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Marine Toxins Targeting Kv1 Channels: Pharmacological Tools and Therapeutic Scaffolds

Illawarra Health and Medical Research Institute, University of Wollongong, Wollongong, NSW 2522, Australia
Electrophysiology Facility for Cell Phenotyping and Drug Discovery, Wollongong, NSW 2522, Australia
College of Engineering and Technology, American University of the Middle East, Kuwait
School of Food Science and Environmental Health, College of Sciences and Health, Technological University Dublin, D07 ADY7 Dublin, Ireland
Authors to whom correspondence should be addressed.
These authors contributed equally to this review.
Mar. Drugs 2020, 18(3), 173;
Received: 3 February 2020 / Revised: 15 March 2020 / Accepted: 16 March 2020 / Published: 20 March 2020
(This article belongs to the Special Issue Ion Channels as Marine Drug Targets)
Toxins from marine animals provide molecular tools for the study of many ion channels, including mammalian voltage-gated potassium channels of the Kv1 family. Selectivity profiling and molecular investigation of these toxins have contributed to the development of novel drug leads with therapeutic potential for the treatment of ion channel-related diseases or channelopathies. Here, we review specific peptide and small-molecule marine toxins modulating Kv1 channels and thus cover recent findings of bioactives found in the venoms of marine Gastropod (cone snails), Cnidarian (sea anemones), and small compounds from cyanobacteria. Furthermore, we discuss pivotal advancements at exploiting the interaction of κM-conotoxin RIIIJ and heteromeric Kv1.1/1.2 channels as prevalent neuronal Kv complex. RIIIJ’s exquisite Kv1 subtype selectivity underpins a novel and facile functional classification of large-diameter dorsal root ganglion neurons. The vast potential of marine toxins warrants further collaborative efforts and high-throughput approaches aimed at the discovery and profiling of Kv1-targeted bioactives, which will greatly accelerate the development of a thorough molecular toolbox and much-needed therapeutics. View Full-Text
Keywords: bioactives; conotoxins 2; Kv1; marine toxins; modulators; potassium channels; sea anemone toxins bioactives; conotoxins 2; Kv1; marine toxins; modulators; potassium channels; sea anemone toxins
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MDPI and ACS Style

Finol-Urdaneta, R.K.; Belovanovic, A.; Micic-Vicovac, M.; Kinsella, G.K.; McArthur, J.R.; Al-Sabi, A. Marine Toxins Targeting Kv1 Channels: Pharmacological Tools and Therapeutic Scaffolds. Mar. Drugs 2020, 18, 173.

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