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Open AccessArticle

New Insights into the Type II Toxins from the Sea Anemone Heteractis crispa

G.B. Elyakov Pacific Institute of Bioorganic Chemistry, Far Eastern Branch of the Russian Academy of Science, 690022 Vladivostok, Russia
Toxicology and Pharmacology, University of Leuven (KU Leuven), Campus Gasthuisberg, O&N 2, Herestraat~49, P.O. Box 922, 3000 Leuven, Belgium
Authors to whom correspondence should be addressed.
These two authors contribute equally to this work.
Toxins 2020, 12(1), 44; (registering DOI)
Received: 16 December 2019 / Revised: 7 January 2020 / Accepted: 8 January 2020 / Published: 10 January 2020
(This article belongs to the Special Issue Venoms and Ion Channels)
Toxins modulating NaV channels are the most abundant and studied peptide components of sea anemone venom. Three type-II toxins, δ-SHTX-Hcr1f (= RpII), RTX-III, and RTX-VI, were isolated from the sea anemone Heteractis crispa. RTX-VI has been found to be an unusual analog of RTX-III. The electrophysiological effects of Heteractis toxins on nine NaV subtypes were investigated for the first time. Heteractis toxins mainly affect the inactivation of the mammalian NaV channels expressed in the central nervous system (NaV1.1–NaV1.3, NaV1.6) as well as insect and arachnid channels (BgNaV1, VdNaV1). The absence of Arg13 in the RTX-VI structure does not prevent toxin binding with the channel but it has changed its pharmacological profile and potency. According to computer modeling data, the δ-SHTX-Hcr1f binds within the extracellular region of the rNaV1.2 voltage-sensing domain IV and pore-forming domain I through a network of strong interactions, and an additional fixation of the toxin at the channel binding site is carried out through the phospholipid environment. Our data suggest that Heteractis toxins could be used as molecular tools for NaV channel studies or insecticides rather than as pharmacological agents. View Full-Text
Keywords: sea anemone; type II toxins; voltage-gated sodium channels; electrophysiology sea anemone; type II toxins; voltage-gated sodium channels; electrophysiology
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Kalina, R.S.; Peigneur, S.; Zelepuga, E.A.; Dmitrenok, P.S.; Kvetkina, A.N.; Kim, N.Y.; Leychenko, E.V.; Tytgat, J.; Kozlovskaya, E.P.; Monastyrnaya, M.M.; Gladkikh, I.N. New Insights into the Type II Toxins from the Sea Anemone Heteractis crispa. Toxins 2020, 12, 44.

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