36; or Michel Lazdunski, IPMC-CNRS, 660 Route des Lucioles, F-06560, Valbonne, France; e-mail: ipmc{at}ipmc.cnrs.fr; fax: 33 (0)4-93-95-77-04.
Acid-sensing ion channels (ASICs) are thought to be important ion channels, particularly for the perception of pain. Some of them may also contribute to synaptic plasticity, learning, and memory. Psalmotoxin 1 (PcTx1), the first potent and specific blocker of the ASIC1a proton-sensing channel, has been successfully expressed in the Drosophila melanogaster S2 cell recombinant expression system used here for the first time to produce a spider toxin. The recombinant toxin was identical in all respects to the native peptide, and its three-dimensional structure in solution was determined by means of 1H 2D NMR spectroscopy. Surface characteristics of PcTx1 provide insights on key structural elements involved in the binding of PcTx1 to ASIC1a channels. They appear to be localized in the ß-sheet and the ß-turn linking the strands, as indicated by electrostatic anisotropy calculations, surface charge distribution, and the presence of residues known to be implicated in channel recognition by other inhibitor cystine knot (ICK) toxins.
Keywords: Spider toxin; NMR structure; ASIC; ICK motif
Abbreviations: PcTx1, psalmotoxin 1 • NOESY, nuclear Overhauser effect spectroscopy • TOCSY, total correlation spectroscopy • COSY, correlation spectroscopy • CNS, crystallography and NMR system • ICK, inhibitor cystine knot
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