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Mar. Drugs 2017, 15(10), 313; https://doi.org/10.3390/md15100313

Conotoxins as Tools to Understand the Physiological Function of Voltage-Gated Calcium (CaV) Channels

1
Centro de Bioinformática y Simulación Molecular, Universidad de Talca, 3460000 Talca, Chile
2
Instituto de Ciencias Biomédicas, Universidad Autónoma de Chile, 3460000 Talca, Chile
3
Millennium Nucleus of Ion Channels-Associated Diseases (MiNICAD), Universidad de Talca, 3460000 Talca, Chile
4
Department of Veterinary and Animal Sciences, University of Massachusetts, Amherst, MA 01003, USA
5
Department of Biology and Chemistry, Faculty of Basic Sciences, Universidad Católica del Maule, 3480112 Talca, Chile
*
Author to whom correspondence should be addressed.
Received: 8 August 2017 / Revised: 6 September 2017 / Accepted: 4 October 2017 / Published: 13 October 2017
(This article belongs to the Special Issue Marine Drugs and Ion Currents)
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Abstract

Voltage-gated calcium (CaV) channels are widely expressed and are essential for the completion of multiple physiological processes. Close regulation of their activity by specific inhibitors and agonists become fundamental to understand their role in cellular homeostasis as well as in human tissues and organs. CaV channels are divided into two groups depending on the membrane potential required to activate them: High-voltage activated (HVA, CaV1.1–1.4; CaV2.1–2.3) and Low-voltage activated (LVA, CaV3.1–3.3). HVA channels are highly expressed in brain (neurons), heart, and adrenal medulla (chromaffin cells), among others, and are also classified into subtypes which can be distinguished using pharmacological approaches. Cone snails are marine gastropods that capture their prey by injecting venom, “conopeptides”, which cause paralysis in a few seconds. A subset of conopeptides called conotoxins are relatively small polypeptides, rich in disulfide bonds, that target ion channels, transporters and receptors localized at the neuromuscular system of the animal target. In this review, we describe the structure and properties of conotoxins that selectively block HVA calcium channels. We compare their potency on several HVA channel subtypes, emphasizing neuronal calcium channels. Lastly, we analyze recent advances in the therapeutic use of conotoxins for medical treatments. View Full-Text
Keywords: conotoxins; voltage-gated calcium (CaV) channels; ω-conotoxin structure; therapeutic potential conotoxins; voltage-gated calcium (CaV) channels; ω-conotoxin structure; therapeutic potential
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).
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Ramírez, D.; Gonzalez, W.; Fissore, R.A.; Carvacho, I. Conotoxins as Tools to Understand the Physiological Function of Voltage-Gated Calcium (CaV) Channels. Mar. Drugs 2017, 15, 313.

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