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Conotoxins as tools to understand the physiological function of voltage-gated calcium (CaV) channels

dc.contributor.authorRamírez D.
dc.contributor.authorGonzalez W.
dc.contributor.authorFissore R.A.
dc.contributor.authorCarvacho I.
dc.date.accessioned2020-09-02T22:26:32Z
dc.date.available2020-09-02T22:26:32Z
dc.date.issued2017
dc.identifier10.3390/md15100313
dc.identifier.citation15, 10, -
dc.identifier.issn16603397
dc.identifier.urihttps://hdl.handle.net/20.500.12728/5951
dc.descriptionVoltage-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. © 2017 by the authors.
dc.language.isoen
dc.publisherMDPI AG
dc.subjectConotoxins
dc.subjectTherapeutic potential
dc.subjectVoltage-gated calcium (CaV) channels
dc.subjectω-conotoxin structure
dc.subjectalpha conotoxin
dc.subjectchi conotoxin
dc.subjectconotoxin
dc.subjectdelta conotoxin
dc.subjectepsilon conotoxin
dc.subjectgamma conotoxin
dc.subjectiota conotoxin
dc.subjectkappa conotoxin
dc.subjectmu conotoxin
dc.subjectomega conotoxin
dc.subjectomega conotoxin CVID
dc.subjectomega conotoxin MVIIA
dc.subjectrho conotoxin
dc.subjectsigma conotoxin
dc.subjecttau conotoxin
dc.subjectunclassified drug
dc.subjectvoltage gated calcium channel
dc.subjectcalcium channel
dc.subjectcalcium channel blocking agent
dc.subjectconotoxin
dc.subjectadrenal medulla
dc.subjectbrain nerve cell
dc.subjectchromaffin cell
dc.subjectchronic pain
dc.subjectdisulfide bond
dc.subjectdrug activity
dc.subjectdrug potency
dc.subjectdrug structure
dc.subjectheart
dc.subjecthomeostasis
dc.subjecthuman
dc.subjectmembrane potential
dc.subjectnonhuman
dc.subjectpharmacological blocking
dc.subjectprotein expression
dc.subjectprotein function
dc.subjectReview
dc.subjectsnail
dc.subjectanimal
dc.subjectchemistry
dc.subjectdrug effect
dc.subjectmetabolism
dc.subjectAnimals
dc.subjectCalcium Channel Blockers
dc.subjectCalcium Channels
dc.subjectConotoxins
dc.subjectHumans
dc.subjectMembrane Potentials
dc.subjectSnails
dc.titleConotoxins as tools to understand the physiological function of voltage-gated calcium (CaV) channels
dc.typeReview


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