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Conotoxins as Tools to Understand the Physiological Function of Voltage-Gated Calcium (Ca(V)) Channels
Voltage-gated calcium (Ca(V)) 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...
Autores principales: | , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2017
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5666421/ https://www.ncbi.nlm.nih.gov/pubmed/29027927 http://dx.doi.org/10.3390/md15100313 |
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author | Ramírez, David Gonzalez, Wendy Fissore, Rafael A. Carvacho, Ingrid |
author_facet | Ramírez, David Gonzalez, Wendy Fissore, Rafael A. Carvacho, Ingrid |
author_sort | Ramírez, David |
collection | PubMed |
description | Voltage-gated calcium (Ca(V)) 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. Ca(V) channels are divided into two groups depending on the membrane potential required to activate them: High-voltage activated (HVA, Ca(V)1.1–1.4; Ca(V)2.1–2.3) and Low-voltage activated (LVA, Ca(V)3.1–3.3). 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. |
format | Online Article Text |
id | pubmed-5666421 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2017 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-56664212017-11-09 Conotoxins as Tools to Understand the Physiological Function of Voltage-Gated Calcium (Ca(V)) Channels Ramírez, David Gonzalez, Wendy Fissore, Rafael A. Carvacho, Ingrid Mar Drugs Review Voltage-gated calcium (Ca(V)) 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. Ca(V) channels are divided into two groups depending on the membrane potential required to activate them: High-voltage activated (HVA, Ca(V)1.1–1.4; Ca(V)2.1–2.3) and Low-voltage activated (LVA, Ca(V)3.1–3.3). 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. MDPI 2017-10-13 /pmc/articles/PMC5666421/ /pubmed/29027927 http://dx.doi.org/10.3390/md15100313 Text en © 2017 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Review Ramírez, David Gonzalez, Wendy Fissore, Rafael A. Carvacho, Ingrid Conotoxins as Tools to Understand the Physiological Function of Voltage-Gated Calcium (Ca(V)) Channels |
title | Conotoxins as Tools to Understand the Physiological Function of Voltage-Gated Calcium (Ca(V)) Channels |
title_full | Conotoxins as Tools to Understand the Physiological Function of Voltage-Gated Calcium (Ca(V)) Channels |
title_fullStr | Conotoxins as Tools to Understand the Physiological Function of Voltage-Gated Calcium (Ca(V)) Channels |
title_full_unstemmed | Conotoxins as Tools to Understand the Physiological Function of Voltage-Gated Calcium (Ca(V)) Channels |
title_short | Conotoxins as Tools to Understand the Physiological Function of Voltage-Gated Calcium (Ca(V)) Channels |
title_sort | conotoxins as tools to understand the physiological function of voltage-gated calcium (ca(v)) channels |
topic | Review |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5666421/ https://www.ncbi.nlm.nih.gov/pubmed/29027927 http://dx.doi.org/10.3390/md15100313 |
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