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Conotoxins as tools to understand the physiological function of voltage-gated calcium (ca-v) channels
- Source :
- Marine Drugs, Artículos CONICYT, CONICYT Chile, instacron:CONICYT, Marine Drugs, Vol 15, Iss 10, p 313 (2017)
- Publication Year :
- 2017
-
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.
- Subjects :
- 0301 basic medicine
Pharmaceutical Science
chemistry.chemical_element
Cellular homeostasis
Calcium
Pharmacology
Biology
conotoxins
03 medical and health sciences
0302 clinical medicine
Drug Discovery
Conotoxin
Receptor
lcsh:QH301-705.5
Pharmacology, Toxicology and Pharmaceutics (miscellaneous)
Ion channel
Membrane potential
Voltage-gated ion channel
Voltage-dependent calcium channel
Cell biology
030104 developmental biology
lcsh:Biology (General)
chemistry
ω-conotoxin structure
voltage-gated calcium (CaV) channels
therapeutic potential
030217 neurology & neurosurgery
Subjects
Details
- Language :
- English
- Database :
- OpenAIRE
- Journal :
- Marine Drugs, Artículos CONICYT, CONICYT Chile, instacron:CONICYT, Marine Drugs, Vol 15, Iss 10, p 313 (2017)
- Accession number :
- edsair.doi.dedup.....f866d2e8937f07e1626819cfcef44443